rexresearch.com
Euphorbia peplus [ Milkwood ] vs Cancer
http://www.dailymail.co.uk/health/article-1350454/Milkweed-miracle-Applying-sap-common-garden-weed-cure-skin-cancer.html
26th January 2011
Common garden weed 'cures skin cancer', say scientists
by Jenny Hope
A common weed could help cure skin cancers, claim researchers.
The sap from a plant known as petty spurge or milkweed [ * a typo -- actually, it's " milkwood " ] - found by roadsides and in woodland - can 'kill' certain types of cancer cells when applied to the skin.
It works on non-melanoma skin cancers, which affect hundreds of thousands of Britons each year.
They are triggered by sun damage and, although not usually fatal, can be disfiguring without treatment.
The plant has been used for centuries as a traditional folk medicine to treat conditions such as warts, asthma and several types of cancer.
But for the first time a team of scientists in Australia has carried out a clinical study of sap from Euphorbia peplus, which is related to Euphorbia plants grown in gardens in the UK.
The study of 36 patients with a total of 48 non-melanoma lesions included basal cell carcinomas (BCC), squamous cell carcinomas (SCC) and intraepidermal carcinomas (IEC), a growth of cancerous cells confined to the outer layer of the skin.
Patients had failed to respond to conventional treatment including surgery, or they refused or were unsuitable for surgery because of their age.
The patients were treated once a day for three consecutive days by an oncologist using a cotton bud to apply enough of the E.peplus sap to cover the surface of each lesion.
The initial results were impressive, says findings to be released this week in the British Journal of Dermatology.
After only one month 41 of the 48 cancers had completely gone.
Patients who had some of the lesions remaining were offered a second course of treatment.
After an average of 15 months following treatment, two thirds of the 48 skin cancer lesions were still showing a complete response.
Of the three types of skin cancer tested, the final outcome was a 75 per cent complete response for IEC lesions, 57 per cent for BCC and 50 per cent for SCC lesions.
Side-effects were low, with 43 per cent of patients in no pain as a result of the treatment and only 14 per cent reporting moderate pain, and only one patient encountered severe short-term pain.
In all cases of successful treatment the skin was left with a good cosmetic appearance.
The researchers, from a number of medical institutions in Brisbane, attribute the benefit to the active ingredient ingenol mebutate which has been shown to destroy tumour cells.
British experts said further studies were needed and people should not try this at home as the weed sap can be harmful to the eyes and should not be eaten.
More than 76,500 people are diagnosed with non-melanoma skin cancer in the UK each year, with 90 per cent caused by ultraviolet light exposure.
Lesions usually appear on the areas most exposed to the sun, such as the head, neck, ears, and back of the hands.
Kimberley Carter of the British Association of Dermatologists said: 'This is a very small test group so it will be interesting to see what larger studies and the development of the active ingredient in E. peplus sap will reveal.
'Whilst it would not provide an alternative to surgery for the more invasive skin cancers or melanoma, in the future it might become a useful addition to the treatments available to patients for superficial, non-melanoma skin cancers.
'Any advances that could lead to new therapies for patients where surgery is not an option are definitely worth investigating.
'It is also very important to note that this is definitely not a treatment people should be trying out at home.
'Exposure of the sap to mucous producing surfaces, such as the eyes, results in extreme inflammation and can lead to hospitalisation.
'The concentration of the active ingredients in the sap also varies between different plants, with high doses able to cause very severe and excessive inflammatory responses.'
Euphorbia peplus : Petty Spurge, Milkwood
http://www.gardenorganic.org.uk
PETTY SPURGE, OR MILKWOOD
Latin name: Euphorbia peplus
Occurrence: Petty spurge is a small, branched annual, plentiful in gardens and arable fields.
It is native and common throughout the UK, in any kind of soil. The plant exudes a milky sap when damaged, which is a severe irritant if applied to the skin.
Biology: Petty spurge flowers from April to November. The seed number per plant ranges from 260 to 1,200.
Petty spurge may be found in fruit for eight months of the year. Seedlings emerge throughout the year except for in winter but the main flush is from April to May. Most seed germinates within a year of shedding.
Just a few seedlings emerge in the following 5 years. Germination occurs at 5 to 10 mm depth in soil.
Persistence and Spread: Seed recovered from house demolitions and archaeological digs and dated at 20, 25, 30 and 100 years old has been reported to germinate.
http://www.wikipedia.org
Euphorbia peplus
Not to be confused with Euphorbia peplis, Purple spurge, a relatively rare plant of coastal sand and shingle.
Scientific classification
Kingdom: Plantae
Division: Magnoliophyta
Class: Magnoliopsida
Order: Malpighiales
Family: Euphorbiaceae
Genus: Euphorbia
Species: E. peplus
Binomial name : Euphorbia peplus L.
Euphorbia peplus (Petty spurge, Radium weed[1] or Cancer weed[2]) is a species of Euphorbia, native to most of Europe, northern Africa, and western Asia, where it typically grows in cultivated arable land, gardens, and other disturbed land.[3][4][5]
It is an annual plant growing to between 5–30 cm tall (most plants growing as weeds of cultivation tend towards the smaller end), with smooth hairless stems. The leaves are oval-acute, 1–3 cm long, with a smooth margin. It has green flowers in three-rayed umbels. The glands, typical of the Euphorbiacae, are kidney-shaped with long thin horns.[5]
The milky latex sap is toxic, and used as a therapeutic agent for the removal of warts and sunspots on the skin.[1] Recent work also suggests that it may also be effective in treating superficial basal cell carcinomas.[6][7]
Outside of its native range it is very widely naturalised and often invasive, including in Australia, New Zealand, North America, and other countries in temperate and sub-tropical regions.[3]
References
1. http://www.beautanicals.com.au/Petty%20spurge.html
2. http://www.environmentalweedsactionnetwork.org.au/images/pdf/EterracinaWorkshopText.pdf
3. Germplasm Resources Information Network: Euphorbia peplus
4. Flora Europaea: Euphorbia peplus
5. Blamey, M. & Grey-Wilson, C. (1989). Flora of Britain and Northern Europe. ISBN 0-340-40170-2
6. Goliath:Skin and Allergy News Sep 07: Plant-based compound shows efficacy against basal cell cs
7. The Age May 06: Peplin cancer gel shows promise
http://plantmed.blogspot.com/2004_02_01_archive.html
February 24, 2004
Other alternative skin cancer treatments
The white sap of petty spurge (Euphorbia peplus), also called cancer weed or radium weed, is excellent on skin cancers and insensitive external tumors. Skin cancers may also be destroyed by repeatedly applying a drop of 35% hydrogen peroxide, preferably protecting the surrounding skin with a barrier cream.
However, the most effective way to remove skin cancer, melanoma and tumors close to the skin, possibly including breast tumors, is to apply an 'Escharotic'. These are caustic remedies, commonly with zinc chloride and the herb bloodroot as main ingredients. These may be available from some health shops or naturopaths. Skin cancers may become inflamed for a few days and then form dry pus (an eschar) and fall out after about 10 days.
Before you rush out to buy the stuff, read this abstract on [negative] Consequences of using escharotic agents as primary treatment for nonmelanoma skin cancer.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12472348&dopt=Abstract
Instructions for using Euphorbia peplus (petty spurge) - more from Australia
Do not get in eye
from email: [it has] different effects on different areas of the body... ...usually apply Betadine (Iodine) if any infection appears present. Typically (on the face eg) the spot will become "angry" looking, and break out into a weeping type sore. You may also see a line or "lines" moving out from the spot. These also may breakout through the skin. Both areas of reaction may take 2-3 weeks to settle, and scab over, and it can look quite messy for a while. Past this point, the area should start to heal and return to normal without the cancer. Applying the sap daily for 3-4 days followed by every 2nd-3rd day may be a better approach for some people. Certainly, reactions can vary from person to person but the biggest risk is from secondary infection and it is surprising how many people miss this point.
United States Patent Application 20090292017
THERAPEUTIC COMPOSITIONS
Brown; Marc Barry ; et al./ November 26, 2009
Abstract
Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.
Inventors: Brown; Marc Barry; (Watford, GB) ; Crowthers; Michael Edward Donald; (Hillsborough, GB) ; Nazir; Tahir; (Isleworth, GB)
Description
[0001] The present invention relates to compositions of compounds obtainable from Euphorbia species and which are useful in the treatment of skin cancers.
[0002] The compound ingenol angelate can be isolated from various Euphorbia species, and particularly from Euphorbia peplus and Euphorbia drummondii. Ingenol angelate exists in three isoforms; ingenol-3-angelate (isoform `b`), ingenol-5-angelate (isoform `a`) and ingenol-20-angelate (isoform `c`). The first of these is also referred to herein as I3A and has the following structure:
##STR00001##
[0003] Ingenol angelate has been found to be highly toxic for skin cancer cells via rapid mitochondrial disruption and cell death by primary necrosis, while leaving healthy cells unaffected.
[0004] U.S. Pat. No. 6,432,452 discloses compounds present in an active principle derived from plants of the species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, which show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). The compounds are selected from jatrophanes, pepluanes, paralianes and ingenanes. The preferred compound is an angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus.
[0005] Microgram quantities of ingenol angelate are typically therapeutically effective. However, the tendency for isoform `b` to undergo rearrangement to isoform `a` and subsequently to isoform `c` presents a formulation problem, where it is desired to restrict the formulation to either a specific isoform or to a ratio of isoforms. This is particularly a problem with I3A, as the different isoforms have different solubilities.
[0006] There is a need for an effective, topical treatment for skin cancer, as systemic treatments involving other drugs necessarily result in exposure of susceptible healthy cells, in non-target parts of the body, to cytotoxic chemicals. In addition, systemic anti-cancer treatments, whether administered orally or by injection, have lower patient acceptance.
[0007] There is a need to provide a stable formulation of ingenol angelate, preferably for topical administration.
[0008] It has now, surprisingly, been found that ingenol angelate can be solubilised, substantially without rearrangement between isoforms, in an acceptable, aprotic solvent in the presence of an acceptable, miscible acidic buffer.
[0009] Thus, in a first aspect, the present invention provides a formulation of ingenol angelate for use in therapy, wherein the ingenol angelate has been dissolved in a pharmaceutically acceptable, aprotic solvent, said formulation further comprising a pharmaceutically acceptable acidifying agent which is at least partially compatible with the solvent and which provides the formulation with an apparent pH of no greater than 4.5.
[0010] The present invention envisages formulations of any of the isoforms of ingenol angelate, or mixtures thereof. At present, the preferred isoform is isoform `b`, also referred to herein as I3A. It will be understood that references to `ingenol angelate` and `I3A` include reference to other isoforms and mixtures thereof, unless otherwise apparent.
[0011] Ingenol angelate can be dissolved in many solvents, and various solvents are illustrated in accompanying Example 1. However, ingenol angelate is generally susceptible to rearrangement in protic solvents, and any substantial degree of rearrangement, typically beyond about 1% for plant derived products, but more preferably about 0.5%, is undesirable in a pharmaceutical formulation.
[0012] In aprotic solvents, which are generally solvents that do not contribute protons to a solution, such as polyethylene glycol, dissolution can take some considerable time and this, together with the temperatures required, can also lead to rearrangement to an extent above acceptable levels.
[0013] Substances such as acetone and acetonitrile are capable of dissolving I3A, but are not generally pharmaceutically acceptable, and may not be suitable for long term storage. More acceptable may be substances such as methyl ethyl ketone, ethyl acetate, or diethyl ether, but benzyl alcohol is generally most preferred.
[0014] A number of substances are suitable to dissolve I3A, but stability is not guaranteed, and generally unacceptable rearrangement levels may be observed after periods ranging between as little as 12 hours and as much as six months or a year.
[0015] In the absence of water, or other protic solvent, there will not be a measurable pH. Under such conditions, and especially at elevated temperatures, rearrangement is likely. Thus, it has been found that it is generally possible to inhibit rearrangement by the presence of a suitable acid.
[0016] Suitable acids are generally organic acids, as it has been established that I3A can decompose much below about a pH of 3, while rearrangement is likely to occur at above a pH of about 4.5. Where it is intended to store the formulation for periods of any length, such as a month or more, then it is preferred that the acid be in the form of a buffer. Suitable buffers include citrate buffer, phosphate buffer, acetate buffer and citrate-phosphate buffer, although other buffers will be apparent to those skilled in the art. In particular, it is preferred that the buffer provides an apparent pH to the formulation of no greater than 4.5 and no less than 2.5. A formulation pH of less than 4 is more preferred, and it is particularly preferred that the apparent formulation pH be 3.8 or less, preferably around 3.5, or less. An apparent pH of around 3 is useful. A buffer having a pH of 2.75 has been found to be particularly advantageous, conferring an apparent pH of about pH 3.5 to the final formulation when used in quantities as illustrated in the accompanying Examples. A preferred pH range of the buffer is between 2.6 and 2.85, preferably pH 2.7-pH 2.8, and is preferably a citrate buffer. It will be appreciated that the acid will generally be in the form of an aqueous solution, preferably in deionised water, unless otherwise indicated. Citrate buffer is preferred. Where acetate buffer is used, this may typically have a pH range of 3.5 to 5.5, while citrate-phosphate buffer may typically have a pH range of 2.75 to 7.0.
[0017] It will be understood that a solution in which the solvent is aprotic cannot have a pH, as this is a measurement of the H.sup.+ ion. However, where such a solution is at least partially miscible with an acid, or acidic buffer, and such is present, then attempts to measure the pH will yield a result. Preferred formulations of the invention are made up as topical administration forms, and will generally comprise a majority of buffer, or ionic solution, but will always comprise aprotic solvent, so that only an apparent, rather than an absolute, pH can be measured, as the measured pH relates only to the ionic component. A suitable means for measuring apparent pH is with the Jenway 3320 pH meter. Accordingly, the result may not have the meaning normally ascribed to an ionic solution, especially where the amount of acid or buffer is small, but the significance is that, insofar as any ionic environment is present, that environment is acidic. As the amount of acid increases, so the apparent pH becomes more equivalent to pH. While not being bound by theory, it is likely that ingenol angelate is primarily dissolved in the aprotic solvent, as it has very low solubility in water. Subsequent addition of the ingenol angelate solution in solvent to an acidified ionic solution allows a suitable, optionally aqueous, ionic solution of ingenol angelate to be prepared, thereby avoiding dissolution of ingenol angelate directly in a protic solvent, which is when the greatest amount of rearrangement appears to take place. Thus, contact with a protic solvent can immediately result in the formation of the other isoforms, but this can be minimised if a small amount of acid or acidic buffer, which terms are used synonymously herein unless otherwise apparent, is added. Even the act of dissolution in protic solvents, given the length of time and conditions necessary, can lead to undesirably high levels of isoforms forming, such is the susceptibility of ingenol angelate to rearrangement.
[0018] The aprotic solvent and the acid are at least partially compatible, in that a stable preparation of the two can be formed. The acid and solvent are preferably miscible, and are preferably miscible at all ratios. In particular, it is generally preferred to add a small amount of buffer to the solvent during, or shortly after, solubilisation of the ingenol angelate, in order to keep the apparent pH at a relatively low level. Subsequently, it may be desirable to make up the solubilised ingenol angelate in an excess of the buffer that was used during the initial solubilisation. Stable preparations made up with an excess of buffer are illustrated in Example 9, below.
[0019] It will be appreciated that it is preferred that the acid and solvent be sufficiently miscible to be able to form a single phase, although immiscible, or less miscible, solvents and acids may be prepared in the form of emulsions or micro-emulsions. Such emulsions can be stable, but the provision of a mixture of solvent and acid as a single phase generally further minimises any risk of angelate rearrangement.
[0020] Solvents that are particularly useful in the present invention are those which exhibit both hydrophilic and lipophilic traits, such as ring systems which are preferably homocyclic, and which have hydroxy groups substituted thereon but separated by at least one carbon atom from the ring structure. A particularly preferred example of such a solvent is benzyl alcohol.
[0021] Although it is possible to use an acid rather than a buffer, it is generally preferred to use an acidic buffer to minimise the fluctuation in pH. As such, it will be appreciated that, whilst the term `buffer` will generally be used herein, this term also encompasses acids and acid preparations, where appropriate. A particularly preferred buffer is citrate buffer, pH 3 or lower, preferably pH 2.75. In benzyl alcohol, a 2.5% w/w quantity of pH 2.5 citrate buffer will generally yield an unmeasurable apparent pH but, at higher quantities, yields a pH of around pH 3. The relationship between pH of buffer and apparent pH is explored in the accompanying Examples. At low quantities of buffer when dissolving I3A in the solvent, it is simply preferred to keep the environment acidic, and the nature of the preferred buffer at these levels is similar to the nature of the preferred buffer when subsequently diluting the formulation for use. It is generally preferred to acidify the solvent, preferably benzyl alcohol, with an amount of acidic buffer, preferably between 1 and 10% by weight, more preferably between 2 and 5%, prior to addition of I3A.
[0022] While the formulation does not have to be diluted for use, it is generally the case that I3A is a potent substance, and stock solutions of I3A in solvent, preferably benzyl alcohol, may be made up for storage, preferably at 8.degree. C. or below. Such stock solutions may then be diluted, preferably with buffer, as desired, when making up any final formulation or preparation.
[0023] The amount of buffer used when solubilising the ingenol angelate can vary between about 0 and 100%. When the amount is 0, it is preferred to add a quantity of buffer shortly after adding the ingenol angelate to the solvent, in order to minimise the likelihood of any rearrangement taking place. It is generally preferred to avoid using amounts of buffer greater than 100% by weight of the solvent, as dissolution directly into the buffer is generally not readily achievable. It is preferred to employ the buffer as a means to keep the apparent pH of the solvent at a low level, without providing any substantial amount of protic solvent during dissolution of the ingenol angelate. Once the ingenol angelate has been substantially dissolved, then it is possible, and may even be desirable, to make up the formulation with an excess of buffer comprising, if desired, other optionally protic constituents, such as antibiotics, for example. Preferred levels of buffer are in the region of 0.5%-10%, and preferably between 1% and 5%, with about 2-3% being most preferred during the dissolution phase. The dissolution phase comprises dissolving at least a majority of the ingenol angelate in the solvent, and preferably at least 95% w/w ingenol angelate in the solvent, more preferably at least 99% w/w.
[0024] Formulations of the present invention may be used directly, or may be stored for future use. In addition, formulations of the present invention may provide a base formulation which can then be further modified prior to use. For example, as described above, the formulation may be made up in an excess of buffer or may be formulated into a gel, for example.
[0025] It has also been found that formulations of the present invention are generally more stable at lower temperatures. Particularly preferred formulations of the present invention, such as those comprising benzyl alcohol and citrate buffer, may exhibit substantial stability at temperatures as high as 40.degree. C. but, in general, increasing stability is observed at temperatures below room temperature and pressure (RTP), and the greatest stability is observed at temperatures below about 8.degree. C. Freezing does not appear to enhance stability so that, in general, the greatest stability is achieved simply by placing formulations of the invention in a conventional refrigerator at a temperature of between about 2.degree. C. and 8.degree. C.
[0026] The present invention further provides a process for preparing a solution of ingenol angelate, comprising dissolving the ingenol angelate in a pharmaceutically acceptable, aprotic solvent, said formulation further comprising a pharmaceutically acceptable acidifying agent which is at least partially compatible with the solvent and which provides the formulation with an apparent pH of no greater than 4.5, said acid being added with, before, or after the ingenol angelate.
[0027] In an alternative, the present invention provides a process for preparing a solution of ingenol angelate, comprising dissolving the ingenol angelate in a pharmaceutically acceptable, aprotic solvent, said process comprising the addition of a pharmaceutically acceptable acidifying agent which is at least partially compatible with the solvent and which provides the formulation with an apparent pH of no greater than 4.5, said acidifying agent being added with, before, or after the ingenol angelate. The acidifying agent is preferably a buffer.
[0028] It is preferred to add the acid, or buffer, sufficiently soon after addition of the I3A to ensure that no more than about 1%, and preferably no more than about 0.5%, of the `b` isoform rearranges into the `a` isoform. Preferably, the acid or buffer is added to the solvent before adding the I3A, although all three ingredients may be combined at the same time. This latter is the least preferred option.
[0029] This process may also be used for the preparation of ingenol angelate formulations using other compounds and solvents, such as polyethylene glycol, where direct solubilisation may be associated with an unacceptable level of rearrangement. Although I3A can dissolve in PEG, it takes in the region of an hour at elevated temperature, which generally leads to the generation of unacceptable levels of the `a` isoform. If the I3A is dissolved in buffered benzyl alcohol first, this can then be introduced directly into the PEG, without the prolonged exposure to heat. As only enough benzyl alcohol is needed to solubilise the I3A, then the total amount of benzyl alcohol in the final PEG formulation need only be in the region of 1% w/w or less.
[0030] These formulations may be kept for sustained periods, especially when kept at temperatures of 8.degree. C. or lower. Preferred compositions see no more than about 1%, and preferably no more than about 0.5%, rearrangement of the `b` isoform to the `a` isoform after 3 months, more preferably 6 months.
[0031] There is further provided the use of a formulation of the invention in the treatment of a skin cancer.
[0032] The invention also provides the use of ingenol angelate in the manufacture of a medicament for the treatment or prevention of a skin cancer, wherein the ingenol angelate is dissolved in a pharmaceutically acceptable, aprotic solvent, said formulation further comprising a pharmaceutically acceptable acidifying agent which is at least partially compatible with the solvent and which provides the formulation with an apparent pH of no greater than 4.5.
[0033] Suitable cancers for treatment in accordance with the present invention include squamous and basal cell cancers.
[0034] It will be appreciated that `treatment`, as used herein, includes both therapy and prophylaxis.
[0035] The present invention also provides a method of treating a subject suffering from a cancerous skin condition, comprising the topical application of a therapeutically effective amount of a composition of the invention to the area of the cancerous condition.
[0036] Suitable subjects for treatment are mammals, including humans, primates, livestock animals (including cows, horses, sheep, pigs and goats), companion animals (including dogs, cats, rabbits, guinea pigs), captive wild animals, and laboratory animals, such as rabbits, mice, rats, guinea pigs and hamsters. The compositions of the present invention are particularly suitable for the treatment of human skin cancers.
[0037] It will be appreciated that the formulations of the present invention may be used in any suitable cancer prophylaxis or treatment. Administration forms may be any suitable, and include creams, gels, ointments, lotions, sprays, lacquers and paints for topical application, powders, solutions and suspensions for the airways, solutions and emulsions for injection, capsules, syrups and elixirs for oral administration, and pessaries and suppositories. Other suitable administration forms will be readily apparent to those skilled in the art, and may include transdermal patches, for example. In a preferred embodiment of the present invention, the ingenol angelate formulations are formulated for topical administration.
[0038] In all cases, the initial formulation is as a formulation of the invention. The formulation may be made up into the final form either just before use as soon as desired after preparation of the formulation, but will usually remain a formulation of the invention at all times.
[0039] Formulations may comprise additional ingredients, as discussed below. It is particularly preferred to employ antioxidants, as these appear to provide enhanced stability to the formulations. Suitable examples of antioxidants include retinol, ascorbic acid, lycopene, butylated hydroxytoluene, and tocopherol.
[0040] The amount of ingenol angelate required for pharmaceutical efficacy will be apparent to those skilled in the art, and may be adapted according to physiological parameters, such as age, weight and sex of the patient, as well as the size of any lesion. In general, an amount of ingenol angelate suitable to provide between about 0.01 .mu.g cm.sup.-2 to about 1 mg cm.sup.-2 may be employed, with a range of 0.1 mg cm.sup.-2 to about 100 .mu.g cm.sup.-2 being more preferred. In the accompanying Examples, a formulation providing 15 .mu.g cm.sup.-2 was used, but formulations of 1 .mu.g cm.sup.-2, or less, have been found to be effective. In the alternative, formulations of the invention may contain I3A in an amount of from 0.001% (w/w) to 0.15% (w/w), more preferably up to about 0.1-0.12% (w/w).
[0041] Topical formulations are a preferred embodiment of the present invention. In this regard, a heretofore unrecognised property of the ingenol angelates is particularly useful, in that it has been found that they have vasoconstrictive properties. Accordingly, systemic distribution of the active ingredient is minimised, owing to the reduced blood flow in the vicinity of treatment.
[0042] It will be appreciated that the nature of the formulation will determine the rate of permeation across the skin. As such, it is generally preferred that the formulation be prepared such that a rate of permeation of at least about 11 ng cm.sup.-2 h.sup.-1 is achieved. There is no special upper limit, although it is generally preferred that this not exceed around 1 .mu.g cm.sup.-2 h.sup.-1.
[0043] Topical formulations may take any suitable form. In general, it is preferred that they exhibit some level of viscosity, in order that they can be targeted at the desired area without running off. Accordingly, it is generally preferred to formulate ingenol angelate as creams, gels, ointments, and paints. Given the potency of ingenol angelate, paints may be employed, as they may be applied sparingly, depending on levels of the active ingredient.
[0044] Poloxamers may be used in preferred formulations of the present invention. They are co-polymers which consist of a hydrophobic poloxypropylene (POP) molecule sandwiched between two hydrophilic molecules of poloxyethylene (POE). Thus, they have the ability to solubilise lipophilic drugs within the hydrophobic core. Furthermore, poloxamer based aqueous gel formulations exhibit thermo-rheological properties, which may be advantageous for localised, sustained delivery of drugs. Above a certain temperature, known as the critical micelle temperature (cmt), the viscosity of the poloxamer gel increases dramatically. An increase in viscosity leads to a decrease in the diffusion of any drugs dissolved in the gel which slows down the release of drug from the gel and leads to sustained delivery. The increase in viscosity may also provide a prolonged, localised `depot` at the site of action.
[0045] The cmt is dependent on a number of variables such as concentration of poloxamer and other additives such as propylene glycol. Ideally, the cmt should be at a temperature such that the formulation can be injected into the lesion as a liquid (ease of administration) and upon contact with body temperature a gel is formed with the aim of achieving a localised, sustained delivery of the drug. Five poloxamers are listed in the USP, and include poloxamer 188 and poloxamer 407. Poloxamer 188 has been approved as an excipient for IV formulations (http://www.accessdata.fda.gov).
[0046] Poloxamer gels have been used for subcutaneous delivery of insulin (Barichello et al., 1999) and other drug delivery systems for percutaneous use (Tobiyama et al., 1994). One particular copolymer, poloxamer 407 has been administered subcutaneously for the slow release of peptides and therapeutics proteins, which included interleukin-2 and human growth hormone (Morikawa et al., 1987; Katakama et al., 1997). Following administration, the gels slowly released the entrapped protein molecules over a period of 1-2 days. Furthermore, a substantial fraction of this poloxamer eventually underwent renal excretion.
[0047] Poloxamers are generally regarded as non-toxic and non-irritant materials. Animal toxicity studies, with dogs and rabbits, have shown poloxamers to be non-irritant and non-sensitising when applied, in 5% w/v and 10% w/v concentration, to the eyes, gums and skin. In a 14-day study of intravenous administration to rabbits, at concentrations up to 0.5 g/kg/day, no overt adverse effects were noted. A similar study with dogs also showed no adverse effects at dosage levels up to 0.5 g/kg/day. Furthermore, no haemolysis of human blood cells was observed over 18 hours at 25.degree. C., with 0.001-10% w/v poloxamer solutions (Wade and Weller, 1994). However, hyperlipidemia in rats has been reported when an intraperitoneal (IP) injection (1.0 g/kg) of poloxamer 407 was introduced (Wasan et al., 2003).
[0048] Oils may also be used in the present invention. The use of an emulsion based intralesional formulation has been reported for the treatment of psoriasis (Ho et al., 1990). Prior to administration, a vehicle, such as polyoxyethylated castor oil, is normally diluted with saline to form the emulsion. However, our studies have shown that dilution of I3A with normal saline increases the conversion of isoform `b` to `a`. This conversion may be minimised if the administration time of the formulation is short.
[0049] There are a number of lipophilic products that are formulated as oily solutions for intramuscular administrations (IM), for example Prolixin Enanthate (Bristol Myers Squibb). The vehicle (oil) used varies widely from vegetable oils such as arachis oil (used with benzyl benzoate in Dimercaprol Injection B.P.) and sesame oil (used in depot injections of Fluphenazine Enanthate Injection B.P). The use of oleaginous vehicles may slow absorption due to delayed partitioning of the drug from the oil to the aqueous body fluids (Ford, 1987). When injected into an aqueous environment (such as muscle tissue) a relatively lipophilic drug such as I3A, dissolved in an oil phase, will have a tendency not to leave the oil and `instantaneously` partition into the aqueous phase. In this way a sustained release effect can be achieved.
[0050] Buccal formulations may also be employed. Transmucosal delivery of therapeutic agents is a popular administration form, because mucous membranes are relatively permeable, allowing for the rapid uptake of a drug into the systemic circulation and avoiding first pass metabolism. Transmucosal products can be designed to be administered via the nasal route and oral/buccal route using mucoadhesives. In the development of these drug delivery systems, mucoadhesion of the device/formulation is a key element. The term `mucoadhesive` is commonly used for materials that adhere to the mucin layer of a biological membrane. Mucoadhesive polymers have been utilised in many different dosage forms in efforts to achieve systemic and localised delivery of drugs through the different mucosae. These dosage forms include tablets, patches, tapes, films, semisolids and powders.
[0051] To serve as mucoadhesive polymers, the polymers should possess physicochemical features such as being predominantly anionic with numerous hydrogen bond-forming groups, suitable surface properties for wetting mucus/mucosal tissue surfaces and sufficient flexibility and length (molecular weight) to penetrate the mucus network or tissue crevices. Diverse classes of polymers have been reported as potential mucoadhesives such as carbomers (polyacrylic acids), hydroxypropyl methylcellulose (HPMC) as well as naturally occurring polymers, such as hyaluronic acid and chitosan.
[0052] Preparation of suitable formulations is within the skill of those in the art, and suitable excipients for inclusion in any such formulation include, for example, gellants, viscosifiers, penetration enhancers, preservatives, such as antibiotics and antifungals, and cosmetic ingredients, such as scents and colourings.
[0053] Suitable gelling agents include: water soluble cellulose derived polymers, such as hydroxyalkyl cellulose polymers (e.g. hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose), carboxymethyl cellulose, methylhydroxyethyl cellulose and methyl cellulose, carbomer (e.g. carbopol); and carrageenans. The gelling agent may be added in any suitable amount, such as 1-5% (w/w). Preferred gelling agents are cellulose derived, most preferably hydroxyalkylcellulose, particularly hydroxyethylcellulose.
[0054] Suitable preservatives will be apparent to those skilled in the art, and include the parabens (methyl, ethyl, propyl and butyl), benzoic acid and benzyl alcohol. Preservatives employed solely for that purpose will generally form 1% (w/w) or less of the final topical formulation.
[0055] Suitable penetration enhancers include isopropyl alcohol, sulphoxides (such as dimethylsulphoxide, DMSO), Azones (e.g. laurocapram), pyrrolidones (for example 2-pyrrolidone), alkanols (e.g. decanol), and glycols (for example propylene glycol).
[0056] Preferred compositions of the invention comprise:
a) I3A;
[0057] b) penetration enhancer;c) preservative;d) gelling agent; ande) buffer;wherein the composition has an apparent pH of between 3 and 4, inclusive.
[0058] A particularly preferred composition comprises:
a) 0.1% (w/w) I3A;b) 30% (w/w) isopropyl alcohol;c) 0.9% (w/w) benzyl alcohol;d) 1.5% (w/w) hydroxy ethyl cellulose; ande) 67.5% (w/w) citrate buffer pH 3, preferably pH 2.75.
PLANTS Profile for Euphorbia peplus (petty spurge) | USDA PLANTS
plants.usda.gov/java/profile?symbol=EUPE6
Euphorbia peplus | Wildflowers of the Pacific Northwest
Euphorbia peplus. Petty Spurge. Erect, hairless, yellow-green plant with milky sap. Stem hairless, 4–14 in. tall. Leaves with short petioles, smaller at top ...
www.pnwflowers.com/flower/euphorbia-peplus
Calflora: Euphorbia peplus
Euphorbia peplus, a dicot, is an annual herb that is not native to California; it was introduced from elsewhere and naturalized in the wild. ...
www.calflora.org/cgi-bin/species_query.cgi?where...3561
Euphorbia Family (Euphorbiaceae)
Petty spurge (Euphorbia peplus), an erect garden weed in southern California with alternate leaves and milky sap. Originally native to Europe, this prolific ...
waynesword.palomar.edu/trmar98b.htm
http://cancerfighter.wordpress.com/2008/06/03/radium-weed-euphorbia-peplus-for-skin-cancers/
Radium weed (Euphorbia peplus) for skin cancers
Posted by cancerfighter on June 3, 2008
The Big Book: Cancer: The Complete Recovery Guide
“This book tells me everything. Why didn’t my doctor tell me this?”- Rev. Bill Newbern
RADIUM WEED
A story from the Australian Naturopathic Network notes the recent announcement that Euphorbia peplus (commonly known as Radium Weed) has been found “to cause sun spots, Basal Cell Carcinoma
(BCC) and Squamous Cell Carcinoma (SCC) to disappear, and drop off!” Brian McDermott, the commentator presenting the story, said, “Our grandmothers taught us this over half-a-century ago, and it was well-
known in the bush, where we grew up!” He predicts the so-called experts will now be stumbling
over each other in the race to patent their “discovery.”
http://species.wikimedia.org/wiki/Euphorbia_peplus
Euphorbia peplusClassification System: APG III (down to family level)
Regnum: Plantae
Cladus: Angiosperms
Cladus: Eudicots
Cladus: Core eudicots
Cladus: Rosids
Cladus: Eurosids I
Ordo: Malpighiales
Familia: Euphorbiaceae
Subfamilia: Euphorbioideae
Tribus: Euphorbieae
Subtribus: Euphorbiinae
Genus: Euphorbia
Species: Euphorbia peplus
Patents
Anti-cancer compounds
US7410656
Inventor(s): AYLWARD JAMES HARRISON
Classification:- international: A61K31/225; A61K36/47; A61K31/21; A61K36/185; (IPC1-7): A61K31/225; A61K35/78- European: A61K31/225; A61K36/47
Abstract -- This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Chinese medicinal preparation for treating esophagus cancer
CN101590176
Abstract -- The invention discloses a Chinese medicinal preparation for treating esophagus cancer. The Chinese medicinal preparation adopts a method of treating both primary and secondary symptoms to strengthen body resistance and eliminate pathogenic factors so as to achieve the aim of treating esophageal cancer by inhibiting the proliferation of cancer cells and the killing cancer cells. The inventor takes ancestral secret prescriptions and Chinese traditional medical theories as foundation, and prepares the Chinese medicinal preparation according to the monarch-minister-assistant-guide composition principle and compatibility of Chinese prescriptions. By taking red sage roots, scorpion, toad skin, airpotato yam and nidus vespae as monarch medicines, taking arrowhead leaves, white stiff silkworms, sun euphorbia herbs, house lizards, kiwi roots, walnuts and peperomia dindygulensis as minister medicines, assisting the monarch medicines and the minister medicines with Chinese olive, seaweed, disporum leschenaultianum, gynura bicolor grass and rhizoma bolbostemmae, and taking dried persimmon frost, magnolia officinalis, rhizoma anemarrhenae, hippocampus, cordyceps sinensis and musk as guide medicines, the Chinese medicinal preparation is prepared through scientific compatibility and a preparation process.
Medicine for treating breast cancer
CN101780187
Abstract -- The invention relates to a medicine for treating breast cancer, which comprises the following components by weight ratio: 70-90 Euphorbia pallasie Steud, 20-30 rhizoma arisaematis, 20-30 pinellia tuber, 5-15 golden thread, 3-7 rhubarb and 3-7 licorice. The invention is prepared by Chinese herbal medicines, has low making cost, low cost of treatment, calm nature, and no toxicity and side effects. At least 50g of liquid finished product or 3-4 capsules are taken once and taken three times a day, the medicine can be safely and reliably taken by patients, and the curative effect is obvious; and the clinical trial results for more than 120 breast cancer patients show that the total effective rate is 98%, and the cure rate is over 85%.
Extraction and preparation method of total phenol of compound abnormal savda munziq
CN101757128 (A)
Abstract -- The invention provides an extraction and preparation method of total phenol of compound abnormal savda munziq, wherein the abnormal savda munziq is prepared by the following steps of: mixing ten kinds of medicines such as cordial fruits, bugloss, licorice, diantaceae, euphorbia humifusa and the like according to the proportion, decocting, soaking, filtering, decompressing, condensing and drying the mixture to obtain an extract solid; crushing the extract solid to obtain dry powder; adding hot water into the dry powder and dissolving and filtering; adding ethanol into filtrate to precipitate; stirring, standing and filtering the precipitation; decompressing and condensing the filtrate; treating the filtrate through a polyamide; sequentially eluting the filter with water and dilute ethanol; discarding eluent; eluting with high-concentration ethanol; and decompressing, condensing, drying and crushing the eluent to obtain a total phenol product with stronger in vitro anti-cancer activity, wherein the content of the total phenol is over 30 percent and the content of total flavone is over 13 percent. The extraction and preparation method has low cost, simple process, practicability and safety; and the prepared total phenol has excellent stability and can be prepared into tablets, capsules, oral liquid, granules, decoction, syrups, pills and the like for use.
Pharmaceutical composition with effects of resisting cancer and alleviating pain
CN101745065
Abstract -- The invention discloses a pharmaceutical composition with effects of resisting cancer and alleviating pain, which is prepared from 40 traditional Chinese medicines: toad venom, pangolin scales, centipede, scorpion, honeycomb, leech, szechuan aconite, wild aconite, arisaema tuber, tuber pinellia, euphorbia kansui, knoxia corymbosa, rhizoma sparganii, rhizoma zedoariae, polyporus umbellatus, rhubarb, amur corktree bark, baikal skullcap root and the like. The pharmaceutical composition of the invention has obvious curative effects on various cancers of early, middle and late stages, and has the efficacies of resisting cancer and inhibiting tumor, promoting blood circulation and removing stasis, removing the necrotic tissue and promoting granulation, and promoting circulation of qi and relieving pain. The pharmaceutical composition of the invention controls cancer pain by resisting cancer and inhibiting tumor, draws out cancer poison, enables the tumor to shrink and disappear to achieve the purposes of improving living quality and prolonging life, and has convenient and safe use and no toxic and side effect. The efficacies are better by pasting the pharmaceutical composition of the invention on corresponding points of a human body.
Medicament for treating lung cancer
CN101703726
Abstract -- The invention relates to a medicament, in particular to a medicament for treating lung cancer, which solves the problem of inapparent curative effect of the conventional medicaments for treating the lung cancer. The medicament comprises is prepared from the following raw materials by conventional method:; mongolian dandelion herb, centipede, scorpion, rhizoma pleionis, black nightshade herb, bittersweet herb, sun euphorbia herb, Indian mockstrawberry herb, toad venom, sarcandra glabra, green tangerine peel, Indian buead, oriental waterplantain rhizome, szechwon tangshen root, villous amomum fruit, plantain seed, glossy ganoderma, honeysuckle flower, weeping forsythiae capsule, chicken's gizzard-membrane, largehead atractylodes rhizome, immature bitter orange, glossy privet fruit, radix astragali, Chinese atractylodes rhizome, katsumade galangal seed, Chinese sage herb, radix asparagi, blackberrykiky rhizome, cassia twig, Chinese magnoliavine fruit, semen armeniacae amarum, radix scutellariae, common coltsfoot flower, bulbus fritillariae thunbergii, radix glycyrrhizae preparata, peach seed, danshen root, rosewood heart wood, szechuan lovage rhizome, sessile stemona root,; pinellia tuber, tatarian aster root, snakegourd fruit, red paeony root, perilla fruit, radish seed, pepperweed seed, greenish lily bulb, scorch-fried crataegus, scorch-fried medicated leaven, hordeum vulgare, longstamen onion bulb, eucommia bark, south dodder seed, tangerine peel, costustoot, nutgrass galingale rhizome, heartleaf houttuynia herb, indigowoad root, dwarf lilyturf tuber, coastal glehnia root, virgate wormwood herb, hairyvein agrimonia herb and bud and spreading hedyotis herb.
Traditional Chinese medicine for treating hepatitis B, cirrhosis, liver cancer and liver ascites
CN101618172
Abstract -- The invention relates to a traditional Chinese medicine for treating cirrhosis, which is prepared by grinding traditional Chinese medicines, i.e. cornu bubali, rhubarb, pariphyllin, melanterite, colla corii asini, rhizoma zedoariae, turtle shell, radix morindae officinalis, cordyceps sinensis, and the like, into powder to be encapsulated, wherein if components, i.e. the large cornu bubali, the pariphyllin and the melanterite, are added to the traditional Chinese medicines, the traditional Chinese medicine for treating the cirrhosis can be used for treating hepatitis B; if the melanterite is removed from the traditional Chinese medicines, the traditional Chinese medicine for treating the cirrhosis has good treatment effect on liver cancer; ascites can be caused by the cirrhosis and the liver cancer, and the traditional Chinese medicine for treating the ascites is prepared from morning glory, euphorbia kansui, yam, matrimony vine, cinnamon, and the like. The traditional Chinese medicines have the advantages of least toxic side effect, tonification and purgation in combination, long-term administration and high cure rate and effective rate.
Chinese medicinal preparation for treating esophagus cancer
CN101590176 (A)
Abstract -- The invention discloses a Chinese medicinal preparation for treating esophagus cancer. The Chinese medicinal preparation adopts a method of treating both primary and secondary symptoms to strengthen body resistance and eliminate pathogenic factors so as to achieve the aim of treating esophageal cancer by inhibiting the proliferation of cancer cells and the killing cancer cells. The inventor takes ancestral secret prescriptions and Chinese traditional medical theories as foundation, and prepares the Chinese medicinal preparation according to the monarch-minister-assistant-guide composition principle and compatibility of Chinese prescriptions. By taking red sage roots, scorpion, toad skin, airpotato yam and nidus vespae as monarch medicines, taking arrowhead leaves, white stiff silkworms, sun euphorbia herbs, house lizards, kiwi roots, walnuts and peperomia dindygulensis as minister medicines, assisting the monarch medicines and the minister medicines with Chinese olive, seaweed, disporum leschenaultianum, gynura bicolor grass and rhizoma bolbostemmae, and taking dried persimmon frost, magnolia officinalis, rhizoma anemarrhenae, hippocampus, cordyceps sinensis and musk as guide medicines, the Chinese medicinal preparation is prepared through scientific compatibility and a preparation process.
Medicated wine for treating cancer and tumor and method for preparing same
CN1966008
Abstract -- The invention discloses a Chinese medicinal liquor preparation for treating cancer and its preparing process, wherein the liquor is prepared from the following raw materials herbs: dysosmapleiantha woods 10-15g, Rhodoendron lacteum 10-15g, Pediculus melo 3-5g, hairy deerhorn 10-1.5g, barbat skullcap 20-30g, Japanese felt fern leaf. 15-20g, seaweed 15-20g, euphorbia helioscopia 40-60g, wasp's nest 10-15g, Pygmy arrowhead 10-5g, airpotato yam 40-60g, walnut kernel 40-60g, acanthopanax root 40-60g, ear of wheat 40-60g, toad 12-15g, buthus martensi kirsch 6-8g, Chinese date 15-20g, white-stiff silkworm 9-15g, house lizard 6-10g, leech 6-10g, musk 9-15g, bat's feces 30-40g, licorice root 6-10g, Chinese actinidia root 40-60g, osmanthus flower wine 500-550ml, and white spirit 4500-5000ml.
Traditional Chinese medicine for treating digestive cancer and its producing method
CN101057945
Abstract -- The invention relates to a Chinese medicament for preventing and treating digestive tract cancer and process for preparation, wherein the medicament is prepared from astragalus root, green tangerine orange peel, banksia rose, linaloe, clove, zedoary, burred tuber, Ligusticum wallichii, pinellia tuber, white mustard seed, euphorbia helioscopia, radical lobelia, barbat skullcap, oldenlandia, selfheal, dried body of ground beetle, leeches and water.
Medicine for treating cancer and preparing method thereof
CN101143167
Abstract -- The invention relates to a drug for remedying the cancer and especially indicates a cancer-washing cure drug of Hunan He pharmacy for remedying the cancer. The invention has good curative effect within the following weight range of 7 to 15 portions of duchesneas, 7 to 15 portions of sun euphorbia, 7 to 15 portions of prepared pinellia tubers, 7 to 15 portions of alums, 5 to 15 portions of rhubarbs and 450 to 550 grams of liquor. The preparation method of active components of the drug of the invention is as follows that the raw materials of the duchesnea, the sun euphorbia, the prepared pinellia tuber, the alum and the rhubarb are washed cleanly for using; the raw materials are dipped in the liquor of high quality in an urn; the drug can be taken out for using after one month.
A Chinese traditional external use medicine for treating medium term and late brain tumor
CN1943644
Abstract -- This invention relates to a Chinese traditional external use medicine for treating medium term and late brain tumor. It includes the main medicine and excipient, the said main medicine is composed with the flowing raw materials by the unit of weight: whole scorpion(25-35), radix aconiti sinensis (16-20), radix aconiti agrestis16-20), meretrix shell(16-20), putamen manidis (15-25), bombyx batryticatus (10-20), dog button (4-8), gecko (3-7), argum groundsel herb (3-8), knoxia root (3-7), Euphorbia kansui Liou (2-6), galla sinensis (1-3), twotooth achyranthes root (1-3), borneol (0.5-1.5), catharsius (0.5-1.5), blister beetle (0.5-1.5), camphor (5-15), musk (6-10) and calculus bovis (10-14). The said excipient is prepared by the following raw materials through using the unit of weight: safflower (3.7), glycyrhiza(3.7), centipede (3.7), succus spissatus of Shanxi vinegar(486 use size as its unit). After preparing the said main medicine and excipient, externally apply to the affected part, the medicine through penetration will make the hydrocephalus discharged, epilepsia eliminated, so to cut off the existence of the cancer cell and kill the target cell of the cancer cell, and at the same time make the dead cancer cell excreted outside of the body, so to have the organist immunity improved, and finally reach the aim of the recovery of the brain tumor.
DITERPENES FROM EUPHORBIA KANSUI AND THEIR USE
WO2006116897
Abstract -- Novel diterpenes with antitumor activity of formula (I), wherein R1 ~ R3 represent aliphatic group; or represent group of RCO-, in which R represents aliphatic group, aryl, or heteroaryl. The compounds of the present invention are prepared by extracting roots of euphorbia kansui with organic solvent (chloroform, ethyl acetate and butanol) and treating the extract by conventional methods. The compounds of the present invention have cell proliferation inhibiting activity, and can inhibit the proliferation of specific cancer cell lines via inhibition of topoisomerase. These compounds can be used for preparing medicaments for treating malignant tumor.
DITERPENES FROM EUPHORBIA KANSUI AND THEIR USE
WO2006116897
Abstract -- Novel diterpenes with antitumor activity of formula (I), wherein R1 ~ R3 represent aliphatic group; or represent group of RCO-, in which R represents aliphatic group, aryl, or heteroaryl. The compounds of the present invention are prepared by extracting roots of euphorbia kansui with organic solvent (chloroform, ethyl acetate and butanol) and treating the extract by conventional methods. The compounds of the present invention have cell proliferation inhibiting activity, and can inhibit the proliferation of specific cancer cell lines via inhibition of topoisomerase. These compounds can be used for preparing medicaments for treating malignant tumor.
Chinese medicine for treating cancer
CN1698738
Abstract-- The invention relates to a Chinese medicine for treating cancer which is prepared from the following raw materials, scorpion, house lizard, dysosmapleiantha woods, creeping euphorbia, hairy deerhorn, black-tail snake, long-nosed pit viper, toad skin, centipede, batryticated silkworm, leeches, earthworm, seaweed, wood louse, pangolin scales, safflower, notoginseng, dry human placenta, decapetalous daesalpinia and gadfly.
Anti-cancer compounds
US7410656
Abstract -- This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
COMBINATION OF ACTIVE FRACTIONS FROM THE PLANTS EUPHORBIA TIRUCALLI L AND FICOS CARICA L. AND METHOD OF TREATING CANCER AND AIDS
WO2006007676
Abstract -- The present invention refers to the combination of active fractions from the plants Euphorbia tirucalli L. e Fícus carica L. more particularly the pharmaceutical compositions comprising the said combinations, which are useful for treatment of cancer and Acquired Immunodeficiency Syndrome (AIDS). The present invention also relates to the process of manufacture of the active fractions from the plants.
Methods of stimulating the immune system
US6844013
Abstract -- This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Cancer treating medicine
CN1256146
Abstract -- The medicine of the present invention is injecta, tablet or capsule prepared with Herba Hedyotis Diffusae, Rhizoma Zedoariae, Euphorbia fisheriana, peach kernel and other over ten Chinese medicinal materials and through water or alcohol extraction and other steps. It may be used to prevent and cure lung cancer, gastric cancer, esophagus cancer, etc.
Anticancer Chinese medicine and its preparation
CN1205890
Abstract -- The medicine is prepared by using euphorbia hilioscopia juice, selfheal, Euphorbia fisheriana, greater celandine, ginseng, etc. as material. During the preparation, euphorbia hiliscopia juice is treated through modern biotechnology. The medicine can control and eliminate cancer cells, eliminate cancer source, and prevent the generation of cancer cell and it has obvious curative effect and no serious effect to health cell. As one product of combined traditional Chinese medicine theory and modern biotechnology, the medicine is widely used in treating esophagns cancer, liver cancer, lung cancer,etc. and may be also used in treating lymphosarcoma, osteonyclitis, obstinats sore, etc.
Powerful anticancer plaster and its preparing method
CN1112011
Abstract -- The powerful anticancer plaster suitable for different stages of cancer is prepared through segmental decoction of edible plant oil, blushred rabdosis herb, dry toad skin, sun euphorbia herb, etc. at 300-350 and 350-400 deg.C, cooling to 200 deg.C, mixing with fine powder processed from 9 Chinese-medicinal materials such as pinellia tuber, prepared aconite root, cloves, Chinese blistering beetle, etc., and stirring, and features high effective rate (96% for esophagus, cardia, stomach and large intestine cancers and 80% for liver and uterus cancer).
