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Gossypin: Naturally occurring substance effective against deadly skin cancer in lab tests


A natural substance called gossypin, extracted from the flowers of cotton and hibiscus plants, has been proven effective as a treatment for melanoma, the deadliest and most aggressive form of skin cancer, in lab tests– the next step is to see whether it works in humans. –link

For the first time, scientists have demonstrated the mechanism of action of gossypin, a naturally-occurring substance found in fruits and vegetables, as a treatment for melanoma, which causes the majority of deaths from skin cancer.

“We identified gossypin as a novel agent with dual inhibitory activity towards two common mutations that are the ideal targets for melanoma treatment,” said Texas Biomed’s Hareesh Nair, Ph.D.

At the moment, there is no single therapeutic agent or combination regimen available to treat all melanomas, of which about 76,000 new cases are diagnosed annually, according to the American Cancer Society.

“Our results indicate that gossypin may have great therapeutic potential as a dual inhibitor of mutations called BRAFV600E kinase and CDK4, which occur in the vast majority of melanoma patients. They open a new avenue for the generation of a novel class of compounds for the treatment of melanoma,” Nair added.

His report, appearing in the March 29, 2013 issue of the journal Molecular Cancer Therapeutics, was funded by the Texas Biomedical Forum and the Robert J. Kleberg, Jr. and Helen C. Kleberg Foundation.

Nair and his colleagues found that gossypin inhibited human melanoma cell proliferation, in vitro, in melanoma cell lines that harbor the two mutations. Gossypin stunted activities of the mutated genes, possibly through direct binding with them. It also inhibited the growth of various human melanoma cells. In addition, gossypin treatment for 10 days of human melanoma cell tumors with the mutations transplanted into mice reduced tumor volume and increased survival rate.

Further studies are planned by Nair’s team to understand how the body absorbs gossypin and how it is metabolized. This idea has been discussed with the Cancer Therapy & Research Center at the UT Health Science Center San Antonio’s Deva Mahalingam, M.D, Ph.D., who is interested in testing gossypin in melanoma patients. …

via Naturally occurring substance proves effective against deadly skin cancer in laboratory tests.


Dr. Hareesh Nair of Texas Biomedical Research Institute led a group of researchers in a study that examined gossypin’s mechanism of action as a potential melanoma treatment, which was recently published in the journalMolecular Cancer Therapeutics.

Melanomas will be diagnosed in about 76,690 Americans this year, according to the American Cancer Society, and the rates have been rising for at least 30 years. Over 9,000 people are expected to die of the illness, and while the cancer typically develops in adults, it is being increasingly more common in children.

Standard melanoma treatments include chemotherapy and surgeries to remove tumors, and the earlier the skin cancer is diagnosed, the more effective treatment can be.

For the time being, however, there is no single therapy that can treat all melanomas. The study researchers write that the median survival rate for patients with advanced melanoma is less than 10 months, and therapies for metastasized melanomas are often ineffective.

“We identified gossypin as a novel agent with dual inhibitory activity towards two common mutations that are the ideal targets for melanoma treatment,” said Nair in a statement.

Nair and his team found that the hibiscus plant extract inhibited the growth of human melanoma cells by stunting the activity of two mutated genes called BRAFV600E kinase and CDK4, which are seen in up to 70 percent of melanoma cases. It’s possible that gossypin shuts these genes down by directly binding to them, taking the place of other molecules that would normally activate them.

Gossypin treatment for 10 days also reduced tumor volume and increased survival rate in mice that had human melanoma cell tumors.

The results “open a new avenue for the generation of a novel class of compounds for the treatment of melanoma,” said Nair.

Recent studies have shown that gossypin has anti-inflammatory and pain-reducing properties, and may also help fight diabetes. Hibiscus vitifolius root extract has been used to treat jaundice in Indian herbal medicine for centuries, and recent research has confirmed its potent liver-protecting properties.

via MedicalDaily

Hepatitis, viral infections, food additives, alcohol, toxic industrial chemicals, and air and water pollutants are the major risk factors of liver toxicity. Carbon tetrachloride (CCl4) is a potent environmental hepatotoxin that generates free radicals. Scientific research has supported the hepatoprotective potential of several herbal compounds. Hibiscus vitifolius (Family: Malvaceae), a medicinal plant is used to treat several ailments in Ayurvedic system of medicine. The root of this plant is traditionally used to treat jaundice by the tribes of Kanyakumari district, India. The present study was aimed to extract the roots of H. vitifolius and evaluate hepatoprotective activity in CCl4 induced hepatotoxic rats to scientifically assess the traditional claim about H. vitifolius roots and to fractionate the pharmacologically active extract. The study was also aimed to isolate the bioactive constituents from the soluble fraction followed by evaluation of hepatoprotective activity and to elucidate the structure. H. vitifolius roots were successively extracted with petroleum ether, chloroform, alcohol and water by cold maceration technique for 6 days. All the extracts (400 mg/kg b.wt. p.o.) were evaluated for their hepatoprotective activity. The active alcohol extract was fractionated using n-hexane, ethyl acetate and n-butanol and the fractions (200 and 400 mg/ kg b.wt. p.o.) were evaluated for hepatoprotective activity. The active ethyl acetate soluble fraction (100 gm) was subjected to column chromatography to elute the active constituent and to establish its structure. The isolated compound (100 and 200 mg/kg b.wt. p.o.) was further evaluated for its acute toxicity and hepatoprotective effect. Hepatotoxic rats were orally treated with extracts, fractions and the isolated compound for 7 days. Silymarin (100 mg/kg) was used as standard drug. Biochemical analysis and histopathology were performed to confirm the activity. Among all the extracts and fractions, alcohol extract of H. vitifolius roots (400 mg/kg) and its ethyl acetate soluble fraction (200 mg/kg and 400 mg/kg) showed significant (P<0.001) hepatoprotective effect. A flavonoid glycoside, gossypin was found to be present in this fraction and was confirmed by melting point and spectral data. This was further evident by comparing with the marker compound gossypin by mixed melting point, Co-TLC and Co-HPTLC analysis. The isolated compound showed no mortality or toxic symptoms up to 1 g/kg b.wt. p.o. Oral administration of isolated gossypin (100 and 200 mg/kg b.wt) exhibited the potent hepatoprotective effect against CCl4 induced hepatotoxicity, as evident by the significant restoration of the biochemical parameters. Histopathological examination also supported the hepatoprotective effect of the isolated compound. The present study validates the traditional use of H. vitifolius roots for the treatment of liver disorders and its hepatoprotective effects are attributed to the presence of the flavonoid, gossypin as active agent.

via Omics

As of August 2018, you can buy 250 mg of gossypin for about $300 or 50 mg for about $80 from chemical companies but I haven’t found it as a supplement. Hibiscus flower extract is available for around $10, however. Does hibiscus flower extract or hibiscus essential oil contain gossypin? Perhaps.



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