Louisiana State University and Agricultural & Mechanical College

Zhijun Liu

Eugene A Woltering

Frank L Greenway

Peiying Yang

The combination of gallic acid, ellagic acid, and rubusoside was shown to inhibit angiogenesis by inhibition of pro-angiogenic factors. These three compounds were shown to be absorbed from the intestine making the compounds orally bioavailable. The ratio of the three compounds in the composition was a weight ratio of approximately 1:1.7:17.0 of gallic acid, ellagic acid, and rubusoside, respectively, resulting in a composition with 5% w/w gallic acid, 9% w/w ellagic acid, and 86% w/w rubusoside. This combination was also shown to reduce weight gain, fat accumulation, and serum cholesterol in mammals fed a high fat diet. It also reduced serum triglycerides and tended to reduce blood glucose in mammals on both normal and high fat diets. This three-compound composition ('GER') can be used to treat diseases associated with angiogenesis and to decrease effects of a high fat diet.

Natural composition to decrease effects of a high fat diet

The present invention is directed to methods for extracting and isolating extracts having angiogenesis inhibiting activity from a latex-containing portion of avariant, pharmaceutical and nutraceutical compositions comprising the extracts, methods of administering the extracts to treat angiogenesis-dependent diseases and to reduce or inhibit neovessel growth in a subject in need thereof, and the use of the extracts in the manufacture of a composition for reducing or inhibiting neovessel growth.

Ficus extracts having angiogenesis inhibiting activity and methods of isolating and using the same

Several terpene glycosides (e.g., mogroside V, paenoiflorin, geniposide, rubusoside, rebaudioside A, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, celecoxib, clofazimine, digoxin, oleandrin, nifedipine, and amiodarone. The use of the diterpene glycoside rubusoside and monoterpene glycoside paenoiflorin increased solubility in all tested compounds. The terpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries.

Terpene glycosides and their combinations as solubilizing agents

An extract of Chinese blackberry () has been found to inhibit angiogenesis, and two active fractions isolated. Gallic acid was shown to be one of the active anti-angiogenic compounds by an in vitro human angiogenesis model. Aqueous extracts from other plants either known or found to have gallic acid were also found to have anti-angiogenic activity. Various derivatives of gallic acid were found to inhibit angiogenesis. The extract from Chinese blackberry also slowed the growth of a pancreatic tumor and of corneal neovascularization in rats. Extracts from pomegranate were shown to inhibit angiogenesis in fat tissue. Extracts fromspp, and other plants with gallic acid, and gallic acid and its derivatives will be useful for treating various diseases associated with neovascularization, including diabetic retinopathy, psoriasis, tumors, obesity, cancer, rheumatoid arthritis, etc.

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Baton Rouge, LA, United States of America

Zhijun Liu