The invention relates to a combination of compounds derived from gallic acid, with an antitumoral and antimetastatic activity via a mechanism that involves the induction of apoptosis and the immunogenic death of the tumor cells and the subsequent activation of the specific immune response. The invention also relates to a composition containing a combination of derivatives of gallic acid and pharmaceutically acceptable excipients for the production of useful medicaments in the treatment of cancer. The invention further relates to the use of said composition in a coadjuvant in conventional chemotherapy, reducing the doses of chemotherapeutic agents used in the treatment of cancer.

Fiorentino; Susana

Hernandez; John Fredy

Uruena; Claudia

Castaneda; Diana

Pombo; Luis Miguel

Sandoval; Tito Alejandro

PONTIFICLA UNIVERSIDAD JAVERIANA

FUNDACION UNIVERSITARIA JUAN N. CORPAS

Combination of compounds derived from gallic acid for the treatment of cancer

An extract of Chinese blackberry (Rubus suavissimus) 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 from Rubus spp, 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.

Board of Supervisors of Louisiana State University And Agricultural and Mechanical College

Angiogenic agents from plant extracts, gallic acid, and derivatives

The present invention provides cytochrome P450 3A (CYP3A) inhibitors and enhancers. Examples of the CYP3A inhibitors include free bases or pharmacologically acceptable salts of at least one of the following compounds: .alpha.-naphthoflavone, .beta.-naphthoflavone, apigenin, baicalein, .beta.-myrcene, catechin, 3-phenylpropyl acetate, formononetin, gallic acid, hesperetin, hesperidin, isoquercitrin, lauryl alcohol, luteolin, luteolin-7-glycoside, narigin, nordihydroguaiaretic acid, quercitrin, swertiamarin, terpineol, and trans-cinnamaldehyde. Examples of the CYP3A enhancers include free bases or pharmacologically acceptable salts of at least one of the following compounds: apigenin, formononetin, and luteolin-7-glycoside. The CYP3A inhibitors can be used, alone or co-administered with a drug, to improve the drug bioavailability. The CYP3A inhibitors can also be used as chemopreventors to prevent biotransformation of procarcinogenic compounds into carcinogens via CYP3A activity or for treatment of intestinal or hepatic cancer by inhibit the CYP3A activity. The CYP3A enhancers can be used to improve the enzymatic activity of CYP3A so as to improve the biotransformation and degradation of active drugs or the sustrates of CYP3A from the body. The CYP3A inhibitors and enhancers of the present invention are natural substances extracted from herbs and non-toxic.

gallic acid/neoplasms

Combination of compounds derived from gallic acid for the treatment of cancer

Angiogenic agents from plant extracts, gallic acid, and derivatives

Cytochrome P450 3A inhibitors and enhancers

Anti-angiogenic extracts from pomegranate

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