Synthesis and uses of new ascorbic acid derivatives which have a

Details Synthesis and uses of new ascorbic acid derivatives which have a Synthesis and uses of new ascorbic acid derivatives which have a

1990-07-30

1992-05-19

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

560121, C07C17700

Patent

active

051149729

ABSTRACT:
The invention is related to the novel compounds that have anti-oxident and anti-cancer activities. These compounds can protect (i) vital organs including the brain and the heart, (ii) skin cells, (iii) circulating cells such as red blood cells and white blood cells from physical, chemical and biological injuries either by pre-administration or post-administration. These compounds can be used to protect (iv) organs during transplant surgery by administering to a donar before removal of the organ and by administering to a receipient after transplantation. (v) These compounds can also protect red blood cells from the attack of malarial parasites. (vi) These compounds can be themselves be administered to cancer patients as low side-effect anti-cancer agents. They can also be administered to (vii) potentiate efficacy of existing other chemotherapeutic agents and (viii) to reduce side-effects of existing other chemotherapeutic agents. The compounds are synthesized by forming esters of ascorbic acid with either monomer of prostaglandin B.sub.2 or oligomers of prostaglandin B.sub.2. When compared with ascorbic acid in its original form, these esters have the following advantageous features: (a) they have high affinity to membrane lipids, thus they are more easily incorporated into cells; (b) they have a remarkable anti-oxidant activity; (c) these novel compounds can protect the cells and cell membranes by scavenging free radicals, which are known to deteriorate cell membranes; (d) these compounds possess anti-cancer activity; (e) they enhance the anti-cancer activity of existing other anti-cancer agents; and (f) they reduced the toxic side effects of other existing anti-cancer agents. These compounds can be administered orally, subcutaneously, intramuscularly, intravenously or topically.

REFERENCES:
patent: 4245111 (1981-01-01), Polis
patent: 4389414 (1983-06-01), Kent

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