Disclosed herein are a novel cinnamaldehyde compound represented by Chemical Formula 1 or pharmaceutically acceptable salts thereof. The cinnamaldehyde compound has improved solubility in water and has inhibitory effects on the growth of cancer cells because it induces cell cycle arrest and cell death. Also disclosed are a method of preparing the cinnamaldehyde compound and an anticancer composition including the compound of Chemical Formula 1. ##STR00001##

Korea Research Institute of Bioscience and Biotechnology

Cinnamaldehyde derivatives having improved solubility in water, a method for preparing the same and a pharmaceutical composition comprising the same

The present invention relates to a hybrid anticancer prodrug simultaneously producing cinnamaldehyde and quinone methide. The hybrid anticancer prodrug according to the present invention sequentially releases quinone methide and cinnamaldehyde by H.sub.2O.sub.2 and acidic pH, and thus alkylates antioxidant GSH through the release of quinone methide, thereby inhibiting an antioxidative system and increasing oxidation stress, and generates and accumulates reactive oxygen species (ROS) through the release of cinnamaldehyde, thereby promoting apoptosis, and thus the hybrid anticancer prodrug according to the present invention can be favorably used as an anticancer drug by creating a synergetic anticancer effect through double stimulus-response and sequential treatment action in a cancer cell-specific manner.

INDUSTRIAL COOPERATION FOUNDATION CHONBUK NATIONAL UNIVERSITY

KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY

Industrial Cooperation Foundation Chonbuk National University

Hybrid anticancer prodrug simultaneously producing cinnamaldehyde and quinone methide and method for preparing same

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.

cinnamaldehyde/rakovina

Cinnamaldehyde derivatives having improved solubility in water, a method for preparing the same and a pharmaceutical composition comprising the same

Hybrid anticancer prodrug simultaneously producing cinnamaldehyde and quinone methide and method for preparing same

Cytochrome P450 3A inhibitors and enhancers

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