Sunday, 3 November 2013

Phytochemicals in Foods - 9 Health Benefits of Coumarin

Coumarin is a phytochemical in the class of Lignans (phytoestrogens), belonging to the flavonoid in Flavonoids (polyphenols), found abundantly in citrus fruits, maize, etc.

Health Benefits
1. Anti tumors
In the investigation of the amphiphilic 7-carboxymethoxy coumarin monoend-functionalized methoxy poly(ethylene glycol) (mPEG-Lys-DCOU) chains and its self-assembled micelles, anti-tumor drug, found that both in vitro and in vivo studies demonstrated that the inhibition efficacy of drug-loaded micelles were comparable to that of doxorubicin hydrochloride. mPEG-Lys-DCOU micelles are promising carriers for anti-tumor drug delivery, according to "A novel micelle of coumarin derivative monoend-functionalized PEG for anti-tumor drug delivery: in vitro and in vivo study" by Lai Y, Long Y, Lei Y, Deng X, He B, Sheng M, Li M, Gu Z.(1)

2. Gastric cancer
In the investigation of
an anti-mitotic potential of the novel synthetic coumarin-based compound, 7-diethylamino-3(2'-benzoxazolyl)-coumarin, in 5-fluorouracil-resistant human gastric cancer cell line SNU-620-5FU and its parental cell SNU-620, found that this compound enhances caspase-dependent apoptotic cell death via decreased expression of anti-apoptotic genes. Taken together, our data strongly support anti-mitotic potential of 7-diethylamino-3(2'-benzoxazolyl)-coumarin against drug-resistant cancer cells which will prompt us to further develop as a novel microtubule inhibitor for drug-resistant cancer chemotherapy, according to "Anti-mitotic potential of 7-diethylamino-3(2'-benzoxazolyl)-coumarin in 5-fluorouracil-resistant human gastric cancer cell line SNU620/5-FU' by Kim NH, Kim SN, Oh JS, Lee S, Kim YK.(2)

3. Anti cancers
In the identification of a novel coumarin analogue with the highest anticancer activity and further to its anticancer mechanisms, found that The compound had a broad spectrum of anticancer activity against 9 cancer cell lines derived from colon cancer, breast cancer, liver cancer, cervical cancer, leukemia, epidermoid cancer with IC(50) value of 75 nmol/L-1.57 μmol/L but with low cytotocitity against WI-38 human lung fibroblasts (IC(50) value of 12.128 μmol/L). The compound (0.04-10 μmol/L) induced G(2)-M phase arrest in HeLa cells in a dose-dependent manner, which was reversible after the compound was removed. The compound (10-300 μmol/L) induced the depolymerization of purified porcine tubulin in vitro. Finally, the compound (0.04-2.5 μmol/L) induced apoptosis of HeLa cells in dose- and time-dependent manners.Conclusion:6-Chloro-4-(methoxyphenyl) coumarin is a novel microtubule-targeting agent that induces G(2)-M arrest and apoptosis in HeLa cells, according to "Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G(2)-M arrest and apoptosis in HeLa cells" by Ma YM, Zhou YB, Xie CM, Chen DM, Li J.(3)

4. Antioxidant and anti-inflammatory activities
In the evaluation of the antioxidant and antiinflammatory activities of methanolic extract of whole plants of Angelica decursiva, and its solvent soluble fractions via in vitro, found that Among the tested fractions, the ethyl acetate fraction was found as the most active antioxidant fraction together with significant anti-inflammatory effect. From the active ethyl acetate fraction, four coumarin derivatives consisting of nodakenin, nodakenetin, umbelliferone, and umbelliferone-6-carboxylic acid, along with a phenolic compound, vanillic acid, were isolated. Among them, umbelliferone 6-carboxylic acid and vanillic acid were isolated for the first time from this plant. In all antioxidant assays, vanillic acid showed the highest antioxidant potential followed by umbelliferone 6-carboxylic acid among the isolated compounds. In the anti-inflammatory assay, umbelliferone 6-carboxylic acid exhibited the highest inhibitory activity against lipopolysaccharide-induced NO production in RAW 264.7 cells with an IC(50) value of 72.98 μg/mL, according to "In vitro antioxidant and anti-inflammatory activities of Angelica decursiva" by Zhao D, Islam MN, Ahn BR, Jung HA, Kim BW, Choi JS.(4)

5. Antimicrobial activity
In the investigation of the antibacterial and antifungal activities of Ulopterol, a coumarin isolated as another major active antimicrobial principle, found that the ethyl acetate extract which was found to possess highest antimicrobial activity was subjected to activity guided fractionation by column chromatography over silica gel. This resulted in the isolation of the coumarin, Ulopetrol, an active principle besides Flindersine which was reported by us earlier, according to " Antimicrobial activity of Ulopterol isolated from Toddalia asiatica (L.) Lam.: A traditional medicinal plant" by Karunai Raj M, Balachandran C, Duraipandiyan V, Agastian P, Ignacimuthu S.(5)

6. Alzheimer's disease
In a review of the differently synthesized coumarin derivatives as AChE inhibitors for management of AD indicated that the coumarin template for synthesizing novel AChE inhibitors with additional pharmacological activities including decrease in beta-amyloid (Aβ) deposition and beta-secretase inhibition are also important for AD management, according to "A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease" by Anand P, Singh B, Singh N.(6)

7. Neuroprotective effects
In the investigation of the potential protective effects of osthole, a coumarin compound isolated from the plant-derived herb Cnidium monnieri in adult rats in the setting of traumatic brain injury (TBI), found that pretreatment with osthole (40 mg/kg) significantly increased the activity of SOD, the level of GSH, and the ratio of Bcl-2/Bax, and also reduced the level of MDA, the expression of active caspase-3, and the number of apoptotic cells at 24h after TBI. In summary, these results suggested that osthole had a neuroprotective effect against TBI, and the protection may be associated with its antioxidative and antiapoptotic functions, according to "Neuroprotective effects of osthole pretreatment against traumatic brain injury in rats" by He Y, Qu S, Wang J, He X, Lin W, Zhen H, Zhang X.(7)

8. Anticonvulsants
In the investigation of a series of coumarin incorporated 1,2,4- triazole compounds (1-14) for their possible anticonvulsant and neurotoxic properties, log P values, pharmacophoric mapping and three dimensional structure analysis, found that Compound (6) with para-fluoro substitution showed significant anticonvulsant activity, according to "Coumarin incorporated triazoles: a new class of anticonvulsants" by Bhat MA, Al-Omar MA.(8)

9. Hepatitis B virus
In the investigation of three new lignans, erythro-strebluslignanol (1), threo-7'-methoxyl strebluslignanol (2) and erythro-7'-methoxyl strebluslignanol (3), together with twelve known compounds were isolated from the n-butanol and chloroform fractions of the heartwood of Streblus asper, found that 6-hydroxyl-7-methoxyl-coumarin (5) and ursolic acid (10) showed anti-HBV activities, with IC(50) values of 29.60μM and 89.91μM for HBsAg at no cytotoxicity, and IC(50) values of 46.41μM and 97.61μM for HBeAg at no cytotoxicity, respectively, according to "Lignans from the heartwood of Streblus asper and their inhibiting activities to Hepatitis B virus" by Li LQ, Li J, Huang Y, Wu Q, Deng SP, Su XJ, Yang RY, Huang JG, Chen ZZ, Li S.(9)

(10). Etc.

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