Apigenin

Publication Title: 
Mycoses

Dermatophytes are the most common causative agents of cutaneous mycosis and remain a major public health problem in spite of the availability of an increasing number of antifungal drugs. It was, therefore considered necessary to pursue the screening of different extracts (compounds) of selected traditional medicinal plants reportedly having antidermatophyte potential. The aim of this study was to isolate and identify specific compound from the most active extract (free flavonoid) of stem of Terminalia chebula of the selected plants to treat dermatophytosis induced on experimental mice.

Author(s): 
Singh, Geeta
Kumar, Padma
Joshi, Suresh Chandra
Publication Title: 
Zhongguo Zhong Yao Za Zhi = Zhongguo Zhongyao Zazhi = China Journal of Chinese Materia Medica

OBJECTIVE: To study the chemical constituents in rhizome of Matteuccia struthiopteris. METHOD: The compounds were isolated by normal phase silica gel chromatography. The structures were identified by physical and spectral data. RESULT: Six compounds were isolated and identified as woodwardic acid (1), ergost-6,22-diene-3beta,5alpha,8alpha-triol (2), apigenin (3), riboflavin (4), 4-O-beta-D-glucopyranosyl-p-coumaric acid (5), 4-O-beta-D-glucopyranosylcaffeic acid (6). CONCLUSION: All the compounds were obtained from this plant for the first time.

Author(s): 
Yang, Lan
Wang, Man-Yuan
Zhao, Yu-ying
Tu, You-you
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

The purpose of present study was to determine the intestinal absorption and metabolism of genistein and its analogs to better understand the mechanisms responsible for their low oral bioavailability. The Caco-2 cell culture model and a perfused rat intestinal model were used for the study. In both models, permeabilities of aglycones (e.g., genistein) were comparable to well absorbed compounds, such as testosterone and propranolol.

Author(s): 
Liu, Yan
Hu, Ming
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The purpose of this study was to determine the importance of intestinal disposition in the first-pass metabolism of flavonoids. A four-site perfused rat intestinal model, rat liver and intestinal microsomes, Caco-2 cell microsomes, and the Caco-2 cell culture model were used. In the four-site model, approximately 28% of perfused aglycones are absorbed (approximately 450 nmol/30 min). Both absorption and subsequent excretion of metabolites were rapid and site-dependent (p < 0.05).

Author(s): 
Chen, Jun
Lin, Huimin
Hu, Ming
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The purpose of this study was to determine the mechanisms responsible for intestinal disposition of apigenin in the human Caco-2 cell culture model. The results indicated that most of the absorbed apigenin (10 microM) were conjugated and only a small fraction was transported intact. The amounts of conjugates excreted, especially that of the sulfate, were dependent on days-post-seeding. Apical efflux of apigenin sulfate did not change with concentration of apigenin (4 to 40 microM), whereas its basolateral efflux increased (p < 0.01) with concentration and plateaued at about 25 microM.

Author(s): 
Hu, Ming
Chen, June
Lin, Huimin
Publication Title: 
Molecular Cancer Therapeutics

Apigenin (4',5,7-trihydroxyflavone) is a promising chemopreventive agent abundantly present in fruits and vegetables that has been shown to promote cell cycle arrest and apoptosis in various malignant cell lines. To determine whether pharmacologic intervention with apigenin has a direct growth inhibitory effect on human prostate tumors implanted in athymic nude mice, we examined cell cycle regulatory molecules as precise molecular targets of apigenin action.

Author(s): 
Shukla, Sanjeev
Gupta, Sanjay
Publication Title: 
Cell Cycle (Georgetown, Tex.)

Apigenin, a dietary plant-flavonoid has shown anti-proliferative and anticancer properties, however the molecular basis of this effect remains to be elucidated. We studied the molecular events of apigenin action in human prostate cancer cells. Treatment of LNCaP and PC-3 cells with apigenin causes G0-G1 phase arrest, decrease in total Rb protein and its phosphorylation at Ser780 and Ser807/811 in dose- and time-dependent fashion.

Author(s): 
Shukla, Sanjeev
Gupta, Sanjay
Publication Title: 
Cancer Research

Deregulation of beta-catenin signaling is an important event in the genesis of several human malignancies including prostate cancer. We investigated the effects of apigenin, a naturally occurring plant flavone, on prostate carcinogenesis in TRAMP mice and further elucidated its mechanism of action. Oral intake of apigenin by gavage at doses of 20 and 50 microg/mouse/d, 6 days per week for 20 weeks, significantly decreased tumor volumes of the prostate as well as completely abolished distant-site metastases to lymph nodes, lungs, and liver in TRAMP mice.

Author(s): 
Shukla, Sanjeev
Maclennan, Gregory T.
Flask, Chris A.
Fu, Pingfu
Mishra, Anil
Resnick, Martin I.
Gupta, Sanjay
Publication Title: 
Frontiers in Bioscience: A Journal and Virtual Library

The development of cancer is associated with disorders in the regulation of the cell cycle. The purpose of this review is to briefly summarize the known sequence of events that regulate cell cycle progression with an emphasis on the checkpoints and the mechanisms cell employ to insure DNA stability in the face of genotoxic stress. Key transitions in the cell cycle are regulated by the activities of various protein kinase complexes composed of cyclin and cyclin-dependent kinases (CDK) molecules.

Author(s): 
Meeran, Syed Musthapa
Katiyar, Santosh Kumar
Publication Title: 
Free Radical Biology & Medicine

Apigenin, a plant flavone, potentially activates wild-type p53 and induces apoptosis in cancer cells. We conducted detailed studies to understand its mechanism of action. Exposure of human prostate cancer 22Rv1 cells, harboring wild-type p53, to growth-suppressive concentrations (10-80 microM) of apigenin resulted in the stabilization of p53 by phosphorylation on critical serine sites, p14ARF-mediated downregulation of MDM2 protein, inhibition of NF-kappaB/p65 transcriptional activity, and induction of p21/WAF-1 in a dose- and time-dependent manner.

Author(s): 
Shukla, Sanjeev
Gupta, Sanjay

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