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      Avicequinone C Isolated from Avicennia marina Exhibits 5α-Reductase-Type 1 Inhibitory Activity Using an Androgenic Alopecia Relevant Cell-Based Assay System

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          Abstract

          Avicennia marina (AM) exhibits various biological activities and has been traditionally used in Egypt to cure skin diseases. In this study, the methanolic heartwood extract of AM was evaluated for inhibitory activity against 5α-reductase (5α-R) [E.C.1.3.99.5], the enzyme responsible for the over-production of 5α-dihydrotestosterone (5α-DHT) causing androgenic alopecia (AGA). An AGA-relevant cell-based assay was developed using human hair dermal papilla cells (HHDPCs), the main regulator of hair growth and the only cells within the hair follicle that are the direct site of 5α-DHT action, combined with a non-radioactive thin layer chromatography (TLC) detection technique. The results revealed that AM is a potent 5α-R type 1 (5α-R1) inhibitor, reducing the 5α-DHT production by 52% at the final concentration of 10 µg/mL. Activity-guided fractionation has led to the identification of avicequinone C, a furanonaphthaquinone, as a 5α-R1 inhibitor with an IC 50 of 9.94 ± 0.33 µg/mL or 38.8 ± 1.29 µM. This paper is the first to report anti-androgenic activity through 5α-R1 inhibition of AM and avicequinone C.

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          Most cited references35

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          The 5 Alpha-Reductase Isozyme Family: A Review of Basic Biology and Their Role in Human Diseases

          Despite the discovery of 5 alpha-reduction as an enzymatic step in steroid metabolism in 1951, and the discovery that dihydrotestosterone is more potent than testosterone in 1968, the significance of 5 alpha-reduced steroids in human diseases was not appreciated until the discovery of 5 alpha-reductase type 2 deficiency in 1974. Affected males are born with ambiguous external genitalia, despite normal internal genitalia. The prostate is hypoplastic, nonpalpable on rectal examination and approximately 1/10th the size of age-matched normal glands. Benign prostate hyperplasia or prostate cancer does not develop in these patients. At puberty, the external genitalia virilize partially, however, secondary sexual hair remains sparse and male pattern baldness and acne develop rarely. Several compounds have been developed to inhibit the 5 alpha-reductase isozymes and they play an important role in the prevention and treatment of many common diseases. This review describes the basic biochemical properties, functions, tissue distribution, chromosomal location, and clinical significance of the 5 alpha-reductase isozyme family.
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            Psychological effect, pathophysiology, and management of androgenetic alopecia in men.

            Androgenetic alopecia In men, or male pattern baldness, is recognized increasingly as a physically and psychologically harmful medical condition that can be managed effectively by generalist clinicians. This article discusses the clinical manifestations, epidemiology, physical and psychosocial importance, pathophysiology, diagnosis, and management of androgenetic alopecia in men. Androgenetic alopecia affects at least half of white men by the age of 50 years. Although androgenetic alopecia does not appear to cause direct physical harm, hair loss can result in physical harm because hair protects against sunburn, cold, mechanical injury, and ultraviolet light. Hair loss also can psychologically affect the balding individual and can Influence others' perceptions of him. A progressive condition, male pattern baldness is known to depend on the presence of the androgen dihydrotestosterone and on a genetic predisposition for this condition, but its pathophysiology has not been elucidated fully. Pharmacotherapy, hair transplantation, and cosmetic aids have been used to manage male pattern baldness. Two US Food and Drug Administration-approved hair-loss pharmacotherapies-the potassium channel opener minoxidil and the dihydrotestosterone synthesis inhibitor finasteride--are safe and effective for controlling male pattern baldness with long-term daily use. Regardless of which treatment modality is chosen for male pattern baldness, defining and addressing the patient's expectations regarding therapy are paramount in determining outcome.
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              Androgenetic alopecia: pathogenesis and potential for therapy

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                Author and article information

                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                23 May 2014
                May 2014
                : 19
                : 5
                : 6809-6821
                Affiliations
                [1 ]Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand; E-Mails: ruchyj@ 123456gmail.com (R.J.); parkpoom.t@ 123456chula.ac.th (P.T.)
                [2 ]Research Unit of Natural Product Biotechnology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand
                [3 ]Division of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand; E-Mail: oramon@ 123456kku.ac.th
                [4 ]Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand
                Author notes
                [* ]Author to whom correspondence should be addressed; E-Mail: dwanchai@ 123456chula.ac.th ; Tel./Fax: +66-2-218-8393.
                Article
                molecules-19-06809
                10.3390/molecules19056809
                6271945
                24858268
                ad187c2d-c3db-47f3-85cb-3bc22777a206
                © 2014 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                : 08 April 2014
                : 18 May 2014
                : 19 May 2014
                Categories
                Article

                avicequinone c,avicennia marina,5α-r1 inhibitory activity,cell-based bioassay

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