Testosterone 5?-reductase inhibitor bisnaphthoquinone derivative fromImpatiens balsamina

Ishiguro, Kyoko; Oku, Hisae; Kato, Toyonari

doi:10.1002/(sici)1099-1573(200002)14:1<54::aid-ptr540>3.0.co;2-q

Cited by 23 publications

(2 citation statements)

References 20 publications

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“…1,4-naphthoquinone was extracted from a natural source for the first time by Ishiguro et al that showed the significant testosterone 5AR inhibitory activity (57). Al-though Ishiguro et al examined the inhibitory activity of 1,4-naphthoquinone, the current study findings showed that it has the lowest binding energy (-7.1 kcal/mol), compared to other inhibitors.…”

Section: Discussionmentioning

confidence: 62%

Identification of Beta-Sitosterol and Stigmasterol as Possible Inhibitors of 5 Alpha-Reductase 1: An In-Silico Study

Zamani

Mokhtari

Dehghanian

2022

Precis Med Clin OMICS

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Background: Dihydrotestosterone (DHT), the most critical pathogenic androgen in hair loss, is identified as an etiologic factor of androgenetic alopecia (AGA). The AGA is a genetically common disorder among men and is characterized by the progressive conversion of hair follicles into small vellus hair. Steroid 5 alpha-reductase type 1 (5AR1) is a crucial target responsible for this gradual replacement. The 5AR1 function is determined by converting testosterone to DHT. The inhibitors of 5AR1 play their role by blocking the DHT production pathway. Objectives: This study focused on the potent inhibitors of the 5AR1 enzyme to suggest effective synthetic drugs for restoring hair loss with fewer side effects. Methods: The three-dimensional structure of 5AR1 was created using homology modeling methods. Then, the inhibitory effects of some significant compounds from natural sources were examined on the 5AR1 protein using molecular docking approaches. Results: The obtained results suggest that two natural compounds isolated from Serenoa repens, including beta-sitosterol and stigmasterol, could inhibit the regular activity of 5AR1 and can be recommended as safe and novel AGA medicines for hair restoration.

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Section: Discussionmentioning

confidence: 62%

Identification of Beta-Sitosterol and Stigmasterol as Possible Inhibitors of 5 Alpha-Reductase 1: An In-Silico Study

Zamani

Mokhtari

Dehghanian

2022

Precis Med Clin OMICS

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“…Especially 4-azasteroids such as finasteride and dutasteride have been developed for clinical purposes [4], [5]. Naturally occurring non-steroidal inhibitors of 5a-reducatse have been reported, for example, (±)-epigallocatechin 3-gallate [6], chlorophorin [7], bisnaphthoquinone derivatives [8], ostenol [9] and a-linolenic acid [10].…”

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confidence: 99%

Torilin fromTorilis japonica,as a New Inhibitor of Testosterone 5α-Reductase

2003

Planta med

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The methanolic extract of the fruits of Torilis japonica showed a potent inhibition against 5 alpha-reductase activity in vitro. Bioassay-guided fractionation of the methanol extract of the fruits followed by repeated silica gel chromatography led to the isolation of an active principle and its structure was identified as torilin on the basis of spectroscopic data. Torilin (IC50 = 31.7 +/- 4.23 microM) showed a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 +/- 24.62 microM) but was weaker than finasteride. (IC50 = 0.38 +/- 0.06 microM). Simple guaiane-type compounds, such as (-)-guaiol and guaiazulene showed weak inhibitory effects on the 5 alpha-reductase activity with IC50 values of f 81.6 microM and 100.8 microM, respectively, while azulene was not active. These results suggest that both degrees of unsaturation and the side-chain in the guaiane skeleton are important for the manifestation of 5 alpha-reductase inhibition.

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Topical and oral complementary and alternative medicine in acne: A consideration of context

Magin¹,

Adams²,

Pond³

et al. 2012

Traditional, Complementary and Integrative Medicine

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Testosterone 5?-reductase inhibitor bisnaphthoquinone derivative fromImpatiens balsamina

Cited by 23 publications

References 20 publications

Identification of Beta-Sitosterol and Stigmasterol as Possible Inhibitors of 5 Alpha-Reductase 1: An In-Silico Study

Identification of Beta-Sitosterol and Stigmasterol as Possible Inhibitors of 5 Alpha-Reductase 1: An In-Silico Study

Torilin fromTorilis japonica,as a New Inhibitor of Testosterone 5α-Reductase

Topical and oral complementary and alternative medicine in acne: A consideration of context

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