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Hypophyllanthin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hypophyllanthin图片
CAS NO:33676-00-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Hypophyllanthin是Phyllanthus spp中的主要木脂素,具有很强的抗炎活性。
Cas No.33676-00-5
别名(7S,8S,9R)-9-(3,4-二甲氧基苯基)-6,7,8,9-四氢-4-甲氧基-7,8-双(甲氧基甲基)萘并[1,2-D]-1,3-二恶茂,NSC 619044
化学名(7S,8S,9R)-9-(3,4-dimethoxyphenyl)-6,7,8,9-tetrahydro-4-methoxy-7,8-bis(methoxymethyl)-naphtho[1,2-d]-1,3-dioxole
Canonical SMILESCOC[C@@H]1[C@@H](COC)CC(C=C(OC)C2=C3OCO2)=C3[C@H]1C4=CC(OC)=C(OC)C=C4
分子式C24H30O7
分子量430.5
溶解度≤0.2mg/ml in ethanol;10mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Hypophyllanthin is a P-glycoprotein (P-gp) inhibitor.

P-glycoprotein (P-gp) and multidrug resistance protein 2 (MRP2), two major drug efflux pumps, play a key role in the translocation of certain drugs and xenobiotics via restrictive barriers. The presence of P-gp and other efflux transporters on the apical membrane of enterocytes can limit absorption and therefore oral bioavailability. Inhibition of the activity of these transporters can increase plasma levels of various drugs that are their substrates, resulting in changes in drug efficacy and adverse reactions.

In vitro: Previous study found that hypophyllanthin could inhibit P-gp function with comparable potencies, but could not affect MRP2 activity. When hypophyllanthin was washed out before addition of substrate, the inhibitory action against P-gp function was lost. These results indicated the reversibility of the inhibition. Moreover, prolonged exposure of the Caco-2 cells to hypophyllanthin up to 7 days had no effect on P-gp function [1].

In vivo: A previous study was conducted to evaluate the effect of carbofuran on estrous cycle and follicular growth in virgin Wister rats as well as recovering from the damaged estrous cycle with treatment of hypophyllanthin. Hypophyllanthin is non-steroidal plant molecule with estrogen-like activities, but with an estrogen-type activity. Hypophyllanthin was capable of interacting with estrogen receptors, showing both agonist and antagonist methods of action. Therefore, hypophyllanthin was found to be systemically transformed into enterolignan, which is known to be responsible for augmenting estrus cycle in rats [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] N.  Sukhaphirom, N. Vardhanabhuti, H. Chirdchupunseree, et al. Phyllanthin and hypophyllanthin inhibit function of P-gp but not MRP2 in Caco-2 cells. Journal of Pharmacy and Pharmacology 65, 292-299 (2012).
[2] Aminul Islam et al.  Estrogenic Properties of Phyllanthin and Hypophyllanthin from Phyllanthus amarus against Carbofuran Induced Toxicity in Female Rats. Pharmacologyonline 3: 1006-1016 (2008).