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Tamoxifen (TAM), a nonsteroidal antiestrogen, is the most widely used drug for chemotherapy of hormone-dependent breast cancer in women. In the present study, we found a new potential metabolic pathway of TAM via N-linked glucuronic acid conjugation for excretion in humans. TAM N(+)-glucuronide was isolated from a reaction mixture consisting of TAM and(More)
It is known that in humans taking soy food, the phytoestrogens, daidzein (DZ) and genistein (GS), exist as sulfates and glucuronides in the plasma and are excreted as conjugates in urine. To investigate which human sulfotransferase (SULT) isoforms participate in the sulfation of these phytoestrogens, the four major cytosolic SULTs, SULT1A1, SULT1A3,(More)
The phenolic active metabolites, cis-4-hydroxytamoxifen (cis-HO-TAM) and trans-4-hydroxytamoxifen (trans-HO-TAM), of the anti-breast-cancer drug, trans-tamoxifen (TAM), were geometrically selectively glucuronidated in the manner of cis>>trans by microsomes and sulfated in the manner of trans>>cis by cytosol from the liver of 10 human subjects (7 females and(More)
Tamoxifen (TAM), a nonsteroidal antiestrogen, is the most widely used drug for chemotherapy of hormone-dependent breast cancer in women. Trans-4-hydroxy-TAM (trans-4-HO-TAM), one of the TAM metabolites in humans, has been considered to be an active metabolite of TAM because of its higher affinity toward estrogen receptors (ERs) than the parent drug and(More)
We investigated the effect of the female hormone 17beta-estradiol (E2) and the hormone mimic bisphenol A (BPA) on the proliferation and differentiation of rat neural stem/progenitors cells (NS/PCs) cultured from the telencephalon of embryonic day-15 rats. Basic fibroblast growth factor (FGF-2) is a potent mitogen of early generated NS/PCs, and is used for(More)
For the purpose of clarification of pharmacological actions of ginseng saponins we tried the isolation of ginseng saponins on a larger scale and succeeded in the isolation of eight saponins in a pure state and in sufficient amounts for the pharmacological assay. These eight saponins agreed all completely with the authentic samples of Shibata-Shoji and(More)
The pharmacological properties of seven pure saponins isolated from Panax ginseng C. A. Meyer were studied. 1. The ginseng saponins showed weak toxicities in mice. Especially, Rg1, Rf and Rb 1, which contained glucose as a sugar component, were weaker in their toxicities than the rest, which contained arabinose and/or rhamnose. It was also noted that the(More)
In the course of a chemical study on pure ginsenosides, a ginsenoside-Rg2 was isolated as colorless needles, from the lateral root of Panax ginseng C. A. Meyer. For the characterization of Rg2, a chikusetsusaponin-I (ginsenoide-Rg2) was isolated as colorless needles from rhizome of Panax japonicus C. A. Meyer. The optical rotation value of both saponins(More)
THe hemolytic and enzymic investigations of the crude venom from Heterometrus gravimanus scorpion have revealed the presence of both direct and indirect (phospholipase A) hemolysins. The direct hemolysins were isolated from the lyophilized crude venom extract by Sephadex G-100 gel filtration, SP-Sephadex C-25 column chromatography, gel filtration of(More)
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