Soyasaponin I, a Potent and Specific Sialyltransferase Inhibitor

Wu, Ching‐Yuan; Hsu, Chi-Cheng; Chen, Shui‐Tein; Tsai, Ying-Chieh

doi:10.1006/bbrc.2001.5002

Cited by 46 publications

(24 citation statements)

References 19 publications

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“…The competitive ST inhibitor, soyasaponin I (SsaI, K i = 2.3μM) was shown to affect CMP-Neu5Ac binding to ST, but did not inhibit other glycosyltransferases and glycosidases [18]. Further, SsaI inhibited α2,3-linked sialic acid expression in B16F10 melanoma and MDA-MB-231 breast cancer cell lines that resulted in increased adhesion and decreased migration and invasiveness of the two cell lines [19, 20].…”

Section: Introductionmentioning

confidence: 99%

α2,3-sialyltransferase type I regulates migration and peritoneal dissemination of ovarian cancer cells

et al. 2017

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Epithelial ovarian cancer (EOC) has the highest mortality rate among gynecologic cancers due to advanced stage presentation, peritoneal dissemination, and refractory ascites at diagnosis. We investigated the role of α2,3-sialyltransferase type I (ST3GalI) by analyzing human ovarian cancer datasets and human EOC tissue arrays. We found that high expression of ST3GalI was associated with advanced stage EOC. Transwell migration and cell invasion assays showed that high ST3GalI expression enhanced migration of EOC cells. We also observed that there was a linear relation between ST3GalI expression and epidermal growth factor receptor (EGFR) signaling in EOC patients, and that high ST3GalI expression blocked the effect of EGFR inhibitors. Co-Immunoprecipitation experiments demonstrated that ST3GalI and EGFR were present in the same protein complex. Inhibition of ST3GalI using a competitive inhibitor, Soyasaponin I (SsaI), inhibited tumor cell migration and dissemination in the in vivo mouse model with transplanted MOSEC cells. Further, SsaI synergistically enhanced the anti-tumor effects of EGFR inhibitor on EOC cells. Our study demonstrates that ST3GalI regulates ovarian cancer cell migration and peritoneal dissemination via EGFR signaling. This suggests α2,3-linked sialylation inhibitors in combination with EGFR inhibitors could be effective agents for the treatment of EOC.

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Section: Introductionmentioning

confidence: 99%

α2,3-sialyltransferase type I regulates migration and peritoneal dissemination of ovarian cancer cells

et al. 2017

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“…Soyasaponin I, which is a natural compound purified from soybean (20), has been shown to be an ST3 b-galactoside a-2,3-sialyltransferase I (ST3Gal I) inhibitor. It effectively inhibits breast cancer cell MDA-MB-231 and murine melanoma cell, B16F10, from metastasis in vivo (21,22).…”

Section: Introductionmentioning

confidence: 99%

A Novel Sialyltransferase Inhibitor Suppresses FAK/Paxillin Signaling and Cancer Angiogenesis and Metastasis Pathways

et al. 2011

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Increased sialyltransferase (ST) activity promotes cancer cell metastasis, and overexpression of cell surface sialic acid correlates with poor prognosis in cancer patients. To seek therapies targeting metastasis for cancer treatment, we developed a novel ST inhibitor, Lith-O-Asp, and investigated its antimetastatic and antiangiogenic effects and mechanisms. We found that cells treated with Lith-O-Asp showed a reduction of activity on various ST enzymes by in vitro and cell-based activity analyses. Lith-O-Asp inhibited migration and invasion abilities in various cancer cell lines and showed inhibitory effect on the angiogenic activity of human umbilical vein endothelial cells. Indeed, Lith-O-Asp treatment consequently delayed cancer cell metastasis in experimental and spontaneous metastasis assays in animal models. Importantly, Lith-O-Asp decreased the sialic acid modification of integrin-b1 and inhibited the expression of phospho-FAK, phospho-paxillin, and the matrix metalloprotease

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“…It has been reported previously that 1 possesses hepatoprotective activity [19], sialyltransferase inhibitory activity [20], and renin inhibitory activity [21], while 2 possesses anti-hepatotoxic activities [22], hypoglycemic and hypolipidemic activity [23], and anti-herpes virus activity [24]. Although these two compounds have already been isolated from Puerariae Flos, to the best of our knowledge, this is the first report to show their inhibitory activities against 5aR.…”

Section: Isolation Of the Active Constituent From Puerariae Flosmentioning

confidence: 61%

Inhibitory activities of Puerariae Flos against testosterone 5α-reductase and its hair growth promotion activities

et al. 2011

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Crude drugs expected to have an estrogenic effect were screened for their inhibitory activity on testosterone 5α-reductase. Testosterone 5α-reductase is an enzyme catalyzing the conversion of testosterone to dihydrotestosterone, which possesses high affinity for the androgen receptor. Among the crude drugs tested, we focused on Puerariae Flos (the flowers of Pueraria thomsonii) due to its potent inhibitory activity and suitability for commercial use. The 50% ethanolic extract of Puerariae Flos (PF-ext) showed inhibitory activity of 60.2% at 500 μg/ml against testosterone 5α-reductase. Interestingly, it was more potent than that of Puerariae Radix (roots of Pueraria lobata). PF-ext also showed in vivo anti-androgenic activity using a hair growth assay in testosterone-sensitive male C57Black/6NCrSlc strain mice. We demonstrated saponins, including soyasaponin I and kaikasaponin III, to be active components in PF-ext. In addition, hair growth promotion activity in C3H/He mice at 2 mg/mouse/day of the topical administration of PF-ext was demonstrated. Thus, Puerariae Flos is a promising crude drug for treating androgenic alopecia.

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Soyasaponin I, a Potent and Specific Sialyltransferase Inhibitor

Cited by 46 publications

References 19 publications

α2,3-sialyltransferase type I regulates migration and peritoneal dissemination of ovarian cancer cells

α2,3-sialyltransferase type I regulates migration and peritoneal dissemination of ovarian cancer cells

A Novel Sialyltransferase Inhibitor Suppresses FAK/Paxillin Signaling and Cancer Angiogenesis and Metastasis Pathways

Inhibitory activities of Puerariae Flos against testosterone 5α-reductase and its hair growth promotion activities

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