Publications

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Journal Article
Sesquiterpenes from Cymbopogon proximus, El-Askary, Hesham I., Meselhy Meselhy R., and Galal Ahmed M. , Molecules, Volume 8, Issue 9, p.670-677, (2003) Abstract
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Shikometabolins A, B, C and D, novel dimeric naphthoquinone metabolites obtained from shikonin by human intestinal bacteria, Meselhy, Meselhy R., KADOTA Shigetoshi, Tsubono Koji, KUSAI Akihiko, Hattori Masao, and NAMBA Tsuneo , Tetrahedron letters, Volume 35, Issue 4, p.583-586, (1994) Abstract
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Simultaneous determination of triterpene saponins in ginseng drugs by high-performance liquid chromatography, Zhu, Shu, Zou Kun, Cai Shaoqing, Meselhy Meselhy Ragab, and Komatsu Katsuko , Chemical and pharmaceutical bulletin, Volume 52, Issue 8, p.995-998, (2004) Abstract
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Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells., Kohyama, Aki, Yokoyama Rei, Dibwe Dya Fita, El-Mekkawy Sahar, Meselhy Meselhy R., Awale Suresh, and Matsuya Yuji , Bioorganic & medicinal chemistry letters, Volume 30, Issue 7, p.126964, (2020) Abstract

E- and Z-guggulsterones and nine guggulsterone derivatives (GSDs) were synthesized and evaluated for their preferential cytotoxicity against human PANC-1 cell in nutrient deprived medium utilizing antiausterity strategy. Among the synthesized compounds, GSD-1 and GSD-7 showed potent cytotoxicity against PANC-1 cells under nutrient-deprived conditions in a concentration dependent manner, with a PC value of 1.6 μM and 3.2 μM, respectively. The effect of GSD-1 and GSD-7 was further evaluated in a real time using live cell imaging. Both of these compounds altered PANC-1 cell morphology, leading to cell death at sub micromolar concentration range. GSD-1 and GSD-7 also inhibited PANC-1 cell colony formation in a concentration-dependent manner. GSD-1 and GSD-7 are lead structure for the anti-austerity drug development.

Synthetic E-guggulsterone derivative GSD-1 inhibits NF-κB signaling and suppresses the metastatic potential of breast cancer cells., Abdellatef, Amira A., Zhou Yue, Yamada Akane, Elmekkawy Sahar A., Kohyama Aki, Yokoyama Satoru, Meselhy Meselhy R., Matsuya Yuji, Sakurai Hiroaki, and Hayakawa Yoshihiro , Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, Volume 140, p.111737, (2021) Abstract

Guggulsterone (GS) [4,17(20)-pregnadiene-3,16-dione], is the main active phytosterol constituent in guggul, the gum resin of Commiphora wightii (Arnott.) Bhand./Commiphora mukul Engl. tree, and is known for its medicinal effects. In this study, we report that GSD-1, a structurally-related synthetic GS derivative, strongly inhibits NF-κB activation induced by TNF-α. GSD-1 prevented the nuclear translocation of p65 through the blockade of IκBα degradation and p65 phosphorylation, and further inhibited the activation of upstream kinases, including transforming growth factor-β activated kinase 1 (TAK1), IκB kinase (IKK) α, and IKKβ. Furthermore, GSD-1 inhibited the cell-intrinsic activation of NF-κB, and exerted its direct anti-cancer and anti-metastatic effects in both murine and human breast cancer cell lines. This study demonstrated GSD-1 to be an attractive compound to target NF-κB activation that has potential for treating breast cancer growth and metastasis.

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