Cancer is a major cause of morbidity and mortality all over the world and a promising area of cancer research is concentrated on chemoprevention by nutritional compounds. Capsaicin, traditionally used as a food additi...Cancer is a major cause of morbidity and mortality all over the world and a promising area of cancer research is concentrated on chemoprevention by nutritional compounds. Capsaicin, traditionally used as a food additive and an analgesic, is one of the main pungent ingredients in chili peppers. Recent studies have shown that capsaicin has anti-cancer effects in various types of cancer model. The purpose of this review is to outline the anticarcinogenic effect of capsaicin and its mechanism.展开更多
We report herein the design and synthesis of a series of novel fluoride-containing gossypol derivatives by the condensation reaction of gossypol with fluoride-containing aromatic amine. These fluoride-containing gossy...We report herein the design and synthesis of a series of novel fluoride-containing gossypol derivatives by the condensation reaction of gossypol with fluoride-containing aromatic amine. These fluoride-containing gossypol derivatives were characterized by IR, 1H-NMR and high resolution mass spectral data, then screened as antitumor agents against three human cancer cell lines (HeLa, A-549 and BGC-823) and a normal cell line (VEC) in vitro by using MTT cell proliferation assays. Results revealed that compounds 3a, 3c and 3f exhibited superior anticancer activity against HeLa, compounds 3b,3c, 3e and 3f exhibited superior anticancer activity against A-549, compounds 3b, 3c and 3f exhibited superior anticancer activity against BGC-823 compared to gossypol. In particular, fluorine substituent at the para positions of the phenyl ring showed remarkable inhibitory effects on HeLa?(3c: IC50 = 14.2 μM, 3f:?IC50 = 8.34 μM), A-549(3c: IC50 = 6.32 μM, 3f: IC50 = 9.76 μM) and BGC-823 cells?(3c: IC50 = 8.62 μM, 3f: IC50 = 4.36 μM). Furthermore, all the compounds 3a-3f exhibited lessened cytotoxicity against VEC compared to gossypol.展开更多
Pd-catalyzed carbonylation,as an efficient synthetic approach to the installation of carbonyl groups in organic compounds,has been one of the most important research fields in the past decade.Although elegant reaction...Pd-catalyzed carbonylation,as an efficient synthetic approach to the installation of carbonyl groups in organic compounds,has been one of the most important research fields in the past decade.Although elegant reactions that allow highly selective carbonylations have been developed,straightforward routes with improved reaction activity and broader substrate scope remain long-term challenges for new practical applications.Here,we show a new type of synergistic Cu/Pd-catalyzed carbonylation reaction using alcohols and dioxgen as the carbonyl sources.A broad range of aryl iodides and alcohols are compatible with this protocol.The reaction is concise and practical due to the ready availability of the starting materials and the scalability of the reaction.In addition,the reaction affords lactones and lactams in an intermolecular fashion.Moreover,DFT calculations have been performed to study the detailed mechanisms.展开更多
文摘Cancer is a major cause of morbidity and mortality all over the world and a promising area of cancer research is concentrated on chemoprevention by nutritional compounds. Capsaicin, traditionally used as a food additive and an analgesic, is one of the main pungent ingredients in chili peppers. Recent studies have shown that capsaicin has anti-cancer effects in various types of cancer model. The purpose of this review is to outline the anticarcinogenic effect of capsaicin and its mechanism.
文摘We report herein the design and synthesis of a series of novel fluoride-containing gossypol derivatives by the condensation reaction of gossypol with fluoride-containing aromatic amine. These fluoride-containing gossypol derivatives were characterized by IR, 1H-NMR and high resolution mass spectral data, then screened as antitumor agents against three human cancer cell lines (HeLa, A-549 and BGC-823) and a normal cell line (VEC) in vitro by using MTT cell proliferation assays. Results revealed that compounds 3a, 3c and 3f exhibited superior anticancer activity against HeLa, compounds 3b,3c, 3e and 3f exhibited superior anticancer activity against A-549, compounds 3b, 3c and 3f exhibited superior anticancer activity against BGC-823 compared to gossypol. In particular, fluorine substituent at the para positions of the phenyl ring showed remarkable inhibitory effects on HeLa?(3c: IC50 = 14.2 μM, 3f:?IC50 = 8.34 μM), A-549(3c: IC50 = 6.32 μM, 3f: IC50 = 9.76 μM) and BGC-823 cells?(3c: IC50 = 8.62 μM, 3f: IC50 = 4.36 μM). Furthermore, all the compounds 3a-3f exhibited lessened cytotoxicity against VEC compared to gossypol.
基金supported by the Science Foundation for Distinguished Young Scholars for Guangdong Province(2020B1515020026)the Science and Technology Program of Guangzhou(202103000089)+6 种基金the Innovation Team Project of Universities in Guangdong Province(2020KCXTD009)the Scientific Research Projects for Key Disciplines of Guangdong Province(2019-GDXK-0009)the Key Projects of Social Welfare and Basic Research of Zhongshan City(2020B2007)the Innovation and Strong School Project of Guangdong Pharmaceutical University(2018KQNCX131)Guangdong Cosmetics Engineering&Technology Research CenterProvincial Experimental Teaching Demonstration Center of Chemistry&Chemical EngineeringSpecial Funds of Key Disciplines Construction from Guangdong and Zhongshan Cooperating。
文摘Pd-catalyzed carbonylation,as an efficient synthetic approach to the installation of carbonyl groups in organic compounds,has been one of the most important research fields in the past decade.Although elegant reactions that allow highly selective carbonylations have been developed,straightforward routes with improved reaction activity and broader substrate scope remain long-term challenges for new practical applications.Here,we show a new type of synergistic Cu/Pd-catalyzed carbonylation reaction using alcohols and dioxgen as the carbonyl sources.A broad range of aryl iodides and alcohols are compatible with this protocol.The reaction is concise and practical due to the ready availability of the starting materials and the scalability of the reaction.In addition,the reaction affords lactones and lactams in an intermolecular fashion.Moreover,DFT calculations have been performed to study the detailed mechanisms.