- Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance
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Glucose intolerance is associated with metabolic syndrome and type 2 diabetes mellitus (T2DM) while some new therapeutic drugs, such as rosiglitazone (Rosi), for T2DM can cause severe cardiovascular side effects. Herein we report the synthesis of Rosi-ferulic acid (FA)-nitric oxide (NO) donor trihybrids to improve glucose tolerance and minimize the side effects. In comparison with Rosi, the most active compound 21 exhibited better effects on improving glucose tolerance, which was associated with its NO production, antioxidant and anti-inflammatory activities. Furthermore, 21 displayed relatively high stability in the simulated gastrointestinal environments and human liver microsomes, and released Rosi in plasma. More importantly, 21, unlike Rosi, had little stimulatory effect on the membrane translocation of aquaporin-2 (AQP2) in kidney collecting duct epithelial cells. These, together with a better safety profile, suggest that the trihybrids, like 21, may be promising candidates for intervention of glucose intolerance-related metabolic syndrome and T2DM.
- Liu, Jingchao,Huang, Zhangjian,Ma, Wenhuan,Peng, Sixun,Li, Yunman,Miranda, Katrina M.,Tian, Jide,Zhang, Yihua
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p. 650 - 665
(2018/11/27)
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- benzyl ethylene acrylic farnesyl thiophosphoro salicylic acid derivatives and its preparation and use
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The invention discloses a phenyl acrylic acid farnesyl thiosalicylic acid (FTA) derivative as well as a preparation method and an application. The phenyl acrylic acid farnesyl thiosalicylic acid derivative is a compound of a formula (I) in the specification, wherein X1 represents O or NH; X2 represents O or NH; n is equal to 1- 3; R represents H or OCH3. By coupling ferulic acid and p-hydroxy cinnamic acid fragments with carboxyl of FTA, the capability of a target molecule in scavenging free radicals is improved, the anti-tumor effect of the molecule is improved, and then a compound with anti-tumor activity or anti-inflammatory activity higher than those of FTA is obtained.
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Paragraph 0101; 0128-0130
(2017/01/23)
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- Benzenediol-berberine hybrids: Multifunctional agents for Alzheimer's disease
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We designed and synthesized a series of hybrid molecules, in an effort to identify novel multifunctional drug candidates for Alzheimer's disease (AD), by reacting berberine with benzenediol, melatonin, and ferulic acid. The products were evaluated for: (i
- Jiang, Huailei,Wang, Xu,Huang, Ling,Luo, Zonghua,Su, Tao,Ding, Ke,Li, Xingshu
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experimental part
p. 7228 - 7235
(2012/01/14)
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- Design and synthesis of novel NO-donor-ferulic acid hybrids as potential antiatherosclerotic drug candidates a
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Novel NO-donor-ferulic acid hybrids were designed and synthesized through a symbiotic approach using ferulic acid and three different NO-donating groups, such as nitric ester, 4-hydroxyl-3-phenylfuroxan, and 4-hydroxymethyl-3- phenylsulfonylfuroxan. Antioxidant, nitric oxide release, and vasodilator properties studies showed that the target phenylsulfonylfuroxan 14, especially 14c, while keeping the antioxidant activity, showed more NO release activity and vasodilating activity than isosorbide dinitrate (ISDN). Thus, 14c may be considered a novel potent anti-atherosclerosis drug candidate.
- Li, Nian-Guang,Wang, Rong,Shi, Zhi-Hao,Tang, Yu-Ping,Li, Bao-Quan,Wang, Zhen-Jiang,Song, Shu-Lin,Qian, Li-Hua,Wei, Li,Yang, Jian-Ping,Yao, Li-Juan,Xi, Jun-Zuan,Xu, Jia,Feng, Feng,Qian, Da-Wei,Duan, Jin-Ao
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experimental part
p. 405 - 415
(2012/05/05)
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