کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8526907 | 1557988 | 2018 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel tanshinone IIA derivatives for treating pain
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
پزشکی و دندانپزشکی
طب مکمل و جایگزین
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چکیده انگلیسی
Due to ineffectiveness and side effects of existing analgesics, chronic pain has become one of the most complex and difficult problems in the clinic. Monoacylglycerol lipase (MAGL) is an essential hydrolase in the endocannabinoid system and has been identified as a potential target for the treatment of pain. In the present study, we designed and synthesized twelve tanshinone IIA analogs and screened their activity against MAGL. Selected compounds were tested for analgesic activity in vivo, with the acetic acid writhing test model. Among the test compounds, compound III-3 (IC50 120 nmol·Lâ1) showed significant activity against MAGL and ameliorated the clinical progression in the mouse pain model. Additionally, compound III-3, substitution with N-methyl-2-morpholinoacetamide, demonstrated improved solubility relative to tanshinone IIA.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Journal of Natural Medicines - Volume 16, Issue 2, February 2018, Pages 113-124
Journal: Chinese Journal of Natural Medicines - Volume 16, Issue 2, February 2018, Pages 113-124
نویسندگان
Qi-Nan LI, Zhi-Peng HUANG, Qin-Lan GU, Zhuo-Er ZHI, Yu-Han YANG, Long HE, Kai-Li CHEN, Jin-Xin WANG,