2. Academic Validation
  3. Rapid, microwave-accelerated synthesis and anti-osteoporosis activities evaluation of Morusin scaffolds and Morusignin L scaffolds

Rapid, microwave-accelerated synthesis and anti-osteoporosis activities evaluation of Morusin scaffolds and Morusignin L scaffolds

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2389-2396. doi: 10.1016/j.bmcl.2017.04.018.
Bing Lin 1,  Jun-Fei Huang 1,  Xiong-Wei Liu 1,  Xi-Tao Ma 2,  Xiong-Li Liu 3,  Yi Lu 1,  Ying Zhou 4,  Feng-Min Guo 1,  Ting-Ting Feng 5
Affiliations

Affiliations

  • 1 Guizhou Engineering Center for Innovative Traditional Chinese Medicine and Ethnic Medicine, Guizhou University, Guiyang 550025, China.
  • 2 Adverse Drug Reaction Department, Affiliated Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu 610072, China.
  • 3 Guizhou Engineering Center for Innovative Traditional Chinese Medicine and Ethnic Medicine, Guizhou University, Guiyang 550025, China. Electronic address: xlliu1@gzu.edu.cn.
  • 4 Guizhou Engineering Center for Innovative Traditional Chinese Medicine and Ethnic Medicine, Guizhou University, Guiyang 550025, China. Electronic address: yzhou71@yeah.net.
  • 5 Guizhou Engineering Center for Innovative Traditional Chinese Medicine and Ethnic Medicine, Guizhou University, Guiyang 550025, China. Electronic address: ttfeng@gzu.edu.cn.
PMID: 28427808 DOI: 10.1016/j.bmcl.2017.04.018
Abstract

Described herein is a facile and efficient methodology toward the synthesis of Morusin scaffolds and Morusignin L scaffolds 4-9 and 12via a novel three-step approach (Michael addition or prenylation, cyclization and cyclization) and use a rapid, microwave-accelerated cyclization as the key step. Furthermore, their biological activities have been preliminarily demonstrated by in vitro evaluation for anti-osteoporosis activity. These Morusin, Morusignin L and newly synthesized compounds 5b, 6a, 8e, 8f greatly exhibited the highest potency, especially at the 10-5mol/L (P<0.01), and had good in vitro anti-osteoporosis activities using the commercially available standard drug Ipriflavone as a positive control. The mechanisms associated with anti-osteoporosis effects of these compounds may be through the inhibition of TRAP Enzyme activity and bone resorption in osteoclasts, and promotion effect of osteoblast proliferation in vitro. The results indicated that Morusin scaffolds and Morusignin L scaffolds may be useful leads for further anti-osteoporosis activity screenings.

Keywords

Anti-osteoporosis activity; Bone resorption; Morusignin L; Morusin; TRAP enzyme.

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