2. Academic Validation
  3. New dammarane-type triterpenoid saponins from Gynostemma pentaphyllum and their Sirt1 agonist activity

New dammarane-type triterpenoid saponins from Gynostemma pentaphyllum and their Sirt1 agonist activity

  • Bioorg Chem. 2021 Nov:116:105357. doi: 10.1016/j.bioorg.2021.105357.
Yun-Yun Lou 1,  Xian Zheng 1,  Ya-Ping Huang 2,  Long Mu 2,  Xiao-Gai Zhang 3,  Zhi-Wei Zhao 1,  Zhe Song 4,  Jian Zhang 5,  Zhi-Qi Yin 6,  Ke Pan 7
Affiliations

Affiliations

  • 1 Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of TCM, China Pharmaceutical University, Nanjing 211198, PR China; Laboratory of Translational Medicine, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, PR China.
  • 2 Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of TCM, China Pharmaceutical University, Nanjing 211198, PR China.
  • 3 Department of Endocrinology, Nanjing Lishui District Hospital of Traditional Chinese Medicine, Nanjing 211200, PR China.
  • 4 Instrumental Analysis Center of CPU, China Pharmaceutical University, Ministry of Education, Nanjing 210009, PR China.
  • 5 Laboratory of Translational Medicine, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, PR China. Electronic address: [email protected].
  • 6 Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of TCM, China Pharmaceutical University, Nanjing 211198, PR China. Electronic address: [email protected].
  • 7 Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of TCM, China Pharmaceutical University, Nanjing 211198, PR China. Electronic address: [email protected].
PMID: 34562675 DOI: 10.1016/j.bioorg.2021.105357
Abstract

Gynostemma pentaphyllum (Thunb.) Makino (Cucurbitaceae family) is a perennial creeping plant with a common Chinese name of "south ginseng". To date, more than 250 individual saponins with dammarane-type skeleton have been isolated from G. pentaphyllum. The purpose of this study was the isolation and structural characterization of novel, minor gypenosides from G. pentaphyllum and evaluation of their SIRT1 agonist activity. Individual saponins from G. pentaphyllum were isolated and purified by a variety of chromatography techniques, and their structures were elucidated by means of various spectroscopic analysis and comparision with the reported data. SIRT1 enzyme activity detection kit was used to preliminarily evaluate the SIRT1 agonist activity of thirty three individual saponins purified from G. pentaphyllum. Fourteen new triterpenoid saponins named gypenoside CII-CXV (1-14) along with twenty six known compounds (15-40) were isolated from G. pentaphyllum. Thirty three of all the isolates were screened for SIRT1 agonist activity, and the results showed that three dammarane-type saponins (2, 18, 37) and one cucurbitane-type saponin 33 exhibited satisfactory SIRT1 agonist activity. These findings suggested that G. pentaphyllum was worthy of further investigation to find small molecule SIRT1 agonist and facilitate their utilization as "south ginseng".

Keywords

Gynostemma pentaphyllum; Minor gypenosides; Sirt1; Triterpenoid saponin.

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