2. Academic Validation
  3. Lepidiline A Improves the Balance of Endogenous Sex Hormones and Increases Fecundity by Targeting HSD17B1

Lepidiline A Improves the Balance of Endogenous Sex Hormones and Increases Fecundity by Targeting HSD17B1

  • Mol Nutr Food Res. 2020 May;64(10):e1900706. doi: 10.1002/mnfr.201900706.
Chuanjing Cheng 1,  Fukui Shen 1,  Guoyu Ding 1,  Aina Liu 1,  Simeng Chu 1,  Yuejiao Ma 1,  Xiaotao Hou 2,  Erwei Hao 2,  Xiaoying Wang 3,  Yuanyuan Hou 1,  Gang Bai 1
Affiliations

Affiliations

  • 1 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300353, China.
  • 2 Collaborative Innovation Center of Research on Functional Ingredients from Agricultural Residues, Guangxi Key Laboratory of Efficacy Study on Chinese Materia Medica, Guangxi University of Chinese Medicine, Nanning, 530200, China.
  • 3 State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China.
PMID: 32239630 DOI: 10.1002/mnfr.201900706
Abstract

Scope: Maca (Lepidium meyenii), a well-known plant from the Andean highlands of Peru, has been used widely as a nutritional supplement to increase sexual function and fecundity. However, the identity of its active ingredients and how they function remain unknown.

Methods and results: Chemical substances in maca are identified by UPLC-Q-TOF, and the active ingredients are screened through HotMap coupled with an artificial neural network. Lepidiline A (LA), an imidazole alkaloid, is identified as the key active compound. LA affects the balance of endogenous sex Hormones in mice and improves fecundity in Drosophila. Using a molecular LA probe, 17ß-hydroxysteroid dehydrogenase type 1 (HSD17B1) is revealed to be the potential target of LA using a fishing-rod strategy. It is demonstrated with experimental data that LA targets HSD17B1 to enhance the enzyme's activity and increases its bioconversion efficiency of actively formed sex Hormones including estrogen to 17β-estradiol and 4-androsten-3,7-dione to testosterone, which ultimately improves reproductive activity.

Conclusion: LA improves the balance of endogenous sex Hormones and increases fecundity by targeting HSD17B1. This underlying mechanism of action provides a useful insight into the application of maca in the regulation of dietary nutrition and healthy fertility.

Keywords

17ß-hydroxysteroid dehydrogenase type 1; fertility; lepidiline A; maca; sex hormones.

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