2. Academic Validation
  3. Meroterpenoids with Antitumor Activities from Guava (Psidium guajava)

Meroterpenoids with Antitumor Activities from Guava (Psidium guajava)

  • J Agric Food Chem. 2017 Jun 21;65(24):4993-4999. doi: 10.1021/acs.jafc.7b01762.
Xu-Jie Qin 1 2,  Qian Yu 3,  Huan Yan 1 2,  Afsar Khan 4,  Mi-Yan Feng 1 2,  Pan-Pan Li 1 2,  Xiao-Jiang Hao 1 2,  Lin-Kun An 3,  Hai-Yang Liu 1 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences , Kunming 650201, People's Republic of China.
  • 2 Yunnan Key Laboratory of Natural Medicinal Chemistry , Kunming 650201, People's Republic of China.
  • 3 Institute of Medicinal Chemistry and Chemical Biology, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
  • 4 Department of Chemistry, COMSATS Institute of Information Technology , Abbottabad 22060, Pakistan.
PMID: 28578580 DOI: 10.1021/acs.jafc.7b01762
Abstract

Psidium guajava L., a species native to South America, has been widely cultivated in the tropical and subtropical areas of China for its popular fruits. The preliminary analysis by liquid chromatography-ultraviolet (LC-UV) indicated the presence of meroterpenoids in the fruits of P. guajava (guava). Subsequent fractionation of the petroleum ether extract resulted in the identification of two new meroterpenoids, psiguajavadials A (1) and B (2), together with 14 previously described meroterpenoids (3-16). Their structures were fully elucidated by comprehensive spectroscopic techniques and theoretical calculations. All of the meroterpenoids showed cytotoxicities against five human Cancer cell lines, with guajadial B (12) being the most effective having an IC50 value of 150 nM toward A549 cells. Furthermore, biochemical Topoisomerase I (Top1) assay revealed that psiguajavadial A (1), psiguajavadial B (2), guajadial B (12), guajadial C (14), and guajadial F (16) acted as Top1 catalytic inhibitors and delayed Top1 poison-mediated DNA damage. The flow cytometric analysis indicated that the new meroterpenoids psiguajavadials A (1) and B (2) could induce Apoptosis of HCT116 cells. These data suggest that meroterpenoids from guava fruit could be used for the development of antitumor agents.

Keywords

DNA topoisomerase I inhibitors; antiproliferative activity; cytotoxicity; guava; meroterpenoids.

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