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Bioactive polycyclic polyprenylated acylphloroglucinols from Hypericum scabrum.

Zhong-Bo Zhou1, Peng-Yun Mou2, You-Yi Huang3

  • 1Research Center for the Prevention and Treatment of Drug Resistant Microbial Infecting, Youjiang Medical University for Nationalities, Baise 533000, PR China; School of Pharmacy, Youjiang Medical University for Nationalities, 98 Chengxiang Road, Baise 533000, PR China.

Fitoterapia
|July 7, 2022
PubMed
Summary

Six new polycyclic polyprenylated acylphloroglucinols from Hypericum scabrum Linn. showed moderate cytotoxic activities against cancer cell lines and weak antimicrobial properties against Bacillus subtilis and MRSA.

Keywords:
Antimicrobial activityCytotoxicityHypericum scabrumPolycyclic polyprenylated phloroglucinols

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Area of Science:

  • Natural Products Chemistry
  • Medicinal Chemistry
  • Pharmacognosy

Background:

  • Hypericum scabrum Linn. is a plant species known for its diverse chemical constituents.
  • Polycyclic polyprenylated acylphloroglucinols (PPAPs) are a class of natural products with reported biological activities.

Purpose of the Study:

  • To isolate and characterize new PPAPs from Hypericum scabrum Linn.
  • To evaluate the cytotoxic and antimicrobial activities of the isolated compounds.

Main Methods:

  • Isolation of compounds using chromatographic techniques.
  • Structure elucidation through comprehensive spectroscopic analyses (NMR, MS).
  • Cytotoxicity assays against SMMC-7721 and MGC-803 cell lines.
  • Antimicrobial activity testing against Bacillus subtilis, Methicillin-resistant Staphylococcus aureus (MRSA), and Methicillin-dependent Pseudomona aeruginosa (MDPRA).

Main Results:

  • Eighteen PPAPs were isolated, including six novel compounds (1-6).
  • Most compounds displayed moderate cytotoxic effects against SMMC-7721 cells, with exceptions for compounds 11 and 12.
  • Compounds 1, 5-7, 13, and 16 exhibited cytotoxic activity against MGC-803 cells.
  • Compounds 12 and 13 showed weak inhibitory activity against Bacillus subtilis.
  • Compounds 7, 13, and 14 demonstrated weak inhibitory activity against MRSA.

Conclusions:

  • The study successfully identified new PPAPs from Hypericum scabrum Linn.
  • The isolated compounds possess varying degrees of cytotoxic and antimicrobial activities.
  • Further investigation into the structure-activity relationships of these PPAPs is warranted.