Antimicrobial and Cytotoxic Activities of Neolignans from Magnolia officinalis

Wiley - Tập 1 Số 3 - Trang 530-537 - 2004
Wan‐Jr Syu1, Chien‐Chang Shen2,3, Jang‐Jih Lu4, Gum‐Hee Lee1, Changming Sun2,3
1Institute of Microbiology and Immunology, National Yang-Ming University, Taipei, Taiwan 112, Republic of China
2Division of Natural Drugs, National Research Institute of Chinese Medicine, No. 155-1, Sec 2, Li-Nong St, Shih-Pai, Taipei, Taiwan 112, Republic of China, (Phone: +886 2 28201999 ext. 6641
3fax: +886 2 28264276)
4Department of Pathology, Tri-Service General Hospital, Taipei, Taiwan 114, Republic of China

Tóm tắt

AbstractIn the light of the steady increase of infections related to vancomycin‐resistant enterococci (VRE) and methicillin‐resistant Staphylococcus aureus (MRSA), the medicinal plant Magnolia officinalis was subjected to bioassay‐directed fractionation, which led to the isolation of the known neolignans piperitylmagnolol (1), magnolol (2), and honokiol (3) from the MeOH extract. In broth‐microdilution assays, 1–3 exhibited antibacterial activities against VRE and MRSA at minimum‐inhibitory concentrations (MIC) in the range of 6.25–25 μg/ml, compound 1 being the most‐potent antibiotic. The ratio of MBC/MIC (MBC=minimum bactericidal concentration) was ≤2 for all compounds. The kinetics of the antibacterial action of 1 and 3 were studied by means of time‐kill assays; both compounds were bactericidal against VRE and MRSA, their actions being time dependent, or both time and concentration dependent. Magnolol (2) was acetylated to magnolol monoacetate (4) and magnolol diacetate (5) (partial or full masking of the phenolic OH functions). The cytotoxic properties of 1–5 against human OVCAR‐3 (ovarian adenocarcinoma), HepG2 (hepatocellular carcinoma), and HeLa (cervical epitheloid carcinoma) cell lines were evaluated. The CD50 values for compounds 1–3 were in the range of 3.3–13.3 μg/ml, derivatives 4 and 5 being much less potent. This study indicates that piperitylmagnolol (=3‐[(1S,6S)‐6‐isopropyl‐3‐methylcyclohex‐2‐enyl]‐5,5′‐di(prop‐2‐enyl)[1,1′‐biphenyl]‐2,2′‐diol; 1) possesses both significant anti‐VRE activity and moderate cytotoxicity against the above cancer cell lines.

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Wiley

Tập 1 Số 3

530-537

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