Kirk Riley D, Rosario Margaret E, Oblie Nana, Jouaneh Terra Marie M, Carro Marina A, Wu Christine, Kim Andrew M, Leibovitz Elizabeth, Hunter Elizabeth Sage, Literman Robert, Handy Sara M, Rowley David C, Bertin Matthew J
Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, Rhode Island 02881, United States.
Center for Food Safety and Applied Nutrition, Office of Regulatory Science, United States Food and Drug Administration, College Park, Maryland 20740, United States.
ACS Omega. 2022 Sep 30;7(40):35677-35685. doi: 10.1021/acsomega.2c03539. eCollection 2022 Oct 11.
Infections caused by the bacterium continue to pose threats to human health and put a financial burden on the healthcare system. The overuse of antibiotics has contributed to mutations leading to the emergence of methicillin-resistant , and there is a critical need for the discovery and development of new antibiotics to evade drug-resistant bacteria. Medicinal plants have shown promise as sources of new small-molecule therapeutics with potential uses against pathogenic infections. The principal Rhode Island secondary metabolite (PRISM) library is a botanical extract library generated from specimens in the URI Youngken Medicinal Garden by upper-division undergraduate students. PRISM extracts were screened for activity against strains of methicillin-susceptible (MSSA). An extract generated from the tulip tree () demonstrated growth inhibition against MSSA, and a bioassay-guided approach identified a sesquiterpene lactone, laurenobiolide, as the active constituent. Intriguingly, its isomers, tulipinolide and -tulipinolide, lacked potent activity against MSSA. Laurenobiolide also proved to be more potent against MSSA than the structurally similar sesquiterpene lactones, costunolide and dehydrocostus lactone. Laurenobiolide was the most abundant in the twig bark of the tulip tree, supporting the twig bark's historical and cultural usage in poultices and teas.
由这种细菌引起的感染继续对人类健康构成威胁，并给医疗系统带来经济负担。抗生素的过度使用导致了导致耐甲氧西林 出现的突变，因此迫切需要发现和开发新的抗生素以对抗耐药细菌。药用植物已显示出有望成为具有对抗病原体感染潜在用途的新型小分子疗法的来源。罗德岛主要次生代谢产物（PRISM）文库是由高年级本科生从罗德岛大学扬肯药用植物园的标本中生成的植物提取物文库。对PRISM提取物进行了针对甲氧西林敏感 （MSSA） 菌株的活性筛选。从鹅掌楸（）中提取的一种提取物对MSSA表现出生长抑制作用，一种生物测定导向的方法确定了一种倍半萜内酯，劳伦诺内酯，为活性成分。有趣的是，它的异构体，郁金香内酯和 - 郁金香内酯，对MSSA缺乏强效活性。劳伦诺内酯对MSSA的效力也比结构相似的倍半萜内酯、木香烯内酯和脱氢木香内酯更强。劳伦诺内酯在鹅掌楸的嫩枝树皮中含量最高，这支持了嫩枝树皮在膏药和茶中的历史和文化用途。
