1. Development of a concise and diversity-oriented approach for the synthesis of plecomacrolides via the diene-ene RCM
Kui Lu, Mengwei Huang, Jiahua Chen, Zheng Xiang, Yongxiang Liu, Zhen Yang Org Lett . 2006 Mar 16;8(6):1193-6. doi: 10.1021/ol060221v.
[reaction: see text] A concise synthesis of the core structures of plecomacrolide with ring sizes varying from 16 to 19 atoms was achieved for the first time by the diene-ene ring-closing olefin metathesis reaction. This approach should allow access to the structurally diverse analogues of plecomacrolide.
2. PC-766B, a new macrolide antibiotic produced by Nocardia brasiliensis. II. Isolation, physico-chemical properties and structure elucidation
S Nabeshima, A Fukui, S Tanaka, K Moriguchi, M Ikemoto, K Kumagai J Antibiot (Tokyo) . 1993 Jul;46(7):1139-44. doi: 10.7164/antibiotics.46.1139.
A new macrolide antibiotic, PC-766B, was isolated from the cells of Nocardia brasiliensis SC-4710 by acetone extraction, and purified by gel filtration, silica gel chromatography, HPLC and TLC. The structure of PC-766B was determined by NMR spectral analysis to be a new class of the hygrolidin family antibiotics. PC-766B had a 16-membered macrocyclic lactone ring, a 6-membered hemiketal ring and a 2-deoxy-D-rhamnose moiety. DL-alpha-Tocopherol, known as an antioxidant agent, significantly improved the stability of PC-766B and prevented the decomposition of PC-766B during the storage of the antibiotic.
3. Screening for microbial potentiators of neutral lipid degradation in CHO-K1 cells
Elyza Aiman Azizah Nur, Keisuke Kobayashi, Satoshi Ohte, Hiroshi Tomoda, Taichi Ohshiro Drug Discov Ther . 2022 Dec 1. doi: 10.5582/ddt.2022.01087.
A cell-based assay was conducted to screen microbial culture broths for potentiators of neutral lipid degradation in Chinese Hamster Ovary K1 cells. A total of 5,363 microbial cultures from fungi and actinomycetes were screened in this assay. Brefeldin A (1) from fungal cultures was found to promote the degradation of triacylglycerol (TG) with an EC50of 2.6 µM. Beauveriolides I (2), III (3), beauverolides A (4), B (5), and K (6) from fungal cultures showed potentiating effect on cholesteryl ester (CE) degradation with EC50s ranging from 0.02 to 0.13 µM. Among these compounds, 2 and 6 exhibited the strongest activities (EC50, 0.02 µM). From actinomycete cultures, oxohygrolidin (7) (EC50for TG and CE, > 1.7 and 0.8 µM, respectively) and hygrolidin (8) (EC50for TG and CE, 0.08 and 0.004 µM, respectively) promoted degradation of CE more preferably than TG.