Macrolide antibiotics (PC-766B, bafilomycin, concanamycin) were potent compounds that increased LDL receptor (LDL-r) mRNA in human hepatoma HepG2 cells.There was no clear relationship between the antimicrobial activity of these compounds and their action on LDL-r mRNA.These macrolides are capable of stimulating expression of promoter of LDL-r; transcription of LDL-r gene was increased resulting in high concentration of LDL-r mRNA in HepG2 cells.

01 Jan 1993·The Journal of AntibioticsQ4 · MEDICINE

PC-766B, a new macrolide antibiotic produced by Nocardia brasiliensis. I. Taxonomy, fermentation and biological activity.

Q4 · MEDICINE

Article

Author: Shigeyasu Nabeshima ; Masaru Fukui ; Kiyoshi Taya ; Masatomo Fukasawa ; Kazuo Kumagai ; Akio Fukui

An actinomycete strain SC-4710, a new soil isolate, was found to produce a new macrolide antibiotic, PC-766B. Chemotaxonomic analysis of the producing organism revealed that the cells of SC-4710 had type IV cell wall, type A whole cell sugar pattern, type PII phospholipids, menaquinone MK-8(H4), cellular fatty acids comprising straight-chain saturated, unsaturated and tuberculostearic acids, and mycolic acids. The strain was identified as Nocardia brasiliensis (Lindenberg) Pinoy. The antibiotic, PC-766B, was active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. It also showed antitumor activity against murine tumor cells in vitro and in vivo, and a weak inhibitory activity against Na+, K(+)-ATPase in vitro.

01 Jan 1993·The Journal of AntibioticsQ4 · MEDICINE

PC-766B, A new macrolide antibiotic produced by Nocardia brasiliensis. II. Isolation, physico-chemical properties and structure elucidation.

Q4 · MEDICINE

Article

Author: Fukui, Akio ; Ikemoto, Masahiko ; Kumagi, Kazuo ; Tanaka, Shin ; Moriguchi, Koichi ; Nabeshima, Shigeyasu

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.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Discovery	JP	Sumitomo Pharmaceuticals Co., Ltd.	-

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