著者
寺田 忠史 藤本 勝彦 野村 誠 山下 純一 / 小武内 尚 武田 節夫 南 慶典 吉田 健一郎 山口 秀夫 山田 雄次 Yuji YAMADA
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.41, no.5, pp.907-912, 1993-05-15 (Released:2008-03-31)
参考文献数
58
被引用文献数
6 10

1-β-Alkyl derivatives of 1-desoxypodophyllotoxin were synthesized, and their cytotoxicity and inhibitory effects on DNA topoisomerase II (Topo-II) and tubulin polymerization were examined.The reaction of epipodophyllotoxin derivatives (1a-c) with trimethylallylsilane in the presence of boron trifluoride etherate gave 1-β-allylated compounds (2a-c). The regiochemistry and the β-stereochemistry of the 1-allyl group were confirmed by comparison of the 13C-NMR spectra and NOE's (%) of 2c, podophyllotoxin (POD) and epipodophyllotoxin (1b). 1-β-Alkyl-1-desoxypodophyllotoxin derivatives (3-8) were prepared from 2b.None of the tested compounds (3-8) showed any inhibitory effect on Topo-II. 1-β-Propyl compound (3) and its 4'-demethyl compound (4) inhibited tubulin polymerization and the cytotoxicities of these compounds were equal to that of VP-16. 1-β-(2, 3-Dihydroxypropyl) compounds (5 and 8) and 1-β-(2, 3-diacetoxypropyl) compounds (6 and 7)showed no inhibitory effect on tubulin polymerization. Although 5 did not inhibit either Topo-II activity or tubulin polymerization, it showed a high cytotoxicity against sarcoma 180.
著者
JILAN HU YU-CHUAN XUE MEI-YU XIE RUI ZHANG TOSHIO OTANI YOSHINORI MINAMI YUJI YAMADA TERUYOSHI MARUNAKA
出版者
JAPAN ANTIBIOTICS RESEARCH ASSOCIATION
雑誌
The Journal of Antibiotics (ISSN:00218820)
巻号頁・発行日
vol.41, no.11, pp.1575-1579, 1988-11-25 (Released:2006-04-19)
参考文献数
14
被引用文献数
77 102

Strain C-1027, an actinomycete isolated from a soil sample collected in China, was found to produce the new antibiotic, C-1027. From taxonomical studies on its morphological, cultural and physiological characteristics, this antibiotic-producing strain was identified as Streptomyces ghbisporus C-1027. Antibiotic C-1027 has antimicrobial activity against most Gram-positive bacteria but not against Mycobacterium sp. or Gram-negative bacteria. This antibiotic shows remarkable activity in spermatogonial assay and potent cytotoxicity against KB carcinoma cells in vitro, and exhibits inhibition on transplantable tumors in mice.
著者
Yuji Yamada Yoshitaka Miyakawa Mitsuaki Sawano Yutaka Okano
出版者
一般社団法人 日本内科学会
雑誌
Internal Medicine (ISSN:09182918)
巻号頁・発行日
vol.53, no.10, pp.1083-1085, 2014 (Released:2014-05-15)
参考文献数
15
被引用文献数
2 10

Acquired coagulation factor deficiency is a rare disorder that occurs in patients with drug reactions, malignancy and collagen diseases as well as during pregnancy. Most cases are caused by factor VIII inhibitors. We herein describe the case of a 61-year-old Japanese man with acquired factor V inhibitor who developed symptoms 11 days after lung surgery for empyema. The patient required mechanical ventilation to treat acute respiratory failure due to severe pulmonary hemorrhage. He responded poorly to steroid pulse therapy; however, treatment with rituximab was successful.