Detail of "2030-63-9"

Reference

Clofazimine binding studies with deoxyribonucleic acid

Clofazimine binding studies with deoxyribonucleic acid. Morrison, N. E.; Marley, G. M. (Dep. Pathobiol., Sch. Hyg. Public Health, Baltimore, Md., USA). Int. J. Lepr. Other Mycobact. Dis., 44(4), 475-81 (English) 1976. CODEN: IJLEAG. ISSN: 0020-7349. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 6 The antileprosy drug, clofazimine (I) [2030-63-9] formed stable complexes with DNA and transfer RNA. A red shift obsd. in the absorption spectrum of I on addn. of DNA appeared specific for I binding to nucleic acid polymers. The degree of I interaction with DNA was related to the G + C content of the DNA strand. Compared with the human strand, I interacted with the mycobacterial strand to give a larger red shift, consistent with the increased G + C content of mycobacterial DNA. I interacted with the synthetic single-std. polynucleotide, poly G [25191-14-4], whereas little interaction occurred with poly A [24937-83-5], poly C [30811-80-4], or poly U [27416-86-0]. Thus, the guanine base region was a predominant site of binding to DNA. There was no evidence that I underwent intercalative binding between the base pairs of DNA. I may undergo binding along the minor groove region of DNA at appropriate base sequences which contain guanine. The resultant effect would inhibit template function of the DNA strand.

Oxygen metabolism in phagocytes of leprotic patients: enhanced endogenous superoxide dismutase activity and hydroxyl radical generation by clofazimine

Oxygen metabolism in phagocytes of leprotic patients: enhanced endogenous superoxide dismutase activity and hydroxyl radical generation by clofazimine. Niwa, Yukie; Sakane, Tsuyoshi; Miyachi, Yoshiki; Ozaki, Motoaki (3rd Dep. Intern. Med., Shimane Med. Univ., Shimane 693, Japan). J. Clin. Microbiol., 20(5), 837-42 (English) 1984. CODEN: JCMIDW. ISSN: 0095-1137. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 14 The generation of the active O metabolites superoxide (O2-), H2O2, and hydroxyl radical (OH×) and the superoxide dismutase (SOD) [9054-89-1] activity of polymorphonuclear leukocytes (PMNs) and monocytes were examd. in 14 leprotic patients manifesting a bacillary index above 2.2. Patients with disease of more than 4 yr in duration showed significantly enhanced SOD activity and a decrease in O2- and OH × prodn. The antileprotic agent, clofazimine [2030-63-9], significantly increased the generation of OH × in a dose-dependent manner, with a subsequent decrease in H2O2, but had no effect on the SOD activity of the PMNs and monocytes. In medium contg. FeSO4 or Fe2+-EDTA, the drug elevated OH × prodn. markedly further. Phagocytic SOD in PMNs and monocytes of leprotic patients was both host and bacillus derived, because the presence of cyanide, to which human-derived SOD is susceptible, did not completely abrogate SOD activity. The difficulty in treating leprosy may be partly ascribable to decreased phagocytic OH × generation, which in leprosy patients is apparently due to the uptake of Hansen bacillus-derived SOD. Clofazimine may be effective in leprosy by chelating Fe2+, with the resultant potentiation of the catalyzing activity of Fe2+ in the Haber-Weiss reaction increasing OH × formation from H2O2.