The in vitro and in vivo activities of a new benzoxazinorifamycin, KRM-1648 (KRM), against Mycobacterium tuberculosis were studied. The MIC at which 50% of the isolates are inhibited (MIC 50 ) and the MIC 90 of KRM for 30 fresh isolates of M. tuberculosis measured by the BACTEC 460 TB System were 0.016 and 2 g/ml, respectively. These values were much lower than those for rifampin (RMP), which were 4 and >128 g/ml, respectively, and considerably lower than those for rifabutin (RBT), which were 0.125 and 8 g/ml, respectively. A correlational analysis of the MICs of these drugs for the clinical isolates revealed the presence of crossresistance of the organisms to KRM and either RMP or RBT although the MICs of KRM were distributed over a much lower range than were those of the other two drugs. KRM and RMP at concentrations of 1 to 10 g/ml almost completely inhibited the bacterial growth of RMP-sensitive strains (H 37 Rv, Kurono, and Fujii) of M. tuberculosis phagocytosed in macrophage-derived J774.1 cells. KRM was more active than RMP in inhibiting the growth of the RMP-resistant (MIC ‫؍‬ 8 g/ml) Kurata strain but failed to show such an effect against the RMP-resistant (MIC >128 g/ml) Watanabe strain. When KRM was given to M. tuberculosis-infected mice at dosages of 5 to 20 mg/kg of body weight by gavage, once daily six times per week from day 1 after infection, it was much more efficacious than RMP against infections induced in mice by the RMP-sensitive Kurono strain, as measured by a reduction of rates of mortality, a reduction of the frequency and extent of gross lung lesions, histopathological changes in lung tissues, and a decrease in the bacterial loads in the lungs and spleens of infected mice. KRM also displayed significant therapeutic efficacy against infection induced by the RMPresistant Kurata strain, while neither KRM nor RMP was efficacious against infection by the RMP-resistant Watanabe strain. In the case of infection with the Kurono strain, the efficacy of the drugs in prolonging the time of survival was in the order KRM, RBT, RMP. KRM was much more efficacious than RMP, when given at 1-to 4-week intervals. These findings suggest that KRM may be useful for the clinical treatment of tuberculosis contracted through RMP-sensitive strains, even when it is administered at long intervals.

SCM low‐sulfur proteins of scalp hairs from Mongoloid, Negroid and Caucasoid individuals were analyzed by two‐dimensional electrophoresis. The electrophoregrams obtained showed no differences among the three races; the low‐sulfur protein composition of the hair did not differ electrophoretically among the three races. This suggested that the low‐sulfur proteins may not be responsible for the macroscopic racial variations in the form of hair.

Fibrous proteins (FPs) and matrix substances (MSs) were extracted as S-carboxymethylated (SCM) derivatives from scalp hair of five individuals each of the Mongoloid, Negroid and Caucasoid races. The ratio of the extracted SCM FPs to SCM MSs in dry weight was calculated for each hair specimen. The ratios obtained from the Mongoloid hair were 0.45 +/- 0.03; those from the Negroid, 0.18 +/- 0.02; and those from the Caucasoid, 0.29 +/- 0.02. It has thus been suggested that the ratios of FP to MS contents in the hair may be involved in the determination of the macroscopic racial variations in the form of hair.

A 71-year-old Japanese woman developed red-brown to yellow papules symmetrically on the eyelids and cheeks. The histopathology of a papule showed caseation necrosis surrounded by epitheloid cells intermingled with giant cells in the dermis. The patient was thus diagnosed as lupus miliaris disseminatus faciei (LMDF). To the best of our knowledge, no LMDF patients of such an age have been described previously.

A 5-year-old Japanese girl developed follicular pustules with erythematous plaques on the lower extremities. The histopathology was compatible with eosinophilic pustular folliculitis (EPF). However, the clinical findings were not typical of EPF; the pustules did not appear in crops, the pustules became ulcers, and the skin lesions appeared exclusively on non-seborrheic areas.