Various microorganisms were screened for their ability to decolorize molasses wastewater under thermophilic and anaerobic conditions. Strain MD-32, which was newly isolated from a soil sample, was selected as the best strain. From taxonomical studies, the strain was concluded to belong to the genus Bacillus, most closely resembling B. smithii. The strain decolorized 35.5% of molasses pigment within 20 d at 55 degrees C under anaerobic conditions, but no decolorization activity was observed when it was cultivated aerobically. At all the concentrations tested molasses pigment was effectively decolorized by MD-32, with decolorization yields of around 15% within 2 d. The molecular weight distribution as determined by gel filtration chromatography revealed that the decolorization of molasses pigment by the isolated strain is accompanied by a decrease in not only small molecules but also large ones.

01 Nov 1997·Arzneimittel-Forschung

Effects of 1-(3-bromobenzofuran-2-ylsulfonyl)hydantoin on human aldose reductase examined by a new application of HPLC system for measuring tissue polyol.

Article

Author: Nakayama, K ; Miwa, I ; Kato, K ; Mizota, M ; Murakami, N ; Ohta, M ; Okuda, J

M16209 (1-(3-bromobenzofuran-2-ylsulfonyl)hydantoin, CAS 128851-36-5) displayed potent inhibitory effects upon recombinant human aldose reductase (rhAR, IC50 = 0.051 mumol/l). The inhibition of rhAR by M16209 was uncompetitive with respect to both glyceraldehyde and NADPH. The effects of M16209 on human AR were investigated using a new application of HPLC system developed for analysis of tissue polyol. M16209 and epalrestat suppressed galactitol accumulation in human erythrocytes cultured in 25 mmol/l galactose with IC50 values of 1.2 and 2.6 mumol/l, respectively. The new application of HPLC system equipped with an electrochemical detector did not require any derivatization procedure for polyols and enabled simultaneous determination of glucose, galactose, fructose, myo-inositol, galactitol and sorbitol.

01 Apr 1997·Life SciencesQ3 · MEDICINE

Antihyperglycemic mechanism of M16209, an antidiabetic agent, in 3T3-L1 adipocytes

Q3 · MEDICINE

Article

Author: Hideshi Kuzuya ; Tatsuya Hayashi ; Katsuaki Kato ; Nobuya Murakami ; Kazuwa Nakao ; Gen Inoue ; Shigeo Kohno ; Yasunao Yoshimasa ; Motozumi Okamoto

We investigated the effect of M16209 (1-(3-bromobenzo[b]furan-2-ylsulfonyl)hydantoin) on glucose transport and the insulin signaling system in mouse-derived 3T3-L1 adipocytes. When M16209 (30 and 100 microM) was added to 3T3-L1 adipocytes and preincubated for 24 hours, the uptake of 2-deoxy-D-[3H]-glucose (2-DG) after insulin stimulation was enhanced. This effect was seen when preincubation with M16209 was performed in the presence of 6 and 20 ng/ml insulin, but M16209 did not increase the response to 600 ng/ml insulin. M16209 (100 microM) did not interfere with (125)I-insulin binding or with tyrosine phosphorylation of the insulin receptor beta-subunit and IRS-1. M16209 (100 microM) also had no effect on the level of glucose transporter (GLUT1 and GLUT4) protein, but it promoted the translocation of intracellular GLUT4 to the plasma membrane. In contrast, M16209 had no effect on the translocation of GLUT1. In summary, M16209 enhanced 2-DG uptake by 3T3-L1 adipocytes. Insulin binding to its receptor, autophosphorylation of the insulin receptor beta-subunit, and tyrosine phosphorylation of IRS-1 were unaffected by M16209. However, translocation of GLUT4 from the intracellular pool to the plasma membrane was facilitated.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus	Phase 2	JP	Mochida Pharmaceutical Co., Ltd.	-

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