A chemical mutagenesis technique was employed for development of mutant strains of Sparassis crispa targeting the shortened cultivation time and the high beta-glucan content. The homogenized mycelial fragments of S. crispa IUM4010 strain were treated with 0.2 vol% methyl methanesulfonate, an alkylating agent, yielding 199 mutant strains. Subsequent screening in terms of growth and beta-glucan content yielded two mutant strains, B4 and S7. Both mutants exhibited a significant increase in beta-glucan productivity by producing 0.254 and 0.236 mg soluble beta-glucan/mg dry cell weight for the B4 and S7 strains, respectively, whereas the wild type strain produced 0.102 mg soluble beta-glucan/mg dry cell weight. The results demonstrate the usefulness of chemical mutagenesis for generation of mutant mushroom strains.
Agaricales ; Efficiency ; Mass Screening ; Mesylates ; Methyl Methanesulfonate ; Mutagenesis ; Sprains and Strains

No abstract available.
Dialysis* ; Heart Arrest* ; Mesylates*

No abstract available.
Dialysis* ; Heart Arrest* ; Mesylates*

The ‘equivalent-or-more-but-not-the-same-data’ provision in the Regulation on the Safety and Efficacy Evaluation of New Drug in Korea has served as the de facto data exclusivity term for any drug identical to a product subject to new drug reexamination. The legal debate that occurred between Abbott Korea and Hanmi in association with the approval of their sibutramine products, i.e., Reductil® vs. Slimmer®, showed why data exclusivity plays an important role to protect intellectual property of the innovator drug when incrementally modified drugs had to rely on the safety and efficacy data of the innovator drug for approval. The regulatory science and legal issues regarding the case of Reductil® vs Slimmer® were discussed, and the importance of data exclusivity was emphasized as a useful tool to protect intellectual property besides patent.
Intellectual Property ; Korea ; Mesylates

PURPOSE: Systemic anticoagulation, usually with heparin, is required to prevent thrombosis in the blood circuit of hemodialysis. In patients at high bleeding risk, strategies to minimize the bleeding risk include heparin-free or regional anticoagulation methods. Nafamostat mesilate with conventional dose (35 mg/hr) has been used for this purpose. But it is an expensive anticoagulant to use conveniently for the dialysis therapy. Application of low-dose nafamostat mesilate has almost never been tried yet on hemodiaysis management. In this study, we examined the effect of low-dose nafamostat mesilate compared to heparin-free in hemodialysis patients with high risk of bleeding. METHODS: The current study was conducted on 35 hemodialysis patients with high bleeding risk (on-going bleeding, hemorrhage, surgery or severe thrombocytopenia). In the low-dose nafamostat group (n=17, mean age: 59+/-15 years), 238 sessions were performed with continuous infusion of nafamostat mesilate (12.5 mg/hr). In the control group with saline-flushing no heparin methods (n=18, mean age: 57+/-17 years), 247 sessions were analyzed. RESULTS: No significant differences were found in baseline characteristics between the low-dose nafamostat group and the saline group. In the progress of bleeding complications, there were no significant differences between the two groups (11.8% vs. 11.1%). In saline group, however, massive clotting occurred in 44.5 per 1000 sessions, while it occurred in 4.2 per 1000 sessions in the low-dose nafamostat group (p=0.006). CONCLUSION: In patients at high bleeding risk, low-dose nafamostat mesilat can be used as an inexpensive, effective, and safe anticoagulant for hemodialysis.
Dialysis ; Guanidines ; Hemorrhage ; Heparin ; Humans ; Mesylates ; Renal Dialysis ; Thrombosis

No abstract available.
Benzamides ; Mesylates* ; Nails, Malformed* ; Piperazines ; Pyrimidines ; Imatinib Mesylate

No abstract available.
Benzamides ; Drug Eruptions* ; Mesylates* ; Piperazines ; Pyrimidines ; Imatinib Mesylate

BACKGROUND: Routine hemodialysis is performed with systemic anticoagulation, usually with heparin, to prevent thrombosis in the extracorporeal blood circuit. However, systemic anticoagulation can produce hemorrhagic complications in patients at high risk of bleeding. To minimize the risk of bleeding, a number of alternative regimens has been proposed, however, each of those methods has its own limitations and complication. METHODS: 58 hemodialysis patients at risk for bleeding due to previous surgery or hemorrhagic complication were treated with Futhan as regional anticoagulant and compared with that of low-dose heparin anticoagulation. There were 29 (50%) postoperative cases and 29 (50%) cases of hemorrhage from various sites. RESULTS: The exacerbation of bleeding by hemodialysis was noted in only 4% in heparin treated group and none in Futhan group. Clotting times at site A (intracorporeal circulation) were not prolonged with Futhan, whereas those of heparin were prolonged slightly, which is not statistically significant. Degrees of residual blood in the dialyzer and blood clottings in the venous drip-chamber were less in Futhan than in heparin group. Adverse reactions related to Futhan therapy were minor and the incidence of adverse reactions was comparable in both groups. CONCLUSION: Futhan is a safe and effective regional anticoagulant for hemodialysis especially for patients with high bleeding risk.
Blood Coagulation ; Hemorrhage* ; Heparin ; Humans ; Incidence ; Mesylates* ; Renal Dialysis* ; Thrombosis

OBJECTIVE: To compare the effect of micro-needle knife therapy and betahistine mesilate tablets in the treatment of cervical vertigo (CV) and the influence on the mean blood flow velocity (Vm) of vertebral artery. METHODS: A total of 200 patients with CV were randomly divided into a micro-needle knife group (100 cases, 5 cases dropped off) and a medication group (100 cases, 3 cases dropped off). In the micro-needle knife group, micro-needle knife was performed on the suboccipital triangle of the atlantoaxial segment of the posterior neck, once every other day, for a total of 7-time treatment. The medication group received oral betahistine mesilate tablets, 6 mg each time, three times a day, for 14 consecutive days. The dizziness handicap inventory (DHI) scores of the two groups were observed before treatment, after treatment and during follow-up 3 months after treatment; the Vm of vertebral artery was compared between the two groups before and after treatment, and the clinical effect was evaluated during follow-up. RESULTS: After treatment and during follow-up, the DHI scores of the two groups were lower than those before treatment (P<0.001), and those in the micro-needle knife group were lower than the medication group (P<0.001). After treatment, the Vm of bilateral vertebral arteries in both groups was higher than that before treatment (P<0.05), and that in the micro-needle knife group was higher than the medication group (P<0.05). The total effective rate of the micro-needle knife group was 96.8% (92/95), which was higher than 67.0% (65/97) of the medication group (P<0.001). CONCLUSION Micro-needle knife therapy can improve vertigo symptoms and balance dysfunction, increase the mean blood flow velocity of vertebral artery in CV patients, and its clinical efficacy is better than oral betahistine mesilate tablets.
Betahistine ; Hemodynamics ; Humans ; Mesylates ; Treatment Outcome ; Vertebral Artery ; Vertigo/therapy*

BACKGROUND: It has been well demonstrated that trypsin inhibitor can stimulate the secretion of cholecystokinin. Camostat mesylate (C20H22N4O5 CH3SO3H) is a synthetic trypsin inhibitor. We demonstrated the effect of camostat mesylate on the chemical composition of bile and the crystallization in gallbladder-stone patients. METHODS: Gallbladder bile sample from 22 patients with GB stones were analyzed. In 11 patients, camostat mesylate (Foy-pan ) was administered orally in a dosage of 600 mg per day for more than 5 days, and the results of the bile analysis were compared to those of 11 controls. RESULTS: The total protein concentration in the camostat group was lower than that in control group (0.21+/-0.10 vs 0.24+/-0.06 g/dl) but the difference was not significant (p=0.41). The total bile acid concentration in the camostat group was significantly lower than that in the control group (5.47+/-1.56 vs 6.85+/-1.32 g/dl, p=0.04). The concentrations of cholesterol and phospholipid were lower in the camostat group (0.35 +/- 0.19 vs 0.44 +/- 0.11 g/dl, 2.10 +/- 1.19 vs 2.92 +/- 0.93, respectively), but the differences were not statistically significant (p=0.20, p=0.09, respectively). The total lipid concentration which reflects the concentrated magnitude of the bile, was significantly lower in the camostat group (7.93 +/- 2.87 vs 10.20 +/- 2.01 g/dl, p=0.04). The cholesterol saturation index didn't demonstrate a significant difference between the two groups (1.06 +/- 0.27 vs 0.95 +/- 0.31, p=0.38). Crystallization in the bile from cholesterol stone patients, was observed every day for 7 days. Crystallizations was less frequent in the camostat group, but the difference was not statistically significant (1/6 vs 4/8, p=0.39). DISIDA (disofenin iminediacetate) scans were performed in 3 healthy volunteers to observe the changes in the radioactivities and the volumes of the gallbladders before and after the administrations of camostat. The peak radioactivities, the transittime to the peak radioactivity, and the gallbladder volume at the peak radioactivity in the scan after the administration of camostat were lower than in the corresponding values before the administration. CONCLUSIONS: Camostat mesylate lowers the concentration of all bile components. We assume that the effects of Camostat mesylate are mediated by CCK, which enhances gallbladder motility and limits the concentrating function of the gallbladder.
Bile* ; Cholecystokinin ; Cholesterol ; Crystallization* ; Gallbladder* ; Healthy Volunteers ; Humans ; Mesylates* ; Radioactivity ; Trypsin