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Objectives: To investigate the efficacy of tadalafil for patients with benign prostatic hyperplasia and especially with chronic prostatitis/chronic pelvic pain syndrome.Methods: Tadalafil 5 mg was given each morning for 12 weeks to patients diagnosed as having either moderate or severe lower urinary tract symptoms. Voiding symptoms were compared between patients with a high (>4; high group) and low (<4; low group) pain subscore of the National Institutes of Health Chronic Prostatitis Symptom Index before and after tadalafil administration. Correlation between changes in the Chronic Prostatitis Symptom Index and the International Prostate Symptom Score during treatment was also investigated.Results: At the pretreatment baseline, the pain subscore of the Chronic Prostatitis Symptom Index was high (>4) in 24 of 74 (32.4%) patients. The International Prostate Symptom Score in the group with high pain subscore was significantly higher than that in the group with low pain subscore. As an indicator of the efficacy of tadalafil, the International Prostate Symptom Score and National Institutes of Health Chronic Prostatitis Symptom Index total score and pain subscore were significantly improved.The change in the Chronic Prostatitis Symptom Index total score correlated positively with the change in the International Prostate Symptom Score. The decrease in the 4 International Prostate Symptom Score was significantly greater in the group with high versus low pain subscore. Conclusion:Tadalafil was sufficiently effective in the treatment of patients with benign prostatic hyperplasia and severe chronic prostatitis/chronic pelvic pain syndrome.

The recently emerged concept of "vessel normalization" implies that judicious blockade of vascular endothelial growth factor (VEGF) signaling may transiently "normalize" the tumor vasculature, making it more suitable for tumor disposition of subsequently administered drugs. In this study, therefore, the effect of pretreatment with SU5416, a selective VEGF receptor-2 inhibitor, on tumor disposition and in vivo antitumor activity of polyethylene glycol (PEG)-modified liposomal paclitaxel (PL-PTX) was evaluated in Colon-26 solid tumor-bearing mice. To improve the solubility and in vivo disposition characteristics of SU5416, the inhibitor was formulated in PEGylated O/W emulsion (PE-SU5416). Pretreatment with PE-SU5416 significantly enhanced the in vivo antitumor effect of PL-PTX, although PE-SU5416 administration alone did not show any antitumor effect. Immunostaining for endothelial cells and pericytes demonstrated that the pretreatment with PE-SU5416 enhanced the pericyte coverage of the tumor vasculature. In addition, tumors treated with PE-SU5416 contained significantly smaller hypoxic regions compared with the nontreated control group, demonstrating that structural normalization of the tumor vasculature resulted in an improvement in tumor vessel functions, including oxygen supply. Furthermore, the pretreatment with PE-SU5416 increased the distribution of PEG liposomes and included PTX in the core region of the tumor, as well as conversely decreasing the ratio of their peripheral distribution. These results suggest that the structural and functional normalization of the tumor vasculature by the pretreatment with PE-SU5416 enabled liposomes to reach the deeper regions within tumor tissues, leading to more potent antitumor activity of PL-PTX.

The photodegradation of benthiocarb (S-4-chlorobenzyl N, N-diethythiocarbamate) under ultraviolet lights or sunlight was investigated using 14C-labelled and unlabelled compounds.Benthiocarb in the aqueous solution was more rapidly degraded by irradiation with ultraviolet lights than seven common pesticides tested. The irradiation resulted in the formation of many degradation products such as benthiocarb sulfoxide, desethyl benthiocarb, 4-chlorobenzyl alcohol, 4-chlorobenzaldehyde, 4-chlorobenzoic acid, 4-hydroxy analogues of the alcohol, the aldehyde and the acid, 8 other identified compounds and about 20 unidentified compounds. Among these, 4-chlorobenzaldehyde and the alcohol were the major products. The degradation in the aqueous solution under sunlight was also considerably rapid, and most of the degradation products detected were the same as those produced by irradiation with ultraviolet lights. The irradiation on the thin film of benthiocarb on glass plate also resulted in the formation of the same degradation products as those in the aqueous solution.