In vitro antibacterial activity and physicochemical properties of a crude methanol extract of the larvae of the blow fly Lucilia cuprina.

The emergence of multidrug-resistant bacterial strains has prompted the reintroduction of maggot therapy in the treatment of chronic, infected wounds. Many previous studies have demonstrated the potent antibacterial activity of larval excretions/secretions of the blowfly Lucilia sericata (Meigen) (Diptera:Calliphoridae) against bacteria. However, the antibacterial activity of its sibling species, Lucilia cuprina (Wiedemann) (Diptera:Calliphoridae) against a wide range of pathogenic bacteria has never been determined. The aim of this study was to develop a new procedure to produce whole body extract of larvae of L. cuprina via methanol extraction as well as to demonstrate the in vitro antibacterial activity of this extract against seven selected wound pathogens (Staphylococcus aureus, methicillin-resistant S. aureus, S. epidermidis, Streptococcus pyogenes, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli). The turbidimetric assay demonstrated that L. cuprina larval extract was significantly potent against all bacteria tested (P < 0.001). Additionally, colony-forming unit (CFU), agar well diffusion and minimum inhibitory concentration assays have confirmed the apparent potency of larval extract against P. aeruginosa. The reconstituted larval extract was highly robust and thermally stable. These observations substantiated the feasibility of the methanol extraction method in the production of larval extract.

The ethanol extract of Cirsium japonicum increased chloride ion influx through stimulating GABA(A) receptor in human neuroblastoma cells and exhibited anxiolytic-like effects in mice.

The aim of the present study was to evaluate the anxiolytic effects of the ethanol extract of Cirsium japonicum (CJ) in mice. The extract was orally administered at dosages of 50, 100, 200, or 400 mg/kg of body weight. The CJ-induced behavioral changes were assessed using the open-field and elevated-plus maze test. The ethanol extract of CJ did not affect overall locomotor activity of mice in the open-field test, however, it showed increase exploration in the unprotected center zone, which is thought to reflect anxiolyticlike effects. Furthermore, the CJ extract (100 and 200 mg/kg) significantly increased the percentage of time spent in the open arms of the elevated plus-maze, indicating the anxiolytic effects of the substance. This anxiolytic effects of the extract were comparable to that of the benzodiazepine, diazepam. To further characterize the anxiolytic activities of CJ, its action on human neuroblastoma cells were assessed. The CJ extract dose-dependently increased chloride ion (Cl(‒)) influx, which was blocked by coadministration of the GABA(A) receptor competitive antagonist, bicuculline, suggesting a GABA(A) receptor - Cl(‒)) channel mechanism of action. Taken altogether, the present study demonstrates that the ethanol extract of CJ has anxiolytic effects, probably mediated through GABAergic neurotransmission.

National-wide data on the treatment of BPH in Korea.

The healthcare system in Korea provides coverage to all the people who are residing in Korea, so the data of the Korea healthcare system are national-wide and relatively accurate. We obtained the recent 5-year data (2004-2008) on the treatment of BPH from the national health insurance system. We tried to determine the trends or changes of BPH treatments in Korea. Over 3.8 million men visited clinics and were prescribed one or more BPH medications, and more than 44 000 men underwent surgical treatment during 2004-2008. Compared with the year 2004, two times the patients were prescribed BPH medications in 2008. With respect to the surgical treatment, the number of cases was increased 1.6 times in 2006 compared with the previous years. The most commonly used surgical option was TURP before 2006, but laser therapy was carried out as much as TURP in 2006 and in the following years. The relative risk of laser therapy in the 50 s is 1.53 (95% CI is 1.47-1.59). In conclusion, our national-wide data for the Korean BPH patients show that these patients' medical treatment increased during the 5 years from 2004 to 2008. Laser treatment had increased and it might replace TURP in several years.

Inophyllin A, a new pyranoxanthone from Calophyllum inophyllum (Guttiferae).

In the authors' continuing search for new natural products, their recent studies on the roots of Calophyllum inophyllum (Guttiferae) have yielded a new prenylated pyranoxanthone, Inophyllin A together with the common triterpenes friedelin and stigmasterol. Structural elucidations of these compounds were achieved through (1)H, (13)C, DEPT, COSY, HSQC and HMBC experiments. The molecular mass was determined using MS techniques. The authors report here the isolation of and structural elucidation for Inophyllin A as well as its toxicity test result. The discovery of this new natural product from the unexploited Malaysian forest will certainly contribute to the search for potential natural larvicides.

Cytotoxic activities of chemical constituents from Mesua daphnifolia.

Detail chemical investigations on the stem bark of Mesua daphnifolia gave three triterpenoids and four xanthones. They are friedelin (1), friedelan-1,3-dione (2), lup-20(29)- en-3ss-ol (3), cudraxanthone G (4), ananixanthone (5), 1,3,5-trihydroxy-4-methoxyxanthone (6) and euxanthone (7). These chemical constituents were tested in vitro for their cytotoxic activities against four cell lines, MDA-MB-231 (human estrogen receptor negative breast cancer), HeLa (cervical carcinoma), CEM-SS (T-lymphoblastic leukemia) and CaOV3 (human ovarian cancer). Compound 4 showed a broad spectrum of activity against the MDA-MB-231, HeLa and CEM-SS cell lines with IC5 0 values of 1.3, 4.0 and 6.7 microg/ml respectively. Meanwhile, the other compounds 1, 2, 3, 5, 6 and 7 gave only selective activities against the cell lines.

Hyperthermic pretreatment decreases microvascular protein leakage and attenuates hypotension in anaphylactic shock in rats.

Systemic anaphylaxis is a life-threatening allergic reaction and its pathologic conditions, such as edema, bronchospasm, and hypotension, have been attributed to release of vasoactive mediators. Heat shock protein (HSP) is known to play a protective role in living cells under various stresses. In these studies, we investigated the protective role of heat shock response in anaphylactic shock, focusing on changes of blood pressure (BP) and vascular permeability. Adult sensitized rats were injected intravenously with Evans blue (EB) and challenged with bovine serum albumin (BSA). The rats were treated with whole-body hyperthermia at 41.5 +/- 0.5 degrees for 15 min 24 h before BSA challenge. Vascular protein leakage in tissues was analyzed with the EB technique. The results showed that BSA challenge induced EB extravasation in all sensitized rats. EB values (EB/tissue; microg/g) in heart and lung (112.3 +/- 41 and 244.4 +/- 90.6; mean +/- SD; n = 6) in the nonheated rats were significantly higher than those (33.4 +/- 23.3 and 103.4 +/- 63.9; n = 9) in the heated rats (P < 0.05). The results showed that BSA challenge caused BP to fall drastically in the sensitized rats. BP in the heated rats was significantly higher than BP in the nonheated rats from 4 to 15 min during anaphylactic shock (P < 0.001). Inducible HSP72 appeared overexpressed in heart, lung, and liver tissue in the heated rats tested by Western immunoblotting. The results indicate that reduction of increased protein leakage and attenuation of hypotension may result from induction of HSP by whole-body hyperthermia.

Synthesis of 6-(methoxycarbonyl)prednisolone and its derivatives as new antiinflammatory steroidal antedrugs.

The synthesis and pharmacological evaluation of 6-(methoxycarbonyl)prednisolone (11) (a 3:1 mixture of 6 alpha-isomer 11a and 6 beta-isomer 11b), its 21-ol acetates 13a (6 alpha-isomer) and 13b (6 beta-isomer), and 17,21-diol acetonide 14 (a 6:1 mixture of 6 alpha-isomer 14a and 6 beta-isomer 14b) as local antiinflammatory steroidal antedrugs are described. The lead compound 11 was prepared via 12 steps from hydrocortisone (1). In the croton oil-induced ear edema assay, the topical antiinflammatory activity of 13a was higher than that of its epimer 13b. Except for 13a, the compounds (11, 13b, and 14) showed less activity than prednisolone. The systemic activities were assessed after 5 days of consecutive administration of these compounds at equiactive doses. Neither 11 nor 14 depressed plasma corticosteroid levels or significantly altered adrenal weights. Thymic involution was absent for 14, 15% for 11, and 47% for prednisolone at the equiactive doses. Both 13a and 13b showed significant reduction of adverse systemic effects assessed as the increase of body weight and the decreases of adrenal and thymus weights. The putative metabolite, carboxylic acid 12, showed 26 times less topical antiinflammatory activity than prednisolone. These results suggest that introduction of a labile methoxycarbonyl group at the C-6 position of prednisolone results in retention of antiinflammatory activity while reducing systemic effects noted following topical application of the parent compound prednisolone.