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Human pancreatic cancer is known to be the most deadly disease with the lowest 5-year survival rate and is resistant to well known conventional chemotherapeutic drugs in clinical use. Screening of medicinal plants from Myanmar utilizing antiausterity strategy led to the identification of Vitex negundo as one of the medicinal plants having potent preferential cytotoxic activity against PANC-1 human pancreatic cancer cells. Bioactivity-guided phytochemical investigation led to the isolation of chrysoplenetin (1) and chrysosplenol D (2) as the active constituents with a PC50 value of 3.4 μg/mL and 4.6 μg/mL, respectively, against PANC-1 cells. Both these compounds induced apoptosis-like morphological changes in PANC-1 cells. Chrysoplenetin was further tested against a panel of 39 human cancer cell lines (JFCR-39) at the Japanese Foundation for Cancer Research, and 25 cell lines belonging to lung, breast, CNS, colon, melanoma, ovarian, prostate cancer and stomach cancer cell lines were found to be highly sensitive to chrysoplenetin at a submicromolar range. In the JFCR-39 panel, lung NCI-H522, ovarian OVCAR-3 and prostate PC-3 cells were found to be most sensitive with GI50 of 0.12, 0.18 and 0.17 μ m, respectively. The COMPARE analysis suggested that the molecular mode of action of chrysoplenetin was unique compared with the existing anticancer drugs. Copyright © 2011 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Abstract: From a MeOH extract of Lunasia amara, which showed the cytochrome P450 2D6 (CYP2D6) inhibition, 14 acridone alkaloids including two new alkaloids [5-hydoroxygraveoline (1) and 8-methoxyifflaiamine (2)] were identified. Among the 14 acridone alkaloids, 5-hydoroxygraveoline (1) and lunamarine (3) showed moderate inhibition selective for CYP2D6, with IC50 values of 4.7μM and 1.8μM, respectively. [Copyright &y& Elsevier]

Syntheses of the structures postulated for 179 and 207E, members of a proposed new class of poison-frog alkaloids, 6,7-dehydro-5,8-disubstituted indolizidines, are described. The FT-IR spectrum and GC retention time of the synthetic 207E were different from those of the natural product; consequently the original structure of 207E needs to be revised. It is likely that the position of the double bond is instead at the 7,8-position. [ABSTRACT FROM AUTHOR]

Two new prenylated flavones, artocarpones A and B ( 1 and 2), and seven known isoprenylated flavonoids, artonin A ( 3), cycloheterophyllin ( 4), artoindonesianin E ( 5), artoindonesianin R ( 6), heterophyllin ( 7), heteroflavanone C ( 8), and artoindonesianin A-2 ( 9), have been isolated from the stem bark of Artocarpus champeden. Their structures were determined by spectroscopic analysis. Among the compounds isolated, 8 had the most potent inhibitory activity against the growth of Plasmodium falciparum 3D7 clone, with an IC50 value of 1 nmol L−1. [ABSTRACT FROM AUTHOR]

Among 42 extracts, prepared from 14 medicinal plants used in Vietnamese traditional medicine to treat malaria, 24 were found to have antiplasmodial activity by inhibiting the growth of the chloroquine-resistant Plasmodium falciparum strain FCR-3 with EC50 values less than 10 μg/ml. Each medicinal plant possessed at least one active extract. The methanol extract of Coscinium fenestratum had the strongest antiplasmodial activity with EC50 value of 0.5 μg/ml. Activity-guided fractionation led to identification of berberine as the major active constituent. [Copyright &y& Elsevier]

Previously purified and isolated compounds of novel alkyl methyl quinolone alkaloids (AM quinolones) from Gosyuyu (Wu-Chu-Yu), a Chinese herbal medicine, have a strong and highly selective antibacterial activity against Helicobacter pylori in vitro. To clarify the antibacterial mechanism(s) of AM quinolones, we examined the effects of AM quinolones on respiration of H. pylori in vitro. One week after treatment with AM quinolones alone (2, 10 or 20 mg/kg/day, orally) or combinations of AM quinolones and omeprazole (30 mg/kg/day) for H. pylori (1 x 10(8) cfu)-infected Mongolian gerbils, we checked viable H. pylori and myeloperoxidase (MPO) activity in the gastric tissues. AM quinolones decreased the number of H. pylori and inhibited H. pylori respiration in a dose-dependent manner. AM quinolones decreased the number of viable H. pylori (AM quinolones alone: 46.0 +/- 22.6 x 10(4), 17.3 +/- 4.9 x 10(4) and 8.1 +/- 6.6 x 10(4) cfu/stomach, respectively; and combinations of AM quinolones and omeprazole: 8.0 +/- 5.6 x 10(4), 4.2 +/- 2.5 x 10(4) and 5.5 +/- 2.7 x 10(4) cfu/stomach) compared with the vehicle-treated group (control: 359.9 +/- 180.3 x 10(4) cfu/stomach). AM quinolones significantly decreased MPO activity of H. pylori-inoculated gastric tissues. These findings suggest that AM quinolones have a potent antibacterial effect against H. pylori through respiratory inhibition, and reduced bacterial growth in vivo. AM quinolones might be novel therapeutic agents for H. pylori eradication. [ABSTRACT FROM AUTHOR]

We analyzed midterm results using the Bicarbon valve in a single center. Forty-four patients had aortic valve replacement (AVR), 48 had mitral valve replacement (MVR), and 13 had both aortic and mitral valve replacement (DVR). The mean age of the 105 patients was 61.2 ± 11.3 years. The mean follow-up was 1.8 ± 1.1 years with a cumulative follow-up of 188 patient-years. There were 5 early deaths (4.7%: 4 in the AVR group and 1 in the MVR group) and 5 late deaths (2.7% per patient-year: 3 malignancy, 1 cerebral hemorrhage, 1 myocardial infarction). Survival at 3 years was 91 ± 4% in the AVR group, 92 ± 5% in the MVR group, and 66 ± 23% in the DVR group. The linearized incidence of thromboembolic complications, hemorrhagic complications, and paravalvular leaks in all patients was 1.06 ± 2.34%, 1.60 ± 2.53%, and 0.53 ± 2.22% per patient-year, respectively. No other complications were observed. In conclusion, the Bicarbon prosthetic heart valve has shown excellent clinical results associated with a low incidence of valve-related complications. [ABSTRACT FROM AUTHOR]

Nine novel highly oxygenated and structurally diverse diterpenes, named norstaminolactone A (1), norstaminols B and C (2 and 3), secoorthosiphols A–C (4–6) and orthosiphols R–T (7–9) have been isolated from the aerial part of Orthosiphon stamineus cultivated in Okinawa Prefecture, Japan. Norstaminolactone A (1) is the first representative of a biogenetically unusual norstaminane-type diterpene bearing a nitrogen atom. Norstaminol C (3) possessed a framework presumed to be biosynthesized from the staminane-type diterpene. Secoorthosiphols A–C (4–6) possessed an unprecedented structural feature of the opened ring A system, encountered for the first time in isopimarane-type diterpenes. Secoorothosiphol C (6) also represents the first example of biogenetically unique and unconventional secoisopimarane-type diterpene bearing a cyano group. Norstaminolactone A (1) showed a potent antiproliferative activity with an IC50 value of 2.16 μg/mL against highly liver metastatic colon 26-L5 carcinoma cell line. [Copyright &y& Elsevier]