Developing Photoactive Coumarin-Caged N-Hydroxysulfonamides for Generation of Nitroxyl (HNO).

Photoactive N-hydroxysulfonamides photocaged with the (6-bromo-7-hydroxycoumarin-4-yl)methyl chromophore have been successfully synthesized, and the mechanisms of photodecomposition investigated for two of the compounds. Upon irradiation up to 97% of a diagnostic marker for (H)NO release, sulfinate was observed for the trifluoromethanesulfonamide system. In the absence of a species that reacts rapidly with (H)NO, (H)NO instead reacts with the carbocation intermediate to ultimately generate (E)-BHC-oxime and (Z)-BHC-oxime. Alternatively, the carbocation intermediate reacts with solvent water to give a diol. Deprotonation of the N(H) proton is required for HNO generation via concerted C-O/N-S bond cleavage, whereas the protonation state of the O(H) does not affect the observed photoproducts. If the N(H) is protonated, C-O bond cleavage to generate the parent N-hydroxysulfonamide will occur, and/or O-N bond cleavage to generate a sulfonamide. The undesired competing O-N bond cleavage pathway increases when the volume percentage of water in acetonitrile/water solvent mixtures is increased.

Exploring the Potential of 2-(2-Nitrophenyl)ethyl-Caged N-Hydroxysulfonamides for the Photoactivated Release of Nitroxyl (HNO).

The emergence of nitroxyl (HNO) as a biological signaling molecule is attracting increasing attention. HNO-based prodrugs show considerable potential in treating congestive heart failure, with HNO reacting rapidly with metal centers and protein-bound and free thiols. A new class of 2-(2-nitrophenyl)ethyl (2-NPE)-photocaged N-hydroxysulfonamides has been developed, and the mechanisms of photodecomposition have been investigated. Three photodecomposition pathways are observed: the desired concomitant C-O/N-S bond cleavage to generate HNO, sulfinate, and 2-nitrostyrene, C-O bond cleavage to give the parent sulfohydroxamic acid and 2-nitrostyrene, and O-N bond cleavage to release a sulfonamide and 2-nitrophenylacetaldehyde. Laser flash photolysis experiments provide support for a Norrish type II mechanism involving 1,5-hydrogen atom abstraction to generate an aci-nitro species. A mechanism is proposed in which the (Z)-aci-nitro intermediate undergoes either C-O bond cleavage to release RSO2NHO(H), concerted C-O/N-S bond cleavage to generate sulfinate and HNO, or isomerization to the (E)-isomer prior to O-N bond cleavage. The pKa of the N(H) of the N-hydroxysulfonamide plays a key role in determining whether C-O or concerted C-O/N-S bond cleavage occurs. Deprotonating this site favors the desired C-O/N-S bond cleavage at the expense of an increased level of undesired O-N bond cleavage. Triplet state quenchers have no effect on the observed photoproducts.

Mechanistic Insights into Rapid Generation of Nitroxyl from a Photocaged N-Hydroxysulfonamide Incorporating the (6-Hydroxynaphthalen-2-yl)methyl Chromophore.

HNO is a highly reactive molecule that shows promise in treating heart failure. Molecules that rapidly release HNO with precise spatial and temporal control are needed to investigate the biology of this signaling molecule. (Hydroxynaphthalen-2-yl)methyl-photocaged N-hydroxysulfonamides are a new class of photoactive HNO generators. Recently, it was shown that a (6-hydroxynaphthalen-2-yl)methyl (6,2-HNM)-photocaged derivative of N-hydroxysulfonamide incorporating the trifluoromethanesulfonamidoxy group (1) quantitatively generates HNO. Mechanistic studies have now been carried out on this system and reveal that the ground state protonation state plays a key role in whether concerted heterolytic C-O/N-S bond cleavage to release HNO occurs versus undesired O-N bond cleavage. N-Deprotonation of 1 can be achieved by adding an aqueous buffer or a carboxylate salt to an aprotic solvent. Evidence is presented for C-O/N-S bond heterolysis occurring directly from the singlet excited state of the N-deprotonated parent molecule on the picosecond time scale, using femtosecond time-resolved transient absorption spectroscopy, to give a carbocation and 1NO-. This is consistent with the observation of significant fluorescence quenching when HNO is generated. The carbocation intermediate reacts rapidly with nucleophiles including water, MeOH, or even (H)NO in the absence of a molecule that reacts rapidly with (H)NO to give an oxime.

Recession, recovery and suicide in mental health patients in England: time trend analysis.

BACKGROUND: The 2008 economic recession was associated with an increase in suicide internationally. Studies have focused on the impact in the general population with little consideration of the effect on people with a mental illness.AimsTo investigate suicide trends related to the recession in mental health patients in England. METHOD: Using regression models, we studied suicide trends in mental health patients in England before, during and after the recession and examined the demographic and clinical characteristics of the patients. We used data from the National Confidential Inquiry into Suicide and Safety in Mental Health, a national data-set of all suicide deaths in the UK that includes detailed clinical information on those seen by services in the last 12 months before death. RESULTS: Between 2000 and 2016, there were 21 224 suicide deaths by patients aged 16 or over. For male patients, following a steady fall of 0.5% per quarter before the recession (quarterly percent change (QPC) 2000-2009 -0.46%, 95% CI -0.66 to -0.27), suicide rates showed an upward trend during the recession (QPC 2009-2011 2.37%, 95% CI -0.22 to 5.04). Recession-related rises in suicide were found in men aged 45-54 years, those who were unemployed or had a diagnosis of substance dependence/misuse. Between 2012 and 2016 there was a decrease in suicide in male patients despite an increasing number of patients treated. No significant recession-related trends were found in women. CONCLUSIONS: Recession-associated increases in suicide were seen in male mental health patients as well as the male general population, with those in mid-life at particular risk. Support and targeted interventions for patients with financial difficulties may help reduce the risk at times of economic hardship. Factors such as drug and alcohol misuse also need to be considered. Recent decreases in suicide may be related to an improved economic context or better mental healthcare.Declaration of interestN.K. is supported by Greater Manchester Mental Health NHS Foundation Trust. L.A. chairs the National Suicide Prevention Strategy Advisory Group at the Department of Health (of which N.K. is also a member) and is a non-executive Director for the Care Quality Commission. N.K. chairs the National Institute for Health and Care Excellence (NICE) depression in adults guideline and was a topic expert member for the NICE suicide prevention guideline.

Folate/Vitamin B12 Supplementation Combats Oxidative Stress-Associated Carcinogenesis in a Rat Model of Colon Cancer.

Folate and vitamin B12 deficiency is associated with depletion of the major intracellular antioxidant glutathione, and oxidative stress is emerging as an etiological mechanism for colon cancer. Azoxymethane (AOM), a potent carcinogen, induces colon cancer in rats by causing pathophysiological changes and oxidative stress. We investigated the synergistic effect of folate and vitamin B12 supplementation against AOM-induced carcinogenesis and oxidative stress in rat colon. Adult male rats were distributed into four groups: 1) Basal diet only; 2) AOM injection (15 mg/kg once per week in weeks 5 and 6); 3) Folate and vitamin B12 supplemented diet; 4) Folate and B12 diet with AOM injection. After 16 weeks, rats were sacrificed, colon tissue dissected, indicators of oxidative stress were measured, and immunohistochemical and ultrastructural changes were evaluated. AOM-injected rats showed oxidative stress, evident by glutathione depletion, oxidation of cellular proteins, and DNA oxidative damage. AOM increased mucosal levels of antiapoptotic and proapoptotic proteins Bcl2 and Bax and caused ultrastructure changes in colonic cell organelles. Folate and vitamin B12 supplementation decreased the level of oxidative stress and ameliorated the cytotoxic effects of AOM. In this in vivo experimental model of colon cancer, folate and vitamin B12 supplementation combats carcinogen-induced oxidative stress.

Amelioration of azoxymethane induced-carcinogenesis by reducing oxidative stress in rat colon by natural extracts.

BACKGROUND: Azoxymethane (AOM) is a potent carcinogenic agent commonly used to induce colon cancer in rats; the cytotoxicity of AOM is considered to mediate oxidative stress. This study investigated the chemopreventive effect of three natural extracts [pomegranate peel extract (PomPE), papaya peel extract (PapPE) and seaweed extract (SE)] against AOM-induced oxidative stress and carcinogenesis in rat colon. METHODS: Eighty Sprague-Dawley rats (aged 4 weeks) were randomly divided into 8 groups (10 rats/group). Control group was fed a basal diet; AOM-treated group was fed a basal diet and received AOM intraperitonial injections for two weeks at a dose of 15 mg/kg bodyweight, whereas the other six groups were received oral supplementation of PomPE, PapPE or SE, in the presence or absence of AOM injection. All animals were continuously fed ad-libitum until aged 16 weeks, then all rats were sacrificed and the colon tissues were examined microscopically for pathological changes and aberrant crypt foci (ACF) development, genotoxicity (induced micronuclei (MN) cells enumeration), and glutathione and lipid peroxidation. RESULTS: Our results showed that AOM-induced ACF development and pathological changes in the colonic mucosal tissues, increased bone marrow MN cells and oxidative stress (glutathione depletion, lipid peroxidation) in rat colonic cells. The concomitant treatment of AOM with PomPE, PapPE or SE significantly ameliorated the cytotoxic effects of AOM. CONCLUSIONS: The results of this study provide in-vivo evidence that PomPE, PapPE and SE reduced the AOM-induced colon cancer in rats, through their potent anti-oxidant activities.

Efficiency of Electronic Nose in Detecting the Microbial Spoilage of Fresh Sardines (Sardinella longiceps).

The assessment of microbial spoilage in fresh fish is a major concern for the fish industry. This study aimed to evaluate the efficiency and reliability of an electronic nose (E-nose) to detect microbial spoilage of fresh sardines (Sardinella longiceps) by comparing its measurements with Total Bacterial Count (TBC), Hydrogen Sulfide (H2S) producing bacterial count and Trimethylamine Oxide (TMAO) reducing bacterial count after variable storage conditions. The samples were stored at 0 °C (0, 2, 4, 6, and 8 days) and 25 °C (0, 3, 6, and 9 h), while day 0 was used as a control. The E-nose measurements were analyzed by Principal Component Analysis (PCA), Linear Discriminant Analysis (LDA) and Artificial Neural Network (ANN). Microbial counts increased significantly and simultaneously with the changes in E-nose measurements during storage. The LDA and ANN showed a good classification of E-nose data for different storage times at two storage temperatures (0 °C and 25 °C) compared to PCA. It is expected as PCA is based on linear relationships between the factors, while ANN is based on non-linear relationships. Correlation coefficients between E-nose and TBC, TMAO-reducing bacterial and H2S-producing bacterial counts at 0 °C were 0.919, 0.960 and 0.915, respectively, whereas at 25 °C, the correlation coefficients were 0.859, 0.945 and 0.849, respectively. These positive correlations qualify the E-nose as an efficient and reliable device for detecting microbial spoilage of fish during storage.

Impact of drinking of saline water on hemato-biochemical parameters of Black Bengal goats in the selected areas of Bangladesh.

Global climatic changes are contaminating ground and surface water sources around the world, resulting in increased salinity. Knowing the animals' typical physiological capability for salinity tolerance without compromising their health is a necessity. The research was undertaken to determine the impacts of drinking water salinity on hemato-biochemical parameters of Black Bengal goats. A total of 40 Black Bengal goats (20 male and 20 female), age ranging from 1 to 5 years, were randomly selected and divided into 2 groups. The animals of group 1 received higher saline water (12 ppt) and those in group 2 received lower saline water (1 ppt) as regular drinking water. Blood parameters of all selected goats were measured. Serum creatinine, uric acid, urea, potassium, sodium, and chloride were significantly higher (P< 0.05) in the animals of group 1 compared with group 2, although serum phosphorous was significantly lower (P < 0.05) in group 1 compared with group 2. There were no significant differences in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), glucose, magnesium, and calcium between the animals of group 1 and 2. AST and magnesium differed significantly (P < 0.05) between young and adult goats in group 1. Glucose and urea levels were slightly higher (P < 0.05) in young goats. In both groups, male goats had significantly higher (P < 0.05) serum potassium and urea levels than female goats. The results suggest that Black Bengal goats of the coastal areas have different salt tolerance capacities based on their age and sex, and adapt to higher salinity by changing kidney functions.

Ovarian tumors associated with pregnancy: a 20-year experience in a teaching hospital.

OBJECTIVE: Pregnancy associated with ovarian tumors was reviewed over a 20-year period to determine the maternal and fetal outcome in patients undergoing surgery during pregnancy. METHOD: A retrospective study of 94 cases of ovarian tumors treated surgically during pregnancy was investigated for incidence, clinico-pathological features and outcome in a teaching hospital between June 1987 and May 2007. RESULTS: The overall incidence of ovarian tumor in pregnant women was 1 in 505 (0.2%) deliveries. Diagnosis of 69.2% tumors resulted in the first and second trimesters of pregnancy. Twenty-two (23.4%) patients presented as an emergency at different periods of gestation and 16 (17.1%) tumors were incidentally discovered at cesarean section which underlines the significance of examining the ovaries routinely at cesarean section. Benign teratoma (39.4%) and serous cystadenoma (24.5%) were the most common types of ovarian tumors found in the study. The incidence of malignant tumors was 5.3%. Tumors with low malignant potential comprised 40% of malignancy. The miscarriage rate after surgery was 44.4% in the first trimester compared with 16.6% in the second trimester. The preterm birth rate was 4.3% in the series. CONCLUSION: The value of clinical and ultrasound examinations in early pregnancy as a diagnostic aid is highlighted. Whenever an ovarian tumor is detected in pregnancy, malignancy should always be suspected. Treatment of an ovarian tumor in pregnancy should be tailored according to the age, parity, clinical presentation, gestational age and histopathology of the tumor. Removal of persisting or enlarging ovarian masses as soon as possible is important to obtain a final histologic diagnosis and rule out malignancy. Early diagnosis and appropriate treatment of malignant tumors offers the best prognosis for the patient.

Analyzing Tumor Heterogeneity by Incorporating Long-Range Mutational Influences and Multiple Sample Data into Heterogeneity Factorial Hidden Markov Model.

Cancer arises from successive rounds of mutations, resulting in tumor cells with different somatic mutations known as clones. Drug responsiveness and therapeutics of cancer depend on the accurate detection of the clones in a tumor sample. Recent research has considered inferring clonal composition of a tumor sample using computational models based on the short read data of the sample generated using the next-generation sequencing (NGS) technology. Short reads (segmented DNA parts of different tumor cells) are noisy; therefore, inferring the clones and their mutations from the data is a difficult and complex problem. Existing methods to infer clones from noisy NGS data do not consider the presence of long-range mutational influences. Therefore, we develop a new model, called extended multiple sample tumor heterogeneity prediction by factorial Hidden Markov model (emHetFHMM), based on factorial hidden Markov models to infer clones and their proportions by capturing the long-range mutational influences. In our model, each hidden chain represents the genomic signature of a clone, and a mixture of chains results in the observed data. We make use of Gibbs sampling and exponentiated gradient algorithms to infer the hidden variables and mixing proportions. We compare our model with strong models from the previous work (PyClone, PhyloSub, and HetFHMM) based on both synthetic data and real cancer data from acute myeloid leukemia. Empirical results confirm that emHetFHMM infers clonal composition of a tumor sample more accurately than previous studies.

HetFHMM: A Novel Approach to Infer Tumor Heterogeneity Using Factorial Hidden Markov Models.

Cancer arises from successive rounds of mutations, resulting in tumor cells with different somatic mutations known as clones. Drug responsiveness and therapeutics of cancer depend on the accurate detection of clones in a tumor sample. Recent research has considered inferring clonal composition of a tumor sample using computational models based on short read data of the sample generated using next-generation sequencing (NGS) technology. Short reads (segmented DNA parts of different tumor cells) are noisy; therefore, inferring the clones and their mutations from the data is a difficult and complex problem. We develop a new model called HetFHMM, based on factorial hidden Markov models, to infer clones and their proportions from noisy NGS data. In our model, each hidden chain represents the genomic signature of a clone, and a mixture of chains results in the observed data. We make use of Gibbs sampling and exponentiated gradient algorithms to infer the hidden variables and mixing proportions. We compare our model with strong models from previous work (PyClone and PhyloSub) based on both synthetic data and real cancer data on acute myeloid leukemia. Empirical results confirm that HetFHMM infers clonal composition of a tumor sample more accurately than previous work.

Bowel injury in gynecologic operations: analysis of 110 cases.

The incidence, risk factors, and morbidity were retrospectively reviewed of 110 intestinal injuries that occurred during gynecologic operations from January 1984 through December 2003 performed for benign and malignant conditions. The incidence of bowel injury was 0.54% in this series. Of the 110 bowel injuries, 37.3% occurred during opening of the peritoneal cavity, 38.2% during adhenolysis and pelvic dissection, 9% during laparoscopy, 9.1% sustained at vaginal operations, and 8.2% during dilatation and curettage. The small intestine was injured in 75.5% and large bowel in 24.5% of cases; 76.4% of all the injuries were minor, and 23.6% major. Standard surgical repair procedure of the bowel injury produced satisfactory results. It is recommended that gynecologists acquire a basic knowledge in the prevention and principles of management of intestinal injuries. Adherence to the standard surgical techniques during gynecologic operations and anticipation of bowel injury in high-risk patients will contribute to minimize the occurrence of such injuries.

Ameliorative Effects of Pomegranate Peel Extract against Dietary-Induced Nonalcoholic Fatty Liver in Rats.

Non-alcoholic fatty liver disease (NAFLD) is caused by fat accumulation and is associated with oxidative stress. In this study, we investigated the potential protective effect of pomegranate (Punica granatum L.) peel extract (PPE) against oxidative stress in the liver of rats with NAFLD. Sprague-Dawley rats were fed a high fat diet (HFD), 20% corn oil, or palm oil for 8 weeks in the presence or absence of PPE. The control group was fed a basal diet. The progression of NAFLD was evaluated histologically and by measuring liver enzymes (alanine transaminase and aspartate transaminase), serum lipids (triglycerides and total cholesterol), and oxidative stress markers. The HFD feeding increased the body weight and caused NAFLD, liver steatosis, hyperlipidemia, oxidative stress, and elevated liver enzymes. Administration of PPE ameliorated the hepatic morphology, reduced body weight, improved liver enzymes, and inhibited lipogenesis. Furthermore, PPE enhanced the cellular redox status in the liver tissue of rats with NAFLD. Our findings suggest that PPE could improve HFD-induced NAFLD via abolishment of hepatic oxidative damage and hyperlipidemia. PPE might be considered as a potential lead material in the treatment of NAFLD and obesity through the modulation of lipid metabolism.

Regioselective synthesis, characterization, and antimicrobial activities of some new monosaccharide derivatives.

A regioselective acylation series of methyl α-D-glucopyranoside (1), methyl 3-O-benzoyl-4,6-O-benzylidene-α-D-mannopyranoside (1A), and methyl 4,6-O-benzylidene-2-O-(3,5-dinitrobenzoyl)-α-D-mannopyranoside (1B) has been carried out by the direct acylation method and afforded the 2,6-di-O-glucopyranoside and 2 or 3-O-mannopyranoside derivatives in an excellent yield. In order to obtain newer products, the 2,6-di-O-glucopyranoside derivative was further transformed to a series of 3,4-di-O-acyl derivatives containing a wide variety of functionalities in a single molecular framework. The structures of the newly synthesized compounds were elucidated on the basis of IR, (1)H-NMR, (13)C-NMR, (13)C-DEPT spectral data, and elemental analysis. These synthesized derivatives were screened for in vitro antimicrobial activities against ten human pathogenic and five phytopathogenic microorganisms. A number of test compounds showed remarkable antimicrobial activity comparable to, and in some cases even higher than, the standard antibiotics employed. It was observed that methyl 3,4-di-O-(3-chlorobenzoyl)-2,6-di-O-hexanoyl-α-D-glucopyranoside (8) exhibited a varied range of MIC from 12.5 µg/disc to 25 µg/disc by the disk diffusion method and 1000 µg/mL to 1250 µg/mL by the broth macrodilution method.

Sedative activity of methanolic extract of Glochidion multiloculare (Rottler ex Willd) Voigt leaves.

Bangladesh is a good repository of medicinal plants. Traditional healers utilize them for treating many pathological states. Unfortunately, very few of them have been scientifically evaluated to know about the deep inside. The current study here is designed to evaluate the in vivo sedative activity of the leaves of Glochidion multiloculare (Rottler ex Willd) Voigt. With this purpose, the plant leaves were collected and powdered for extraction with methanol. Initially, the plant extract was subjected to brine shrimp lethality bioassay to monitor the presence of bioactive molecules. Later on, different neuropharmacological studies including hole cross, open field, thiopental-sodium induced sleeping time and Elevated-Plus Maze (EPM) tests were conducted to investigate sedative action. In the brine shrimp lethality bioassay, the LC50 value of the extract was found 37.19 µg mL(-1), whereas the standard vincristine sulphate showed the LC50 10.50 µg mL(-1). The moderate toxicity of the extract on brine shrimp indicated the existence of bioactive secondary metabolites in this extract. Besides, the extract decreased the locomotor activity of mice in hole cross, open field and EPM test indicating the CNS depression capability of the plant. Moreover, the extract was very much effective for prolonging the sleeping time (103 min) with quick onset of action (22 min) in comparison to the control group. The efficacy of the plant extract was found closer to the common sedative drug diazepam. Further investigations are required to explore the underlying mechanism of the sedative action and isolate bioactive principles.

Pomegranate (Punica granatum) peel extract efficacy as a dietary antioxidant against azoxymethane-induced colon cancer in rat.

Functional foods include antioxidant nutrients which may protect against many human chronic diseases by combating reactive oxygen species (ROS) generation. The purpose of the present study was to investigate the protective effect of pomegranate peel extract (PPE) on azoxymethane (AOM)-induced colon tumors in rats as an in vivo experimental model. Forty Sprague-Dawley rats (4 weeks old) were randomly divided into 4 groups containing 10 rats per group, and were treated with either AOM, PPE, or PPE plus AOM or injected with 0.9% physiological saline solution as a control. At 8 weeks of age, the rats in the AOM and PPE plus AOM groups were injected with 15 mg AOM/kg body weight, once a week for two weeks. After the last AOM injection, the rats were continuously fed ad-libitum their specific diets for another 6 weeks. At the end of the experiment (i.e. at the age of 4 months), all rats were killed and the colon tissues were examined microscopically for lesions suspected of being preneoplastic lesions or tumors as well as for biochemical measurement of oxidative stress indices. The results revealed a lower incidence of aberrant crypt foci in the PPE plus AOM administered group as compared to the AOM group. In addition, PPE blocked the AOM-induced impairment of biochemical indicators of oxidative stress in the examined colonic tissue homogenates. The results suggest that PPE can partially inhibit the development of colonic premalignant lesions in an AOM-induced colorectal carcinogenesis model, by abrogating oxidative stress and improving the redox status of colonic cells.

Ovarian tumors in children and adolescents--a clinical study of 52 patients in a university hospital.

STUDY OBJECTIVE: To review the clinical presentation of ovarian tumors in children and adolescents treated at the University of Dammam and King Fahad University Hospital. DESIGN: Data of the patients was noted retrospectively from the hospital medical records regarding age, presentation, diagnosis, treatment, and outcome. SETTING: The study was carried out in the Ob/Gyn department at King Fahad Hospital of Dammam University, Saudi Arabia between January 1985 and December 2009. PARTICIPANTS: There were 52 patients between 6 and 20 years of age who presented with an ovarian tumor during the study period. INTERVENTION: Preoperative diagnostic approach included history, physical examination, ultrasonography, radiological examination, tumor markers, operative treatment, and histopathological examination of the tumor. Chemotherapy was given to patients where indicated. RESULTS: The main presenting symptom was abdominal pain in 30 (58%) patients. Of the neoplastic tumors, 87% were germ cell tumors, of which 73% were benign while 13% were malignant. Operative procedures included 48 (92%) exploratory laparotomies and 4 (8%) laparoscopic resections. Ovarian cystectomy was done in 23 (44%) patients and salpingoophorectomy in 28 (54%) patients. Of the 7 (13%) patients with malignant tumors, five received postoperative chemotherapy. Three patients with malignancy died in the series. CONCLUSION: Early diagnosis of ovarian masses in young girls is important. Since most of these masses are benign, operation should be designed to optimize future fertility, while the treatment of malignant tumors would involve complete staging, resection of the tumor, postoperative chemotherapy when indicated, to give the patient a chance for future childbearing.

A new 7-oxygenated coumarin from Clausena suffruticosa.

A new coumarin, 7-[(2'E,6'E)-7'-carboxy-5'(zeta)-hydroxy-3'-methylocta-2',6'-dienyloxy]-coumarin, was isolated from the leaf of Clausena suffruticosa. Its structure was established by means of spectroscopic data analyses, including mass spectrometry and both 1D and 2D NMR spectroscopy.

An unusual bisnor-clerodane diterpenoid from Polyalthia simiarum.

The stem bark of Polyalthia simiarum has yielded a new bisnor-type clerodane diterpenoid, 2-oxo-14,15-bisnor-3,11E-kolavadien-13-one (1), and three previously known clerodane derivatives, kolavenic acid (2), 16beta-hydroxycleroda-3,13(14)Z-dien-15,16-olide (3), and 16-oxocleroda-3,13(14)E-dien-15-oic acid (4). The structures of these compounds were unambiguously determined by extensive NMR studies as well as by comparison with related compounds. Till now this is the second report of the occurrence of any unusual C-18 clerodane diterpenoid from nature. The crude light petroleum extract and the purified compound 3 demonstrated moderate free radical scavenging activity with IC50 values of 21.5 and 23.5 microg/mL, respectively.

Chemical and biological investigations of Delonix regia (Bojer ex Hook.) Raf.

In this study, five compounds, lupeol (1), epilupeol (2), ß-sitosterol (3), stigmasterol (4) and p-methoxybenzaldehyde (5) were isolated from the petroleum ether and dichloromethane fractions of a methanolic extract of the stem bark of Delonix regia. Antimicrobial screening of the different extracts (15 µg mm-2) was conducted by the disc diffusion method. The zones of inhibition demonstrated by the petroleum ether, carbon tetrachloride and dichloromethane fractions ranged from 9-14 mm, 11-13 mm and 9-20 mm, respectively, compared to kanamycin standard with the zone of inhibition of 20-25 mm. In brine shrimp lethality bioassay, the carbon tetrachloride soluble materials demonstrated the highest toxicity with LC50 of 0.83 µg mL-1, while petroleum ether and dichloromethane soluble partitionates of the methanolic extract revealed LC50 of 14.94 and 3.29 µg mL-1, respectively, in comparison with standard vincristine sulphate with LC50 of 0.812 µg mL-1. This is the first report on compounds separation from D. regia, their antimicrobial activity and cytotoxicity.