Dry ripe fruit of Aegle marmelos as anti-ulcer agent against ethanol induced gastric mucosal injury.

Aegle marmelos is cost-effective valuable South Asian tree. The folklore data reported its wide range pharmacological effects. In spite of vast reported work on various parts, the dry ripe fruit extract has not yet been studied for gastric ulcers. Present study is planned to investigate its potential protective effects against ethanol-induced gastric injury in rats. In current study the gastro protective effect of ethanolic crude extract of A. marmelos dried ripe fruit at 200, 400 and 800mg/kg body weight were studied in albino rats. Ranitidine used as standard drug (50mg/kg body weight). Absolute ethanol increase the degree of ulceration (UI) in rats while a significant improvement in the level of inhibition against ulceration was observed in test and standard groups as compare to control. Pre-fed test drug exhibited a significant reduction in the sore area (UI), accelerate % age protection and increased of gastric content in dose dependence manner. Test drug at 800mg/kg dose showed marked deduction in mean UI 3.0, significant increase in protection 83% with pH 7.3 (p<0.01). Standard drug exhibited 3.25 UI, 81% protection with pH 7.1. In conclusion, it was found that dry ripe fruit of A. marmelos possesses a significant anti-ulcer effect in rats.

Substituted Benzimidazole Analogues as Potential α-Amylase Inhibitors and Radical Scavengers.

Benzimidazole scaffolds are known to have a diverse range of biological activities and found to be antidiabetic and antioxidant. In this study, a variety of arylated benzimidazoles 1-31 were synthesized. Except for compounds 1, 6, 7, and 8, all are new derivatives. All compounds were screened for α-amylase inhibitory, 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. In vitro screening results revealed that all molecules demonstrated significant α-amylase inhibition with IC50 values of 1.86 ± 0.08 to 3.16 ± 0.31 µM as compared to standard acarbose (IC50 = 1.46 ± 0.26 µM). However, compounds showed significant ABTS and DPPH radical scavenging potentials with IC50 values in the range of 1.37 ± 0.21 to 4.00 ± 0.10 µM for ABTS and 1.36 ± 0.09 to 3.60 ± 0.20 µM for DPPH radical scavenging activities when compared to ascorbic acid with IC50 values of 0.72 ± 0.21 and 0.73 ± 0.05 µM for ABTS and DPPH radical scavenging potentials, respectively. Structure-activity relationship (SAR) was established after critical analysis of varying substitution effects on α-amylase inhibitory and radical scavenging (ABTS and DPPH) potentials. However, molecular docking was also performed to figure out the active participation of different groups of synthetic molecules during binding with the active pocket of the α-amylase enzyme.

New Hybrid Scaffolds based on Hydrazinyl Thiazole Substituted Coumarin; As Novel Leads of Dual Potential; In Vitro α-Amylase Inhibitory and Antioxidant (DPPH and ABTS Radical Scavenging) Activities.

BACKGROUND: Despite many side effects associated, there are many drugs which are being clinically used for the treatment of type-II diabetes mellitus (DM). In this scenario, there is still need to develop new therapeutic agents with more efficacy and less side effects. By keeping in mind the diverse spectrum of biological potential associated with coumarin and thiazole, a hybrid class based on these two heterocycles was synthesized. METHOD: Hydrazinyl thiazole substituted coumarins 4-20 were synthesized via two step reaction. First step was the acid catalyzed reaction of 3-formyl/acetyl coumarin derivatives with thiosemicarbazide to form thiosemicarbazone intermediates 1-3, followed by the reaction with different phenacyl bromides to afford products 4-20. All the synthetic analogs 4-20 were characterized by different spectroscopic techniques such as EI-MS, HREI-MS, 1H-NMR and 13C-NMR. Stereochemical assignment of the iminic double bond was carried out by the NOESY experiments. Elemental analysis was found in agreement with the calculated values. RESULTS: Compounds 4-20 were screened for α-amylase inhibitory activity and showed good activity in the range of IC50 = 1.829 ± 0.102-3.37 ± 0.17 µM as compared to standard acarbose (IC50 = 1.819 ± 0.19 µM). Compounds were also investigated for their DPPH and ABTS radical scavenging activities and displayed good radical scavenging potential. In addition to that molecular modelling study was conducted on all compounds to investigate the interaction details of compounds 4- 20 (ligands) with active site (receptor) of enzyme. CONCLUSION: The newly identified hybrid class may serve as potential lead candidates for the management of diabetes mellitus.

Synthesis, in vitro ß-glucuronidase inhibitory activity and in silico studies of novel (E)-4-Aryl-2-(2-(pyren-1-ylmethylene)hydrazinyl)thiazoles.

Current research is based on the synthesis of novel (E)-4-aryl-2-(2-(pyren-1-ylmethylene)hydrazinyl)thiazole derivatives (3-15) by adopting two steps route. First step was the condensation between the pyrene-1-carbaldehyde (1) with the thiosemicarbazide to afford pyrene-1-thiosemicarbazone intermediate (2). While in second step, cyclization between the intermediate (2) and phenacyl bromide derivatives or 2-bromo ethyl acetate was carried out. Synthetic derivatives were structurally characterized by spectroscopic techniques such as EI-MS, 1H NMR and 13C NMR. Stereochemistry of the iminic double bond was confirmed by NOESY analysis. All pure compounds 2-15 were subjected for in vitro ß-glucuronidase inhibitory activity. All molecules were exhibited excellent inhibition in the range of IC50=3.10±0.10-40.10±0.90µM and found to be even more potent than the standard d-saccharic acid 1,4-lactone (IC50=48.38±1.05µM). Molecular docking studies were carried out to verify the structure-activity relationship. A good correlation was perceived between the docking study and biological evaluation of active compounds.

Evaluation of nutritional and sub-acute toxicological study of plant based supplement of Achyranthes aspera.

The present study was conducted for the nutritional, microbiological and toxicological evaluation of test compound having main ingredient Achyranthes aspera. Nutritional value assessment, microbiological analysis and toxicological studies were conducted according to the standard reported methods which exhibited that A. aspera contains moisture 4.05%, proteins 20.54%, fats 0.903%, ash 20.25%, carbohydrates 54,26% and energy 294 Kcal. Vitamin profile was found to be B(1) 0.27mg/100g, B(2) 0.28mg/100g, B(3) 0.58mg/100g, B(6) 0.27mg/100g and B(9) 39µg/100g. The content of sodium, calcium, magnesium, potassium, chloride and phosphorus was found to be 1119.67, 5385.23, 5446.08, 1343.6, 675880.73 and 1447.5mg/kg respectively and trace metals i.e. iron, copper, zinc, manganese and aluminum were detected as 283.05, 8.062, 48.37, 16.12 and 9.853 mg/kg respectively. The microbiological result indicated that the compound qualifies the international standards of microbial limit and was found free from Salmonella species. The toxicological study was conducted to find safe use of Achyranthes aspera compound in human as a nutritive supplement in blood disorders. The toxicity studies exhibited that the test compound has a good effect on general health as an increase in body weights of animals of test group was noticed as compared to that of control group. Blood parameters before and after the study were monitored which confirms our hypothesis by showing an increase in hemoglobin from 9.133 to 10.96, RBC count from 3.11 to 3.6, WBC count from 5.68 to 5.73 and platelets from 245 to 319.

A large unilocular mucinous cystadenoma in third trimester of pregnancy.

Ovarian malignancy is the second most common gynaecological malignancy diagnosed during pregnancy. A grand multipara, aged 30 years presented with gestational amenorrhea with abdominal discomfort and breathlessness for last 15 days. Sonographic examination demonstrated a huge, unilocular ovarian cyst and an alive fetus of about 30 weeks gestation. Intraoperative findings were huge left ovarian cyst (42x40x20 cm) with straw coloured mucinous fluid. Left salpingo-oophorectomy was performed followed by peritoneal washings and omental biopsy. Histopathology revealed mucinous cystadenomas with inflammatory changes in omentum and no malignant cells in peritoneal washings. She delivered vaginally a female baby of 3.5 kg at 38 weeks with good Apgar score.

Uterine rupture associated with the use of intra-vaginal misoprostol during second-trimester pregnancy termination.

Intravaginal Misoprostol is being used with excellent results for second trimester pregnancy termination, worldwide. However, there are many case reports of serious complications of uterine rupture in such cases, both in previously scarred as well as in unscarred uterus. In this report, we describe a case of uterine rupture in an unscarred uterus during second-trimester pregnancy termination with intravaginal misoprostol.

Oral misoprostol for induction of labour.

OBJECTIVE: To determine the effect of oral Misoprostol in labour induction with respect to ease of administration and induction-to-delivery time interval. STUDY DESIGN: Observational study. PLACE AND DURATION OF STUDY: Gynaecology/Obstetrics Department, Holy Family Hospital, Rawalpindi, from March to August 2006. METHODOLOGY: Women with live singleton pregnancy of > 37 weeks gestation with cephalic presentation, with an indication for induction of labour were inducted. Oral misoprostol 50 microg to 400 microg was given in divided doses at 4 hours interval upto a maximum of 4 doses, till labour was induced. Fetomaternal outcome and induction to delivering time interval in hours was noted. RESULTS: In 6 months duration, 250 mothers were recruited for the study. The main indication for labour induction was post date pregnancy (52%) and oxytocin was given in 50% cases. The majority (96%) of mothers went into labour but 4% (9) had failed induction. The majority (73%, n=176/241) of mothers delivered vaginally, 99% being delivered in the first 24 hours. Mean induction-delivery interval was 11+/-2.7 hours. Sixty five (27%) had to undergo emergency lower segment caesarean section, the major indication being fetal distress (41.5%, n=27) and meconium staining of liquor (40%, n=26). Again, a majority (95%) of the babies were delivered with good Apgar score. However, 10.8% developed meconium aspiration syndrome. Early neonatal deaths occurred in 0.8% (2) cases. Maternal hyper stimulation was seen in 1 case (0.4%). CONCLUSION: Oral misoprostol as an agent for labour induction in term pregnancy was easy to administer and the majority of women (99%) delivered in the first 24 hours.