Neuropharmacological and Antidiarrheal Potentials of Duabanga grandiflora (DC.) Walp. Stem Bark and Prospective Ligand-Receptor Interactions of Its Bioactive Lead Molecules.

Duabanga grandiflora (DC.) Walp. is an ethnomedicinally significant plant used to treat various illnesses, but there is little scientific evidence to support its use. This study explored the pharmacological activities of methanol extract of D. grandiflora stem barks (MEDG) through in vivo approaches in Swiss albino mice and a computer-aided molecular approach. The forced swimming test (FST), tail suspension test (TST), elevated plus maze (EPM), and hole board test (HBT) were used to determine anti-depressant and anxiolytic activity in experimental mice. In addition, anti-diarrheal studies were performed using castor oil-induced diarrhea, castor oil-induced enter pooling, and the charcoal-induced gastrointestinal motility test. MEDG showed substantial depletions in the immobility times in both FST and TST after treatment with the MEDG extract, whereas moderate anxiolytic activity was manifested at a higher dose (400 mg/kg) compared with the control. Correspondingly, MEDG extract revealed a significant reduction in wet feces and decreased the small intestinal transit of charcoal meal in castor oil-induced diarrhea and charcoal-induced gastrointestinal motility test. In the computer-aided molecular approaches, vanillin displayed a promising binding score for both anxiolytic and anti-diarrheal activities, while duabanganal C showed a promising score for the anti-depressant activity. The present experimental findings along with a computer-aided model conclude that MEDG could be a possible Phyto therapeutic agent with potential anti-depressant, anxiolytic and anti-diarrheal activity.

Plant-Based Indole Alkaloids: A Comprehensive Overview from a Pharmacological Perspective.

Plant-based indole alkaloids are very rich in pharmacological activities, and the indole nucleus is considered to contribute greatly to these activities. This review's fundamental objective is to summarize the pharmacological potential of indole alkaloids that have been derived from plants and provide a detailed evaluation of their established pharmacological activities, which may contribute to identifying new lead compounds. The study was performed by searching various scientific databases, including Springer, Elsevier, ACS Publications, Taylor and Francis, Thieme, Wiley Online Library, ProQuest, MDPI, and online scientific books. A total of 100 indole compounds were identified and reviewed. The most active compounds possessed a variety of pharmacological activities, including anticancer, antibacterial, antiviral, antimalarial, antifungal, anti-inflammatory, antidepressant, analgesic, hypotensive, anticholinesterase, antiplatelet, antidiarrheal, spasmolytic, antileishmanial, lipid-lowering, antimycobacterial, and antidiabetic activities. Although some compounds have potent activity, some only have mild-to-moderate activity. The pharmacokinetic profiles of some of the identified compounds, such as brucine, mitragynine, 7-hydroxymitragynine, vindoline, and harmane, were also reviewed. Most of these compounds showed promising pharmacological activity. An in-depth pharmacological evaluation of these compounds should be performed to determine whether any of these indoles may serve as new leads.

Pesticidal and pest repellency activities of rhizomes of Drynaria quercifolia (J. Smith) against Tribolium castaneum (Herbst).

BACKGROUND: Tribolium castaneum (Herbst) is a harmful pest of stored grain and flour-based products in tropical and subtropical region. In the present study, rhizome of Drynaria quercifolia (J. Smith) was evaluated for pesticidal and pest repellency activities against T. castaneum, using surface film method and filter paper disc method, respectively. In addition, activity of the isolated compound 3,4-dihydroxybenzoic acid was evaluated against the pest. RESULTS: Chloroform soluble fraction of ethanol extract of rhizome of D. quercifolia showed significant pesticidal activity at doses 0.88 to 1.77 mg/cm(2) and significant pest repellency activity at doses 0.94 to 0.23 mg/cm(2). No pesticidal and pest repellency activity was found for petroleum ether, ethyl acetate and methanol soluble fractions of ethanol extract as well as for 3,4-dihydroxybenzoic acid. CONCLUSION: Considering our findings it can be concluded that chloroform soluble fraction of rhizome of D. quercifolia is useful in controlling T. castaneum of stored grain and flour-based products.

Antinociceptive and cytotoxic activities of an epiphytic medicinal orchid: Vanda tessellata Roxb.

BACKGROUND: Vanda tessellata (Orchidaceae) has been used in different sorts of ailments such as inflammations, rheumatism, dysentery, bronchitis, dyspepsia and fever in folk medicine. In this study we evaluated the antinociceptive and cytotoxic effect of methanol and aqueous extracts of V. tessellata leaf. METHODS: Oral administration of V. tessellata aqueous (VTA) and methanol (VTM) leaf extracts at 200 and 400 mg/kg body weight (bw) doses were assessed for antinociceptive activity in acetic acid-induced writhing test, hot plate test, and tail immersion test in mice. In this study we also screened for cytotoxicity of the extracts by the brine shrimp (Artemia salina) lethality assay. RESULTS: The extracts, at both doses, exhibited a significant (p < 0.05 - < 0.01) dose-dependent antinociceptive activity in hot plate and tail immersion test. The reaction time was increased to the thermal stimuli at 200 and 400 mg/kg doses up to 90 min. In acetic acid-induced writhing test, oral administration of VTA and VTM (200 and 400 mg/kg) also decreased the writhing significantly while compared to control. The dose 400 mg/kg showed maximum percentage of pain inhibition 42.37% and 45.08% for VTA and VTM respectively. Diclofenac sodium (10 mg/kg) and nalbuphine (10 mg/kg) were used as reference antinociceptive drugs. Very low cytotoxicity was observed on brine shrimps lethality assay. CONCLUSIONS: The leaf extract has potential antinociceptive activity with minimum cytotoxicity. The present study supports the use of V. tessellata in different inflammatory disorders.

Evaluation of Antioxidant, Cytotoxic, Anti-Inflammatory, Antiarthritic, Thrombolytic, and Anthelmintic Activity of Methanol Extract of Lepidagathis hyalina Nees Root.

Lepidagathis hyalina Nees is an ethnomedicinally potential Asian herb, locally used to treat cardiovascular diseases and coughs. The study was intended to evaluate qualitative and quantitative investigation to ensure numerous pharmacological properties of methanol extracts of L. hyalina Ness root (MELHR). MELHR manifested strong radical scavenging activity in the reducing power and DPPH (1, 1-diphenyl-2-picrylhydrazyl) assays, and phenol and flavonoid in the quantitative assays. In the study of the thrombolytic assay, MELHR showed moderate explicit percentage of clot lysis (29.39 ± 1.40%) with moderate (135.35 µg/mL) toxic properties. The in vitro anti-inflammatory activity was evaluated by the inhibition of hypotonicity-induced RBC hemolysis, whereas the plant extract exhibited a significant (pp ˂ 0.005) dose-dependent inhibition and the highest inhibition was found 55.01 ± 3.22% at 1000 µg/mL concentration. Moreover, the MELHR also showed significant (p < 0.005) dose-dependent potentiality on protein denaturation which is considered as antiarthritic activity, and the peak inhibition was found significant (71.97 ± 2.71%) at 1000 µg/mL concentration. MELHR also exhibited the dose-dependent and statistically significant anthelmintic potential on aquarium worm (Tubifex tubifex). So, the present investigation suggests that L. hyalina could be the best choice for the management of cardiovascular, inflammation, arthritis, and anthelmintic diseases. Further investigation should be necessary to determine behind the mechanism of bioactivity and therapeutic potential of this plant.

An integrated exploration of pharmacological potencies of Bischofia javanica (Blume) leaves through experimental and computational modeling.

Bischofia javanica (Blume), an edible wild plant, has both prospective nutraceutical and therapeutic properties. Here, we intended to explore the pharmacological potentials of the methanol extract of B. javanica (MEBJ) through integrated approaches. Phytochemical screening revealed the presence of important phytoconstituents which were found to be safe during cytotoxicity analysis. The sedative potential of MEBJ (200 and 400 mg/kg) was determined by employing open field, hole cross, and thiopental sodium-induced sleeping time tests, where a significant reduction of the locomotor performance and an enhancement in the duration of sleeping have been observed, respectively. In addition, mice treated with MEBJ exhibited superior exploration during both elevated plus maze and hole board tests. In parallel, anti-diabetic potency was investigated via alpha-amylase inhibitory assay, where a dose-response increase in the percentage of inhibition has been marked. A similar response, such as an increased percentage of clot lysis, was observed during the thrombolytic test. Furthermore, molecular docking was performed with the identified compounds, demonstrated strong binding affinities to the target receptors of the experiments as mentioned above. Also, ADME/T and toxicological parameters verified the drug-like properties of the identified compounds. Collectively, these results indicate bioactivity of Bischofia javanica, which can be a potential candidate in the food and pharmaceutical industries.

Studies on the anti-diarrheal properties of leaf extract of Desmodium puchellum.

OBJECTIVE: To evaluate the pharmacological activity against diarrhea of methanol and petroleum ether extract of Desmodium puchellum (Family: Fabaceae) leaves. METHODS: The extract was evaluated for castor oil-induced diarrhea and enteropooling as well as intestinal motility in rats. Both of the extracts were given to the rats at 200 mg/kg orally. Loperamide was used as a standard drug for diarrhea. RESULTS: The diarrheal severity was reduced significantly (P<0.05) by methanol and petroleum ether extracts by 31.95% and 28.33%, respectively, whereas 54.75% inhibition was found for standard drug loperamide at 5 mg/kg. The two extracts also significantly (P<0.05) reduced the intestinal volume in case of castor oil induced enteropooling. CONCLUSIONS: It is concluded that both fractions contain some biologically active ingredients that are active for anti-diarrheal actions whereas methanol fraction has better potential.

Incidence of diabetes in Asian-Indian subjects: a five year follow-up study from Bangladesh.

AIMS: To determine the incidence of Type 2 diabetes and its risk factors. Further, to examine the effect of relative changes in obesity (BMI and waist circumference). METHODS: A sample of 2011 non-diabetic adults aged 20 and above were randomly selected and followed from 1999 to 2004. Fasting blood glucose including biophysical and anthropometric measures was measured. RESULTS: The overall 5 year cumulative incidence of diabetes was 16.4 per 1000 person-years and 65.1 per 1000 person-years in those with impaired fasting glucose adjusted for age and sex. Among obesity measures, only waist >85in. increased the risk for diabetes in males (RR=3.0). Relative changes stratified by loss in BMI and WC ≥5% or gain of BMI >15% from the baseline values for men were significantly associated with the incidental cases of diabetes. Increased hip circumference for men was significantly associated with a protective effect while an opposite association was observed for women. CONCLUSION: Relative change in both loss and excessive gain of BMI were risks for increased diabetes. Targeted intervention in those with impaired fasting blood glucose will expectedly reduce the incidental cases. Further investigations are needed for non obese related diabetes in Asian Indian subjects.

Pesticidal and pest repellency activities of rhizomes of Drynaria quercifolia (J. Smith) against Tribolium castaneum (Herbst)

BACKGROUND: Tribolium castaneum (Herbst) is a harmful pest of stored grain and flour-based products in tropical and subtropical region. In the present study, rhizome of Drynaria quercifolia (J. Smith) was evaluated for pesticidal and pest repellency activities against T. castaneum, using surface film method and filter paper disc method, respectively. In addition, activity of the isolated compound 3,4-dihydroxybenzoic acid was evaluated against the pest. RESULTS: Chloroform soluble fraction of ethanol extract of rhizome of D. quercifolia showed significant pesticidal activity at doses 0.88 to 1.77 mg/cm² and significant pest repellency activity at doses 0.94 to 0.23 mg/cm². No pesticidal and pest repellency activity was found for petroleum ether, ethyl acetate and methanol soluble fractions of ethanol extract as well as for 3,4-dihydroxybenzoic acid. CONCLUSION: Considering our findings it can be concluded that chloroform soluble fraction of rhizome of D. quercifoliais useful in controlling T. castaneum of stored grain and flour-based products.