Comparative Phytochemical Screening and In vitro Evaluation of Biological Activities between Aqueous and Ethanolic Extract of Momordica charantia L. Fruits.

Aims: The study was conducted to compare the presence of different phytochemicals and biological activities like cytotoxicity, anthelmintic activity, antioxidant and free radical scavenging activities between aqueous and ethanolic extract of Momordica charantia L. Fruits. Methodology: The cytotoxic assay was undertaken using brine shrimp lethality test (BSLT) while the anthelmintic activity was carried out with the determination of time of paralysis and death of earthworm (Pheritima posthuma) at five different concentrations. Antioxidant and free radical scavenging activities were measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and determining the total phenolic contents. Results: Study revealed that several phytochemicals were found common for both of the extracts, though proteins and amino acids were only found in ethanolic extract. Both the extracts showed mild cytotoxic activity where the ethanolic extract showed better potency (LC50=24.245 μg/ml) than aqueous extract (LC50=24.515 μg/ml). In case of anthelmintic activity, ethanolic extract was also found significantly potent than aqueous extract at five different concentrations. IC50 values for the total antioxidant activity were 304.41±0.903 μg/ml and 479.05±1.393 μg/ml for ethanolic and aqueous extract, respectively. Ethanolic extract contained a significantly higher concentration of total phenols (71.08 ± 0.380 mg of GAE/g of extract) in comparison to aqueous extract (57.33±0.520 mg of GAE/g of extract). Conclusion: Therefore, in all aspects of the study, ethanolic extract was found more potent than aqueous extract. It can be concluded that M. charantia fruits are abundant of various phytochemicals and possess versatile biological activities.

In vivo analgesic, antipyretic, and anti-inflammatory potential in Swiss albino mice and in vitro thrombolytic activity of hydroalcoholic extract from Litsea glutinosaleaves

BACKGROUND: The study was conducted to evaluate the in vitro thrombolytic activity, and in vivo analgesic, anti-inflammatory and antipyretic potentials of different hydrocarbon soluble extracts of Litsea glutinosaleaves for the first time widely used in the folkloric treatments in Bangladesh. This work aimed to create new insights on the fundamental mechanisms of the plant extracts involved in these activities. RESULTS: In thrombolytic activity assay, a significant clot disruption was observed at dose of 1 mg/mL for each of the extracts (volume 100 µL) when compared to the standard drug streptokinase. The n-hexane, ethyl acetate, chloroform, and crude methanolic extracts showed 32.23 ± 0.26, 37.67 ± 1.31, 43.13 ± 0.85, and 46.78 ± 0.9% clot lysis, respectively, whereas the positive control streptokinase showed 93.35 ± 0.35% disruption at the dose of 30,000 I.U. In hot plate method, the highest pain inhibitory activity was found at a dose of 500 mg/kg of crude extract (15.54 ± 0.37 sec) which differed significantly (P <0.01 and P <0.001) with that of the standard drug ketorolac (16.38 ± 0.27 sec). In acetic acid induced writhing test, the crude methanolic extract showed significant (P <0.01 and P <0.001) analgesic potential at doses 250 and 500 mg/kg body weight (45.98 and 56.32% inhibition, respectively), where ketorolac showed 64.36% inhibition. In anti-inflammatory activity test, the crude methanolic extract showed significant (P <0.001) potential at doses 250 and 500 mg/kg body weight (1.51 ± 0.04 and 1.47 ± 0.03 mm paw edema, respectively), where ketorolac showed 1.64 ± 0.05 mm edema after 3 h of carrageenan injection. In antipyretic activity assay, the crude extract showed notable reduction in body temperature (32.78 ± 0.46°C) at dose of 500 mg/kg-body weight, when the standard (at dose 150 mg/kg-body weight) exerted 33.32 ± 0.67°C temperature after 3 h of administration. CONCLUSIONS: Our results yield that the crude hydroalcoholic extract has better effects than the other in all trials. In the context, it can be said that the leaves of L. glutinosa possess remarkable pharmacological effects, and justify its traditional use as analgesic, antipyretic, anti-inflammatory, and thrombolytic agent.

In vivo antipyretic, antiemetic, in vitro membrane stabilization, antimicrobial, and cytotoxic activities of different extracts from Spilanthes paniculata leaves

BACKGROUND: The study was conducted to evaluate the in vitro antimicrobial activity, cytotoxic, and membrane stabilization activities, and in vivo antiemetic and antipyretic potentials of ethanolic extract, n-hexane and ethyl acetate soluble fractions of Spilanthes paniculata leaves for the first time widely used in the traditional treatments in Bangladesh. RESULTS: In antipyretic activity assay, a significant reduction (P < 0.05) was observed in the temperature in the mice tested. At dose 400 mg/kg-body weight, the n-hexane soluble fraction showed the effect (36.7 ± 0.63°C ) as like as the standard (dose 150 mg/kg-body weight) after 5 h of administration. Extracts showed significant (P < 0.001) potential when tested for the antiemetic activity compared to the standard, metoclopramide. At dose 50 mg/kg-body weight, the standard showed 67.23% inhibition, whereas n-hexane and ethyl acetate soluble fractions showed 37.53% and 24.93% inhibition of emesis respectively at dose 400 mg/kg-body weight. In antimicrobial activity assay, the n-hexane soluble fraction (400 µg/disc) showed salient activity against the tested organisms. It exerts highest activity against Salmonella typhi (16.9 mm zone of inhibition); besides, crude, and ethyl acetate extracts showed resistance to Bacillus cereus and Bacillus subtilis, and Vibrio cholera respectively. All the extracts were tested for lysis of the erythrocytes. At the concentration of 1mg/ml, ethanol extract, and n-hexane and ethyl acetate soluble fractions significantly inhibited hypotonic solution induced lysis of the human red blood cell (HRBC) (27.406 ± 3.57, 46.034 ± 3.251, and 30.72 ± 5.679% respectively); where standard drug acetylsalicylic acid (concentration 0.1 mg/ml) showed 77.276 ± 0.321% inhibition. In case of heat induced HRBC hemolysis, the plant extracts also showed significant activity (34.21 ± 4.72, 21.81 ± 3.08, and 27.62 ± 8.79% inhibition respectively). In the brine shrimp lethality bioassay, the n-hexane fraction showed potent (LC50 value 48.978 µg/ml) activity, whereas ethyl acetate fraction showed mild (LC50 value 216.77 µg/ml) cytotoxic activity. CONCLUSIONS: Our results showed that the n-hexane extract has better effects than the other in all trials. In the context, it can be said that the leaves of S. paniculata possess remarkable pharmacological effects, and justify its folkloric use as antimicrobial, antipyretic, anti-inflammatory, and antiemetic agent. Therefore, further research may be suggested to find possible mode of action of the plant part.

Development and evaluation of Methocel K15M based Theophylline floating tablets.

The purpose of the investigation highlights the formulation and optimization of floating tablets containing theophylline as a model drug. Formulations were optimized for different concentrations of cetyl alcohol, citrc acid and methocel K15M by direct compression method. The dissolution study of the tablet matrices of 9 different formulations were carried out in 0.1N HCl as the medium (pH 1.3) for 8 hours using USP type II dissolution apparatus. It was observed the floating lag time for the tablet was 30 seconds and the total floating time was more than 8 hours. The drug release pattern was simulated in different kinetic orders such as Zero Order, First Order, Higuchi, and Korsmeyer release kinetic model. From the study, we observed that Higuchi release kinetics was predominant over other release kinetics and diffusion was the drug release mechanism from the matrices. Korsmeyer-Peppas release kinetics suggests that formulation F3, F4 and F9 followed Fickian type release mechanism whereas formulation F1, F2, F5, F6, F7 and F8 followed Non-Fickian type release mechanism. Thus, it is possible to design theophylline loaded Methocel K15M sustained release matrix tablets with desirable release characteristics by judicious and critical combination of Methocel K15M with other hydrophilic materials.

Evaluation of total phenolic content, free radical scavenging activity and phytochemical screening of different extracts of Averrhoa bilimbi (fruits).

The present study was designed to investigate the phytochemical screening, the free radical scavenging activity and to determine the total phenolic content of methanolic extract and different solvent soluble fractions of Averrhoa bilimbi Linn. (Oxalidiaceae) fruits. The free radical scavenging activity was evaluated by analyzing the bleaching rate of 1,1-diphenyl-2-picrylhydrazyl (DPPH), and total phenolic content was determined by using Folin-Ciocalteau reagent, which results were expressed in gallic acid equivalent (mg of GAE/g of sample). The phytochemical screening revealed the potent source of different phytochemical constituents on different extractives including, phenol, flavonoid, tannin that are responsible for antioxidant action. In the determination of total phenolic content, different extractives showed a significant content of phenolic compounds ranging from 50.23-68.67 mg of GAE/g of extractive. The plant sample displayed significant DPPH free radical scavenging activity with highest IC50 value in crude methanolic extract (30.365 μg/ml) followed by chloroform, carbon tetrachloride, pet-ether and aqueous soluble fractions having value of 32.852 μg/ml, 36.708 μg/ml, 50.35 μg/ml, and 79.918 μg/ml, respectively as opposed to that of the scavenging effects of BHT of 19.656 μg/ml.

Evaluation of total phenolic content, free radical scavenging activity and phytochemical screening of different extracts of Averrhoa bilimbi (fruits).

The present study was designed to investigate the phytochemical screening, the free radical scavenging activity and to determine the total phenolic content of methanolic extract and different solvent soluble fractions of Averrhoa bilimbi Linn. (Oxalidiaceae) fruits. The free radical scavenging activity was evaluated by analyzing the bleaching rate of 1,1-diphenyl-2-picrylhydrazyl (DPPH), and total phenolic content was determined by using Folin-Ciocalteau reagent, which results were expressed in gallic acid equivalent (mg of GAE/g of sample). The phytochemical screening revealed the potent source of different phytochemical constituents on different extractives including, phenol, flavonoid, tannin that are responsible for antioxidant action. In the determination of total phenolic content, different extractives showed a significant content of phenolic compounds ranging from 50.23-68.67 mg of GAE/g of extractive. The plant sample displayed significant DPPH free radical scavenging activity with highest IC50 value in crude methanolic extract (30.365 μg/ml) followed by chloroform, carbon tetrachloride, pet-ether and aqueous soluble fractions having value of 32.852 μg/ml, 36.708 μg/ml, 50.35 μg/ml, and 79.918 μg/ml, respectively as opposed to that of the scavenging effects of BHT of 19.656 μg/ml.

Antimicrobial and Cytotoxic Activity of the Methanol Extract of Paederia foetida Linn. (Rubiaceae).

The antibacterial activities of n-hexane, chloroform, ethyl acetate fractions of methanolic extracts of the whole plants Paederia foetida (family Rubiaceae) were screened against various pathogenic bacteria such as Bacillus cereus, Bacillus megaterium, Bacillus subtilis, Staphylococcus aureus, Sarcina lutea, Escherichia coli, Pseudomonas aeruginosa, Salmonella paratyphi , Salmonella typhi, Shigella boydii, Shigella dysenteriae, Vibrio mimicus, Vibrio parahemolyticus, Candida albicans, Aspergillus niger, Sacharomyces cerevacae by ‘disc diffusion method’. The methanol extract of the whole plants possesses no antimicrobial activity but the ethyl acetate, chloroform and n-hexane fractions exhibited moderate to less activity against some organisms tested compared with the standard antibiotic Kanamycin. Brine shrimp lethality bio-assay was done using brine shrimp Nauplii and dimethyl sulfoxide as a solvent for the methanol plant extracts of Paederia foetida. The LC50 value of methanol extract of the plant indicated that the cytotoxicity was very significant.

Development and Validation of RP-HPLC Method for the Simultaneous Estimation of Domperidone and Naproxen in Tablet Dosage Form.

A simple, selective and rapid reversed phase High Performance Liquid Chromatographic (RP-HPLC) method has been developed and validated for the simultaneous analysis of domperidone and naproxen in tablet dosage form. The chromatographic system consisted of two LC-20 AT pump, SPD-20A UV detector, SIL-20A auto-sampler and CTO- 10ASVP column oven. Chromatographic separation of drugs was achieved on an Shim-Pack C18 column (250 mm x 4.6 mm, 5 μm) as stationary phase with a mobile phase comprising of phosphate buffer (pH adjusted to 3.00 with sodium hydroxide): methanol in the ratio 30:70 (v/v) at a flow rate of 1.0 ml/min with UV detection at 280 nm. Retention time was 3.17 minutes for domperidone and 5.42 minutes for naproxen. The method was found selective and peaks of domperidone and naproxen were well separated (resolution 10.72). The proposed method is linear (r2 = 0.999 for domperidone and naproxen), accurate with 99.5% recovery for domperidone and 99.39% recovery for naproxen and precise (%RSD < 1%). The method has been used to determine potency of commercial product and potency was found within limit. The method can be used for the analysis of domperidone and naproxen in tablet dosage form.