Posted by admin on Jul 31, 2019 in |
Though possessing a lot of ethnopharmacological use, Mimosa diplotricha did not explore thoroughly for its bioactivity & the phytoconstituents responsible for its bioactivity. The purpose of the current work was to conduct phytochemical screening and antinociceptive activity of methanolic extract and its different fractions of Mimosa diplotricha leaves. Phytochemical screening of methanolic extract revealed the presence of alkaloids, carbohydrates, saponins, glycosides, phytosterols, phenols, flavonoids, proteins and lipids in Mimosa diplotricha leaves. The antinociceptive activity was assessed by using acetic acid induced writhing method and tail immersion method at two different doses using Swiss-albino mice as an animal model. In the mice model the methanolic extract and its n-hexane fraction showed Significant peripheral-antinociceptive activity at a dose of 400 mg/kg body weight with percentage of inhibition of acetic acid-induced writhing 56.25% (P<0.001) and 51.62% (P<0.001) respectively compared to the standard diclofenac sodium (62.50%, P<0.001) group. The antinociceptive effect of methanolic extract and its n-hexane fraction of Mimosa diplotricha at the 400 mg/kg and 200mg/kg dose level was also found to...
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Posted by admin on Jul 31, 2019 in |
A series of new Schiff bases were synthesized by condensation of 3-(5-bromothiophen-2-yl)-1-(4-chlorophenyl)-1H-pyrazole-4-carbaldehyde with different aromatic aldehydes. The 3-(5-bromothiophen-2-yl)-1-(4-chlorophenyl)-1H-pyrazole-4-carbaldehyde was prepared from 1-(1-(5-bromothiophen-2-yl)ethylidene)-2-(4-chlorophenyl)hydrazine by the Vilsmeier Haack reaction. The 1-(1-(5-bromothiophen-2-yl)ethylidene)-2-(4-chlorophenyl) hydrazine was prepared by the condensation reaction of 2-acetyl-5-bromothiophene with 4-chlorophynylhydrazine hydrochloride. The structures of newly synthesized compounds were elucidated by NMR, IR, and Mass spectral – data. Prepared Schiff bases were evaluated for antibacterial activity against four organisms: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumoniae using streptomycin as a standard drug. Agar well-diffusion method was followed to determine the antimicrobial activity. All prepared Schiff bases showed poor to good activity against test organisms. Based on the zone of inhibition results, it is observed that the newly prepared Schiff bases showed better activity against Klebsiella pneumoniae than Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Schiff base 4c showed good activity against Pseudomonas aeruginosa, Schiff base 4l showed good activity against Staphylococcus aureus and all the Schiff bases 4a-4l except 4c showed good activities against Klebsiella...
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Posted by admin on Jul 31, 2019 in |
Objective: The Failure in chemotherapy is mainly because of the resistance of the chemotherapeutic drugs towards the neoplastic cells. The main reason behind this study was to develop a novel combination of 5-Fluorouracil (5-FU) lipid curcumin conjugates for the treatment of cancer. Methods: In this study, the lipid group stearic acid and oleic acid was conjugated with the parent drug moiety 5-Fluorouracil to acquire lipophilicity. The next step involves the conjugation of curcumin with 5-Fluorouracil lipid to form a lipid dual drug conjugate. The characterization of conjugates followed the synthesis part by using FT-IR, DSC, and LCMS. The conjugates hence obtained were further carried for formulation aspect. After the successful completion of the formulation part, in-vitro studies and MTT Assay was performed. Results: The results depict the successful synthesis of the conjugates, and its characterization was successfully done. The conjugates are formulated into Self Nanomulsifying drug delivery system (SNEDDS). The results obtained from the MTT assay also shown a significant cytotoxic effect in both the conjugation. Conclusion: The in-vitro...
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Posted by admin on Jul 31, 2019 in |
Degradation studies are important to know the potentials degradation products and to develop a stability indicating method. Ranolazine active pharmaceutical ingredients subjected to in detailed forced degradation study using several stressing agents (HCl, NaOH, H2O2). Degradation products of Ranolazine under hydrolytic and oxidative stress conditions were identified, and their stabilities were assessed. Three degradation products were formed when the drug was subjected to acid stress and two products were formed in oxidative stress condition. Ranolazine was stable to base hydrolysis. The degradants were separated on a C-8 column employing preparative HPLC using gradient elution. The structures of all the five degradation products (DP-1, DP-2, DP-3, DP-OX1, and DP-OX2) were established by extensive 1D (1H, 13C) and 2D (COSY, HSQC and HMBC) NMR spectroscopic studies and mass spectra. The products were identified as 2-(4-(2-hydroxy-3-(2-hydroxyphenoxy) propyl) piperazine-1-yl) acetic acid (DP-1), 2-(4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine-1-yl) acetic acid (DP-2), N-(2,6-dimethylphenyl)-2 -(4-(2-hydroxy-3 (2-hydroxyphenoxy) propyl) piperazine-1-yl) acetamide (DP-3), 1-(2-((2,6-dimethylphenyl)amino)-2oxoethyl)-4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1, 4-dioxide (DP-OX1), 4-(2-((2, 6 dimethyl phenyl) amino)-2-oxoethyl)-1-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1-oxide (DP-OX2)....
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Posted by admin on Jul 31, 2019 in |
A novel synthesis of N-(2, 4′-dioxo-1, 2-dihydro-3′H-spiro [indole-3, 2′-[1, 3] thiazolidin]-3′-yl)-2 -hydroxybenzamide derivatives were synthesized by cyclization of isatin hydrazones with thioglycolic acid. The synthesized compounds were characterized by spectral data (IR, 1H-NMR, Mass) and evaluated for antibacterial activity against various strains of bacteria at the concentrations of 200 µg/ml. Among the tested compounds X(i) is highly active against E. coli, X(f) is active against B. subtilis, X(h) is active against S. aureus and X(c) is active against S....
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