Posted by admin on Nov 30, 2022 in |
Heterocyclic chemistry has grown very rapidly, particularly in evaluating synthetic methods and investigating synthesized materials’ bioactive properties. Heterocycle compounds are important in many facets of life’s pharmacological activities. In their structure, many biologically active compounds such as amino acids, vitamins, hormones, nucleic acids, alkaloids, dyes, and drugs (natural and synthetic) possess heterocyclic ring molecules. Various pyrazole derivatives and their numerous physiological and pharmacological effects have been the subject of numerous investigations during the last decade. Part of the goal of these investigations was to uncover the vast spectrum of drug-like properties of pyrazole derivatives and their structure-activity connections to unlock the full potential of these molecules. This article focuses on the chemistry and pharmaceutic activity of the heterocycle pyrazoline, i.e., nitrogen-containing five-membered ring. An account of a different mode of synthesis from different starting materials is shown, along with the highlights of the therapeutic activity of...
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Posted by admin on Nov 30, 2022 in |
Introduction: Coumarins are secondary metabolites widely spread in nature. Due to their broad pharmacological activities, many natural and synthetic coumarins and more complex related derivatives are of interest. The coumarin is extremely variable in structure due to the various types of substitutions in their basic structure, influencing their biological activity. Metal complexes of coumarins obtained revealed higher biological activity than their ligand. Metal complexes play a vital role as chemotherapeutic agents. Methods: 7-amino-4-methylcoumarin refluxed with substituted aromatic aldehydes in absolute alcohol in presence of acetic anhydride and was washed with cold water to give Schiff bases of 7-amino-4-methylcoumarin (4a-4j). Further, the metal complexes of coumarin Schiff base (5a-5j) were synthesized by dissolving both Schiff base of 7-amino-4-methylcoumarin and metal sulphates in methanol and are stirred at 250C with dropwise addition of a dil. ammonia. Result and Conclusion: Screening the copper metal complexes against breast cancer cell line (MDA MB 231) with standard Paclitaxel using MTT assay method. The synthesized metal complexes show anticancer activity in a concentration-dependent manner. The...
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Posted by admin on Nov 30, 2022 in |
The current research is an attempt to investigate the antibacterial and synergistic bioefficacy of Curcuma caesia (Roxb.) versus human pathogenic bacteria viz., Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumonia, Pseudomonas aeruginosa and Proteus vulgaris procured from IMTECH, Chandigarh, India. Agar well diffusion assay was performed, and one-way ANOVA examined the outcome. The qualitative phytochemical examination revealed a positive test for flavonoids, glycosides, phytosterols, resins, saponins, and tannins. However, the quantitative estimation of phytochemicals revealed that the root sample contains highest amount of flavonoid followed by total phenol, saponin and alkaloid. The bioactive extract was purified using column chromatography. The purified fraction and commercially available antibacterials viz., tetracycline, streptomycin, and penicillin was evaluated for their synergistic or antagonistic efficacy counter to multi-drug resistant human pathogenic bacteria. The outcome divulge that a purified fraction of C. caesia was found to act synergistically with tetracycline against all the bacterial cultures under investigation. The results with streptomycin showed maximum synergistic activity against B. cereus. However, penicillin and purified...
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Posted by admin on Nov 30, 2022 in |
Background: In the present investigation Antineoplastic loaded transdermal patch was formulated using Liposomes, eudragit-RL, hydroxypropyl methyl cellulose K-50, and ethyl cellulose. Materials and Methods: Liposomes were formulated by solvent evaporation method using poly (sebacic acid-co-ricinoleic acid) in varying ratios and evaluated for particle size, drug loading, entrapment efficiency, transmission electron microscopy, differential scanning calorimetry and X-ray diffraction. Formulated tamoxifen-loaded liposomes were finally incorporated into transdermal patch and evaluated for thickness drug content, moisture content, moisture uptake, folding endurance, tensile strength diffusion coefficient, permeability coefficient, in-vitro permeation, and skin irritation. Optimized transdermal patches were tested for its pharmacokinetic and pharmacodynamics parameters. Results: Formulated transdermal patches showed improved bioavailability of tamoxifen when compared to its oral route. Conclusion: Tamoxifen-loaded liposomal transdermal patches could serve as a better alternative to existing marketed formulation in terms of...
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Posted by admin on Nov 30, 2022 in |
Background: Depression is a state of mental illness characterized by long-lasting moods of desolation. Typical to atypical antidepressants are available in modern medicine for depression therapy, but the side effects are still questionable. Aqueous extract of Abelmoschus esculentus seeds (AEAES) from the Okra has been chosen for the study. AEAES has already been shown to exhibit an antidepressant-like effect, but there is no information about its mechanism. The current study has studied the monoaminergic and opioid systems’ involvement in the antidepressant effect of AEAES. Methods: The current study has shown the signal for the role of nor-adrenergic and serotonergic systems in the antidepressant activity of AEAES in mice using the Forced swim test (FST). Swiss Albino female mice were treated with vehicle AEAES (200 mg/kg) orally, and different types of receptor antagonists were used to demonstrate the mechanism of action of an AEAES. Results: The antidepressant action exhibited by AEAES was obliterated by the pre-treatment of mice with p-chlorophenylalanine (100 mg/kg, i.p., serotonin synthesis inhibitor), Ketanserin (5 mg/kg, i.p.,...
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