THERAPEUTIC POTENTIAL AND IN VITRO ANTHELMINTIC ACTIVITY OF RIDGE GOURD FRUIT

Objective: The objective of the study was to evaluate the therapeutic potential and in vitro anthelmintic activity of ridge gourd fruit (Luffa acutangula) against Indian earthworms. Methods: For anthelmintic activity against Indian earthworms (Pheretima posthuma, Ascaridia galli, and Raillietina spiralis), various different extracts concentration of L. acutangula fruit have been taken. Five concentrations as 10, 20, 30, 40, and 50 mg/ml of various extracts were tested and results were expressed in terms of time for paralysis and time for the death of worms. Albendazole (20 mg/ml) was used as reference standard and water (0.5%) as a control group. Results: Preliminary phytochemical screening of the different extracts of ridge gourd fruit was shown to produce anthelmintic activities. In the present study, it was observed that all the extracts of ridge gourd fruit have exhibited a positive response to a certain degree of anthelmintic activity. Ethyl acetate extract exhibited more potent activity at the lower concentration of 10 mg/mL against A. galli (Roundworm). The anthelmintic activity of L. acutangula fruit extract has, therefore, been demonstrated

Synthesis, molecular docking, and apoptogenic efficacy of novel N-heterocycle analogs to target B-cell lymphoma 2/X-linked inhibitors of apoptosis proteins to regress melanoma

The novel series of piperidine conjugated benzophenone analogs with amide link 11a–l were synthesized in a multistep process. The structures of these compounds were confirmed by IR, 1H, 13C, NMR, and mass spectra and also by elemental analyses. The newly synthesized molecules were screened for selectivity against cancers of different origin through cell based assay system using B16F10, A375, A549, HepG2, ACHN, and MCF7 cells. The results postulated that compound 11f with two bromo groups at the para position in rings A and E and two methyl groups at ortho position in rings B and D evokes target specific action against melanoma highlighting the importance of substituted groups. Down the line studies further inferred compound 11f evokes the apoptotic cellular event leading to cell death. Investigation of eventual mechanism revealed that compound 11f turned out to be a dual inhibitor of B-cell lymphoma-2 and X-linked inhibitors of apoptosis causing the up regulation of Bax and Bad. Further, the antiproliferative effects were mimicked in murine melanoma with similar mechanisms. Molecular docking experiments further confirmed that compound 11f possessed a superior affinity for of B-cell lymphoma-2 and X-linked inhibitors of apoptosis through strong hydrogen bonds. The study implies the identification of compound 11f with selective target against melanoma by inducing apoptogenic effect, which could be the future hope for the treatment of skin cancer

Synthesis of 2-(2-aroylaryloxy)methyl-oxazolines as potent analgesic and anti-inflammatory agents

The synthetic strategies and characterization of some novel benzophenone derivatives carrying oxazoline ring are described using microwave irradiation technique. The compounds 2a-h, 3a-h and 4a-h were screened for their analgesic, anti-inflammatory, ulcerogenic, cyclooxygenase activities and acute toxicity. The results revealed that halo compounds 4a (48.3%), 4c (45.4%) and 4f (40.2%) displayed significant anti-inflammatory activity with low ulcerogenic activity in comparison with that of the standard drugs, aspirin (35.3%) and phenyl butazone (35.5%

Synthesis, characterization, crystal structure and Hirshfeld surface analysis of ethyl 2-(2-oxo-2H-chromen-4-yloxy) acetate

The title compound ethyl 2-(2-oxo-2H-chromen-4-yloxy) acetate has been synthesized and characterized by NMR, IR and mass spectral studies, and finally the structure was confirmed by single crystal X-ray diffraction studies. The title compound C13H12O5 crystallizes in the orthorhombic space group P212121 with a single molecule in the asymmetric unit and the unit cell parameters, a = 5.1037(7) Å, b = 7.9867(10) Å, c = 28.300(4) Å, and Z= 4. The crystal structure of the title compound exhibit several C–H •••O intermolecular interactions resulting in a three dimensional architecture. Further, the Hirshfeld surface analysis reveals the nature of intermolecular contacts. The fingerprint plot provides the information about the percentage contribution which clearly states that H…H (37.4) bonding appears to be a major contributor in the crystal packing, whereas the O…H (33.2), C…H (20.2) from the intermolecular contacts to the surface

IN VITRO EVALUATION OF HYPOLIPIDEMIC EFFECT OF EXTRACTS OF MEDICINAL DRACAENA CINNABARI BALF. F. RESIN: In vitro evaluation of hypolipidemic effect

Objective: The objective of the study was to in vitro evaluate of hypolipidemic effect of extracts of medicinal Dracaena cinnabari Balf. f. resin. Methods: About 800 g of dry powder of the resin of dracaena cinnabar was taken in a Soxhlet apparatus and subjected for sequential extraction of solvents from non-polar to polar end (hexane, benzene, diethyl ether, dichloromethane, chloroform, ethyl acetate, acetone, ethanol, methanol, and water); the extract samples were kept at 4°C for further assays. All the extracts were subjected to glucose uptake assay. Results: The ethanol extract showed significant (p<0.05) hypolipidemic effect by decreasing the activity of enzyme such as significant reduction in the pancreatic lipase enzyme, malic dehydrogenase enzyme, and glucose-6-phosphate dehydrogenase enzyme with IC50~13, ~13, and ~14, respectively. This results were similar to the standard drug atorvastatin with IC50~12, ~16, and ~17, respectively. Ethanol extract exhibited significant atherogenic index and percentage protection against hyperlipidemia. The potential biological activity of ethanol extract may be attributed to the highest polarity which needs further investigation

Synthesis, characterization, crystal structure and Hirshfeld surface analysis of o-tolyloxy acetic acid (1H-indol-3-yl-methylene)-hydrazide

o-Tolyloxy acetic acid (1H-indol-3-yl-methylene)-hydrazide was synthesized by treating 2-methyl phenoxy acetic acid hydrazide with indole carboxaldehyde. It was characterized by NMR, IR studies and mass spectral studies and finally, the structure was confirmed by single crystal X-ray diffraction studies. The title compound C18H17N3O2 crystallizes in the monoclinic crystal system in the space group P21/n. The intermolecular interactions in the crystal structures are quantified using the Hirshfeld surface analysis method. The majority contribution to the Hirshfeld surfaces is from H⋯H (45.4) contacts

Analysis of antimicrobial data of 2-aryloxy methyl oxazoline analogues using ANOVA

Antibacterial and antifungal agents are widely used in the management of infectious disease but most of them have developed resistance to micro-organism. To overcome this problem and to lower the side effects, many approaches can be utilized. In this article, the mode of action of antimicrobial agents and their mechanisms of resistance is discussed by synthesized different oxazoline analogues (3a-n). The series was evaluated for antimicrobial and antifungal activity to calculate zone of inhibition fallowed by MIC value of some selected compounds which show more zone of inhibition. Further, One Way Analysis of Variance (ANOVA) followed by Duncan multiple range test for pair-wise comparison is used to study the significant different in mode of action of different antifungal and antibacterial activities resistance data to different bacteria and fungi, (3a-n). The test revealed that compound 3e with a chloro group at ortho position in phenyl ring was found to be more potent among the series 3a-n. The results showed that synthesized compound 3e might be a potential antibacterial agent in near future

Structural elucidation, synthesis, characterization and hirshfeld surface analysis of ethyl 2-(2-bromophenoxy)acetate

The title compound, ethyl 2-(2-bromophenoxy)acetate was synthesized in good yield by refluxing O-bromophenol with ethyl chloroacetate in the presence of K2CO3 in anhydrous acetone. The product obtained was characterized by spectroscopic techniques and finally the structure was confirmed by X-ray diffraction studies. The compound crystallizes in the monoclinic crystal system with the space group P21/n with unit cell parameters a = 5.3473(3) Å, b = 26.7605(15) Å, c = 7.9862(5) Å, β = 107.796(4)o and Z=4. The crystal packing exhibits intermolecular C—H...O hydrogen bonds forming a infinite linear chain propagating along [100] direction with graph set notation C(4). Hirshfeld surface analysis for visually analyzing intermolecular interactions in crystal structures employing molecular surface contours and 2D fingerprint plots have been used to examine molecular shape

Statistical analysis of antimicrobial data of 2-[2-(aroyl) aroyloxy]methyl1, 3, 4 oxadiazoles analogues using ANOVA

Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic molecules containing nitrogen and oxygen (like oxadiazole ring system) have shown most potent biological activities. Microorganisms are strictly attendant with the fitness and well-being of human beings. The present treatments of bacterial and fungal infections are a bit unsatisfactory, owing to rapidly developing drug resistance and side effects. The improved of antibacterial and antifungal agents results in resistant to drugs. A series of substituted Oxadiazoles analogues 4a-jwere synthesized and screened for their antibacterial and antifungal activities to evaluate zone of inhibition. The significant effect ofin-vitroantimicrobial and antifungal activities of compounds 4a-jwere studied using one way ANOVA. It was shown that the variables 4a-j series weresignificant. Further pairwise comparison of significant differences between the variables were analyzed using Tukey HSD. The data revels that compound 4a with 2-methyl and 3chloro group in phenyl and benzoyl ring respectively, have shown excellent activity and more potent among the 4a-j series