Posted by admin on Feb 29, 2024 in |
Aegle marmelos L. (Bael Fruit) is rich in bioactive compounds such as coumarins, alkaloids, terpenoids, tannins, flavonoids, and essential oils. This article focused on the pharmacokinetic profiling of coumarins present using an in silico ADME tool called SwissADME which contributes to a better understanding of enhanced drug monitoring and individualization of drug therapy. Log S (ESOL), Log S (Ali), and Log S (SILICOS-IT) values of umbelliferon, scopoletin, scoparone, xanthotoxol, and marmesin show that they are soluble in water which shows they have good absorption and excretion properties. Lipophilicity data shows that all coumarins can penetrate through the blood-brain barrier (BBB) except marmin, while marmesin and marmin have good oral bioavailability. These coumarins can inhibit the CYP1A2, CYP2C19, and CYP2C9 except CYP2D6, and CYP3A4 isoenzymes. This data helps to select leads for further drug discovery and...
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Posted by admin on Feb 29, 2024 in |
Background: Sinigrin (allyl-glucosinolate or 2-propenyl-glucosinolate), an aliphatic glucosinolate, is naturally present in Brassicaceae plants, while carvacrol (2-methyl-5-isopropylphenol) is a monoterpene phenolic component of the essential oil generated by many aromatic plants. This study is aimed to determine the hepatoprotective potential of these phytoconstituents on Paracetamol-induced liver damage in Wistar rats. Methods: Seven groups of six Wistar rats, each weighing between 180 and 230 g, were selected. The animals’ weight range was evenly divided throughout the groups. The control group, group I, got normal saline; the PCM group, group II, received paracetamol (3 g/kg, p.o.); groups III and IV, carvacrol (25, 50 mg/kg/p.o.); and the groups V and VI, sinigrin (25, 50 mg/kg/p.o.) once daily for 14 days. Silymarin was given daily to group VII- Standard at a dose of 25 mg/kg p.o. Result: Serum samples were used to determine levels of marker enzymes such as aspartate transaminases (AST), alanine transaminases, lactate dehydrogenase (LDH), alkaline phosphatase (ALP), and glutamyl transpeptidase (GGT). The proinflammatory cytokines interleukin-1beta (IL-1b) and interleukin-6 (IL-6) as...
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Posted by admin on Feb 29, 2024 in |
Phytochemicals are intensively addressed for clinical uses, and nanostructured phytochemical delivery vehicles are on the limelight. A viable potential treatment for neurological disorders is resveratrol. In the current investigation, we sought to create a nanoemulsion containing resveratrol utilising the response surface methodology. Using Neem oil, Pluronic-f 68, and Tween 80, the effects of the formulation and probe sonication processing parameters were analysed even during nanoemulsification process. As process factors, the duration of probe sonication has been preferred. The concentrations of oil and surfactant, along with their intensity, were revealed have a significant influence on globule size. The optimum nanoemulsion formulation constituted 2.6442 mg/ml of resveratrol. The responses picked were globule size, PDI, and zeta potential. The optimised RES-nanoemulsion had a globule size of 179 3.4 nm, a PDI of 0.175, a zeta potential of 29.9 2.1 mV, and an entrapment efficiency of RES-NEs of 96.47 2.3%. The in vitro drug release in pH 6.8 phosphate buffer displayed the nanoemulsion formulation’s superiority. The results indicate that resveratrol nanoemulsion can be...
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Posted by admin on Feb 29, 2024 in |
The Siddha medicine system, predominantly practiced in South India, encompasses a diverse range of medicinal formulations. Among them, Pancha Moola Kudineer Chooranam (PMKC) from the Therayar Maha Karisal literature is claimed to be effective against ulcers. Helicobacter pylori, causes gastric and duodenal ulcers through various transmission routes. It colonizes the duodenal epithelial cells, leading to gastritis, gastric atrophy, and potentially gastric carcinoma. This study provided valuable insights on the potential anti-ulcer activity of root extracts of the formulation PMKC, which includes Glycyrrhiza glabra, Chukrasia tabularis, Terminalia chebula, Terminalia bellirica, and Phyllanthus emblica against Helicobacter pylori through molecular docking. Eight bioactive compounds were identified which underwent docking calculations. The results indicated that these phytochemicals interacted with the active amino acid residues of H. pylori urease, suggesting potential inhibitory effects on the enzyme. Among the compounds tested, Glycyrrhizin demonstrated the highest inhibition against H. pylori urease, followed by Gallic acid. Maslinic acid and Chuktabrin showed minimal inhibition. In conclusion, the active components of PMKC exhibited significant binding affinity to H. pylori...
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Posted by admin on Jan 31, 2024 in |
Cancer is a complex and life-threatening disease characterized by abnormal cell growth. Several AAA+ ATPases are involved in the oncogenic pathways, however, the role of an ATPase protein i.e. N-ethylmaleimaide-Sensitive Factor (NSF) was unclear. Therefore, we performed systematic bioinformatics analysis to predict the prospect of NSF as a cancer biomarker. NSF is found to be upregulated in some cancers whereas down regulated in others. Additionally, this expression was found to be associated with the reduced survival rate of cancer patients. We investigated NFS’s mutation and copy number amplification status across the cancers since the genetic alteration is a major cause of cancer. Several hotspot mutation sites were observed at the ATPase domain of NSF indicating that these mutations might have a role in carcinogenesis. Additionally, the copy number amplification study revealed a high amplification percentage of NSF across the cancers. We further focused on the functional characteristics of NSF across cancers. Fascinatingly, we found many interacting protein partners of NSF that are key in carcinogenesis. We further focused on the probable oncogenic...
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