Natural treasures from Picrorhiza kurrooa: a computational exploration of drug-like properties and bioactivity of kutkin, cucurbitacin, apocynin and lupanine

Background: To analyse and predict the basic pharmacokinetic and toxicological properties of four compounds of interest found in Picrorhiza kurroa (Kutkin, cucurbitacin, apocynin and lupanine) using computational bioinformatics tools. Methods: The chemical structures and molecular properties of the compounds were obtained from authentic sources and processed for data profiling. 2D structures were converted to 3D structures using ChemSketch software and PHASE module. In silico screening of the 3D structures was performed using bioinformatics prediction software to assess drug-likeness, absorption, blood-brain barrier penetration, enzyme interaction potential, skin penetration, and acute oral toxicity. Results: Kutkin exhibited poor drug-likeness and low oral absorption, while the other three compounds showed promising drug-like properties and good oral absorption. Cucurbitacin and lupanine were predicted to cross the blood-brain barrier, while Kutkin and Apocynin were not. None of the compounds were substrates for P-glycoprotein, but Kutkin and cucurbitacin were substrates for CYP3A4. All four compounds had low skin penetration. Acute oral toxicity varied, with cucurbitacin classified as highly toxic and the others as slightly toxic. Conclusions: Cucurbitacin, apocynin, and lupanine have potential for further development as therapeutic agents due to their favorable drug-like properties and good absorption. Kutkin's poor drug-likeness and low absorption make it less suitable for oral drug development. This information provides valuable insights for further research on the medicinal properties of Picrorhiza kurroa and the development of new drugs based on its active compounds.

Mechanistic insights into the analgesic and anti-inflammatory effects of alcoholic extracts from Curcuma longa

Background: Aim of the study was to scientifically validate the traditional Indian claims of Curcuma longa's (turmeric) antinociceptive (pain-relieving) and anti-inflammatory effects. Methods: The alcoholic extract of C. longa was tested in three rodent nociceptive models: acetic acid-induced writhing: examines visceral pain, formalin test: evaluates both acute and chronic neurogenic and inflammatory pain and tail immersion test to assess thermal pain. The extract's effects were compared to a control group and morphine (reference drug). Results: C. longa extract significantly reduced abdominal constrictions in the acetic acid test (59.36% inhibition). In the formalin test, the extract significantly decreased paw licking response time in both early (54.12% inhibition) and late phases (78.59% inhibition). C. longa extract significantly increased the tail flick reaction time in the immersion test, indicating pain relief. Conclusions: This study confirms the antinociceptive and anti-inflammatory activities of C. longa, providing scientific evidence for its traditional use in pain management.

Formulation, in vitro Characterization and Stability Studies of Fast Dispersing Tablets of Diclofenac Sodium.

The present study was aimed to formulate, develop and evaluate the fast dissolving tablets of diclofenac sodium, used for the treatment of arthritis, inflammation, pain. Fast dissolving tablets of diclofenac sodium were prepared by direct compression method using crospovidone and sodium starch glycolate as superdisintegrants in concentrations of 5.3%, 6.6% and 8% w/w and in combination. In this work microcrystalline cellulose and mannitol are investigated as diluents. Prepared powder mixtures were evaluated for drug excipient compatibility with FTIR spectroscopy and DSC analysis. Prepared formulations are evaluated for In vitro dissolution, disintegration dispersion and wetting time. Formulation FCS6 prepared with combination of crospovidone and sodium starch glycolate at weight ratio of 6.6 and 2.3% showed better results compare with control. Post compression parameters like hardness (3.4 kg/cm2) and friability (0.31%) are at good acceptable levels in accordance with official compendia. FCS6 showed improved dissolution (99.8 %) and dispersion (75 seconds) profiles compared to control. The FTIR and DSC showed no interaction between the drug and excipients. The optimized formula FCS6 showed good drug release characteristics with acceptable mouth feel and fast dissolving properties.