Exploring the Antibacterial Potential of Semisynthetic Phytocannabinoid: Tetrahydrocannabidiol (THCBD) as a Potential Antibacterial Agent against Sensitive and Resistant Strains of Staphylococcus aureus.

Antimicrobial resistance (AMR) is one of the most challenging problems and is responsible for millions of deaths every year. We therefore urgently require new chemical entities with novel mechanisms of action. Phytocannabinoids have been adequately reported for the antimicrobial effect but not seriously pursued because of either stringent regulatory issues or poor drug-like properties. In this regard, the current work demonstrated the antibacterial potential of tetrahydrocannabidiol (THCBD, 4), a semisynthetic phytocannabinoid, against Staphylococcus aureus, the second-most widespread bug recognized by the WHO. THCBD (4) was generated from cannabidiol and subjected to extensive antibacterial screening. In in vitro studies, THCBD (4) demonstrated a potent MIC of 0.25 µg/mL against Gram-positive bacteria, S. aureus ATCC-29213. It is interesting to note that THCBD (4) has demonstrated strong effectiveness against efflux pump-overexpressing (SA-1199B, SA-K2191, SA-K2192, and Mupr-1) and multidrug-resistant (MRSA-15187) S. aureus strains. THCBD (4) has also shown a good effect in kill kinetic assays against ATCC-29213 and MRSA-15187. In the checkerboard assay, THCBD (4) has shown additive/indifference effects with several well-known clinically used antibiotics, tetracycline, mupirocin, penicillin G, and ciprofloxacin. THCBD (4) also exhibited good permeability in the artificial skin model. Most importantly, THCBD (4) has significantly reduced CFU in mice's in vivo skin infection models and also demonstrated decent plasma exposure with 16-17% oral bioavailability. Acute dermal toxicity of THCBD (4) suggests no marked treatment-related impact on gross pathophysiology. This attractive in vitro and in vivo profile of plant-based compounds opens a new direction for new-generation antibiotics and warrants further detailed investigation.

Rapid determination and optimisation of berberine from Himalayan Berberis lycium by soxhlet apparatus using CCD-RSM and its quality control as a potential candidate for COVID-19.

SARS-CoV-2 (or COVID-19) has become a global risk and scientists are attempting to investigate antiviral vaccine. Berberis are important plants due to the presence of bioactive phytochemicals, especially berberine from the protoberberine group of benzylisoquinoline and recent studies have shown its potential in treating COVID-19. B. lycium Royle growing in subtropical regions of Asia had wide applications in Indian system of medicine. Rapid determination and novel optimisation method for berberine extraction has been developed by Soxhlet extraction utilising central composite design-response surface methodology (CCD-RSM). Berberine was detected by high-performance liquid chromatography (HPLC), and the highest yield (13.39%) was obtained by maintaining optimal extraction conditions i.e., extraction time (7.28 hrs), ethyl alcohol (52.21%) and solvent to sample ratio (21.78 v/w). Investigation of two geographic regions (Ramnagar and Srinagar) showed high berberine content in lower altitude. This novel optimisation technique has placed berberine as a potential candidate for developing pharmaceutical products for human health care.