Saurabh Satija

Antioxidant and cytotoxic potential of a new thienyl derivative from Tagetes erecta roots.

Context: The search for newer compounds against pathogenic species continues unabated due to drug resistance. Traditionally, Tagetes erecta Linn. (Compositae) has been used for the treatment of various parasitic and microbial diseases. Objective: To evaluate the antioxidant activity of the ethanol extract of Tagetes erecta roots and its cytotoxicity against prostate and HeLa cancer cell lines followed by activity-guided isolation. Materials and Methods: The antioxidant screening was carried out using diphenylpicrylhydrazyl (DPPH) radical scavenging assay with serial concentrations ranging from 2 to 100 µg/mL, and cytotoxicity was evaluated against prostate (PC-3) and HeLa cell lines using microculture tetrazolium test (MTT) assay with concentrations ranging from 500 to 1.89 µg/mL. Isolation of the ethanol extract was carried out using column chromatography whereby 21 isolates were obtained (T1-T21), and the most active isolate was subjected for characterization using ultraviolet (UV), infrared (IR), nuclear magnetic resonance (NMR), and mass spectroscopic techniques. Results: The ethanol extract scavenged DPPH free radicals thereby exhibiting antioxidant activity with an IC50 of 35.9 µg/mL. In addition, the extract conferred noticeable cytotoxicity against the HeLa (LD50 of 164.28 µg/mL) and PC-3 cell lines (LD50 of 407.3 µg/mL). Among all the isolates, T3 showed antioxidant activity with IC50 of 11.56 µg/mL and cytotoxicity with LD50 of 12.5 µg/mL against HeLa and 30.25 µg/mL against PC-3 cell lines and was characterized as 2-ethynyl-5-(thiophen-2-yl) thiophene. Discussion: The new thienyl compound (T3) exhibited profound antioxidant activity and cytotoxicity at relatively lower concentrations than the extract. Conclusion: The observations provide support for the ethnobotanical use of the plant.

Development of a new, rapid, and sensitive validated high-performance thin-layer chromatographic method for the estimation of berberine in Tinospora cordifolia

A straightforward, delicate, and fast elite thin-layer chromatographic system (high-performance thin-layer chromatography [HPTLC]) has been produced and validated for the quantitative determination of berberine in Tinospora cordifolia. The chromatographic development was completed on HPTLC plates precoated with silica gel 60 F254 utilizing a blend of methanol, acetic acid, and water (8:1:1, v/v) as the mobile phase. Detection was completed densitometrically at 366 nm. The RF estimation of berberine was observed to be 0.71 ± 0.02. The system was validated according to the International Conference on Harmonization (ICH) guidelines regarding linearity, precision, accuracy, robustness, and so forth. The calibration curve was observed to be straight over a scope of 120–360 ng spot−1 with a regression coefficient of 0.971. The accuracy was observed to be as high as 98.56%, and the relative standard deviation (% RSD) values for intra-day and between-day variations were under 2%. The system showed high affectability and specificity. The strategy is new, basic, and economical for the routine estimation of berberine in T. cordifolia plant tests to help the commercial ventures and, in addition, scientists for their quick touchy determination of critical phytoconstituent berberine, requiring little to no effort in routine examination.

Multi-drug resistant Mycobacterium tuberculosis & oxidative stress complexity: Emerging need for novel drug delivery approaches

Tuberculosis (caused by Mycobacterium tuberculosis, Mtb) treatment involves multiple drug regimens for a prolonged period. However, the therapeutic benefit is often limited by poor patient compliance, subsequently leading to treatment failure and development of antibiotic resistance. Notably, oxidative stress is a crucial underlying factor that adversely influences the various treatment regimens in tuberculosis. Little information is available with advanced drug delivery systems that could be effectively utilized, in particular, for targeting the oxidative stress in tuberculosis. Thus, this presents an opportunity to review the utility of various available, controlled-release drug delivery systems (e.g., microspheres, liposomes, niosomes, solid lipid nanoparticles, dendrimers) that could be beneficial in tuberculosis treatments. This will help the biological and formulation scientists to pave a new path in formulating a treatment regimen for multi-drug resistant Mtb.