Nigella sativa Oil-loaded Ethanolic Vesicular Gel for Imiquimod-induced Plaque Psoriasis: Physicochemical Characterization, Rheological Studies, and In vivo Efficacy.

BACKGROUND: The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone ( < 15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions. AIMS: This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity. OBJECTIVE: The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity. METHODS: The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model. RESULTS: A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 µg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil). CONCLUSION: It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.

Molecular recognition of carbonate ion using a novel turn-on fluorescent probe.

A novel turn-on fluorescent probe 3 was synthesized by condensing salicylaldehyde and nicotinic hydrazide for the selective detection of CO32- in aqueous medium. Probe 3 exhibited a turn-on fluorescence response toward CO32- with excellent selectivity, sensitivity (DL = 2.76 µM), and good reversibility. The binding constant (K) of probe 3 with CO32- was calculated to be 5 × 103 M-1 (log K 3.69). The 1:1 stoichiometry of the complex between probe 3 and CO32- ions was confirmed by Job's plot and ESI-MS spectra. Deprotonation and hydrogen-bonding interactions are involved in the recognition of CO32- ion, which was also suggested by 1H NMR, ESI-MS spectra, and Density Functional Theory (DFT) calculations. Moreover, an INHIBIT type molecular logic gate was constructed by using 3:CO32- and CH3COOH as inputs and current signal as output. Owing to the practical applications, probe 3 demonstrated its efficiency in quantifying CO32- ion in real water samples through standard addition method, thus showcasing its potential in real environment. Further, the MTT assay indicated very low cytotoxicity (IC50 = 1 mM) of probe 3 and also the cell imaging experiments demonstrated the effective sensing of CO32- ions with probe 3 in the biological systems.

Two new anticancer phenolic derivatives from leaves of Piper betle Linn.

In this study, phytochemical analyses of the chloroform extract of Piper betle L. var. haldia and maghai, Piperaceae, leaves led to the isolation of two new phenolic derivatives: 1-n-decanoyl hydroxy-benzoic acid/1-n-decanoyl phenol (H2) and 3-butylphenol (M1) on the basis of spectroscopic data 1D NMR (1H, 13C) and 2D NMR (1H - 1H COSY, HMBC) as well as ESI-MS, FT-IR and HR-ESI-MS analyses. Compounds H2 and M1 showed excellent antioxidant DPPH free radical scavenging activity with IC50 values of 10.66 µ/mL and 13.65 µg/mL compared to ascorbic acid as a standard antioxidant with an IC50 value of 2.52 µg/mL. Evaluation of cytotoxic activity against two human oral cancer cell lines (SCC-40 and SCC-29B) showed significant effect with GI50 values of 24.08 and 33.08 µg/mL for compound H2 and 35.03 and 47.06 µg/mL for compound M1, compared to Doxorubicin® as a standard cytotoxic drug with GI50 value of < 10 µg/mL.

New chemical constituents from the Piper betle Linn. (Piperaceae).

The phytochemical investigation of chloroform extract from Piper betle var. haldia, Piperaceae, leaves has resulted in the isolation of two new chemical constituents which were identified as 1-n-dodecanyloxy resorcinol (H1) and desmethylenesqualenyl deoxy-cepharadione-A (H4), on the basis of spectroscopic data 1D NMR (1H and 13C) and 2D NMR (1H-1H COSY and HMBC) as well as ESI-MS, FT-IR and HR-ESI-MS analyses. Compounds H1 and H4 showed excellent antioxidant DPPH free radical scavenging activity with IC50 values of 7.14 µg/mL and 8.08 µg/mL compared to ascorbic acid as a standard antioxidant drug with IC50 value of 2.52 µg/mL, respectively. Evaluation of cytotoxic activity against human hepatoma cell line (PLC-PRF-5) showed moderate effect with the GI50 values of 35.12 µg/mL for H1, 31.01 µg/mL for H4, compared to Doxorubicin® as a standard cytotoxic drug with GI50 value of 18.80 µg/mL.