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Present study was aimed to investigate the antibacterial activity, bactericidal mechanism of action, killing kinetics and anti-inflammatory activity of Isodon melissoides (Benth.) H. Hara essential oil. The gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS) analysis revealed the presence of carvacrol (45.4%), p-cymene (11.6%) and thymol (11.3%) as major constituents of the oil. The oil displayed broad spectrum significant antibacterial activity (MIC: 0.13–8.33 ppm; MBC: 0.13–>33.34 ppm) against test strains. The oil exhibited a time and dose-dependent bactericidal effect. The oil disrupted the cell membrane by changing the cell membrane permeability. The essential oil significantly decreased the overproduction of proinflammatory cytokines in LPS-induced inflammation in HaCaT cells without any cytotoxic effect. I. melissoides essential oil can be a promising alternative antimicrobial agent for the control of methicillin resistant staphylococci and other pathogenic bacteria tested, and also useful for the topical anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

A polyphenolic flavonoid, Silymarin isolated from Silybum marianum is widely known for its hepatoprotective action. In the present study anti-plasmodial activity of Silymarin has been demonstrated for the first time having IC50 of 14 ± 0.33 μM against the NF-54 strain of P. falciparum with high selectivity index (>100). The parasitostatic action is exerted through inhibition of β-hematin/hemozoin formation which is due to the interaction (Kd = 3.63 ± 0.9µM) of silymarin with free heme in a Stoichiometry of 1:1 Silymarin: heme complex resulting into heme-induced membrane damage in the parasite. Silymarin could hinder the glutathione and hydrogen peroxide-induced heme detoxification. Silymarin also induces apoptosis in the parasite through the elevation of caspase-3 level in a dose-dependent manner. Results from the docking studies suggest that Silymarin interacts with heme. [ABSTRACT FROM AUTHOR]

In this study, antimicrobial activity of the essential oil (EO) and extracts of Himalayan-thyme (Thymus linearis Benth.) was evaluated against nine pathogenic microbial strains using disc diffusion and microdilution broth assays. The chemical composition of the EO was determined by gas chromatography-flame ionisation detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The molecular mechanism of action of the EO was investigated against three pathogenic bacteria (Staphylococcus aureus, Staphylococcus epidermidis and Enterococcus faecalis) and three fungal strains (Candida albicans, Candida glabrata, and Candida tropicalis) using the assays of protein leakage, and DNA and RNA leakage through the membrane. Major components of the EO were thymol (54.9%), γ-terpinene (16.6%) and p- cymene (5.2%). The EO showed broad-spectrum potent antibacterial and antifungal activity (MIC 240–990 µg/mL) against test strains. The EO damaged cell membranes and altered cell membrane permeability of test microorganisms. The EO showed a time- and dose-dependent bactericidal and fungicidal effect. It could act as a promising antimicrobial agent due to its short killing time. [ABSTRACT FROM AUTHOR]

Eugenol is a phytochemical present in aromatic plants has generated considerable interest in the pharmaceutical industries mainly in cosmetics. A series of eugenol esters (ST1-ST7) and chloro eugenol (ST8) have been synthesized. The structures of newly synthesized compounds were confirmed by ¹H and 13C NMR and mass spectrometry. In an effort to evaluate the pharmacological activity of eugenol derivatives, we explored its anti-inflammatory potential against skin inflammation using in-vitro and in-vivo bioassay. Synthesized derivatives significantly inhibited the production of pro-inflammatory cytokines against LPS-induced inflammation in macrophages. Among all derivatives, ST8 [Chloroeugenol (6-chloro, 2-methoxy-4-(prop-2-en-1-yl)-phenol)] exhibited most potent anti-inflammatory activity without any cytotoxic effect. We have further evaluated the efficacy and safety in in-vivo condition. ST8 exhibited significant anti-inflammatory activity against TPA-induced skin inflammation without any skin irritation effect on experimental animals. These findings suggested that ST8 may be a useful therapeutic candidate for the treatment of skin inflammation. [ABSTRACT FROM AUTHOR]

Prostate cancer is fourth most abundant cancer type around the globe. Brevifoliol, a rearranged taxoid from Taxus walllichiana needles has been derivatized as C5 esters using Steglich esterification reaction. Seventeen diverse analogues were evaluated against a panel of human cancer cell lines by MTT assay. Among these, two of the semi‐synthetic analogues, that is, 13 and 16 exhibited potent cytotoxicity, selectively against PC‐3, prostate cancer cell lines. In cell cycle analysis, analogue 13 induced S and G2/M phase arrest and induced apoptosis by activating caspase‐3. Compound 13 showed moderate efficacy in in‐vivo Ehrlich ascites carcinoma in Swiss albino mice. Further, compound 13 was found to be safe in Swiss albino mice up to 1,000 mg/kg dose in acute oral toxicity. Brevifoliol ester 13 may further be optimized for better efficacy. [ABSTRACT FROM AUTHOR]

Background: Three key coumarinolignoids, cleomiscosins A, B, and C of Cleome viscosa seed origin in particular ratio, are a proven hepatoprotective agent known as Cliv-92. Objectives: However, the bioavailability and pharmacokinetics of Cliv-92 are still not clear. The present study is the first validated method which deals with the assay of Cliv-92 in mouse plasma. Methods: Single-step sample preparation meets the criteria of recovery (80%-93% with relative standard deviation [RSD] 2.14%-4.80%). Reverse-phase high-performance liquid chromatography with photodiode array detection has resulted into acceptable separation and sensitivity of three structurally similar cleomiscosins - A, B, and C of Cliv-92. The analysis involved a binary gradient of mobile phase and flow rate. Quantification was done at peak area at 326 nm using linear regression curve (r² > 0.999). The precision (0.46%-2.68% RSD) and accuracy (±2.09% bias) of Cliv-92 determination in plasma complied the criteria of the current international guidelines. We have also evaluated the matrix effect on sensitivities by spiking method. Limit of detection and limit of quantification in mouse plasma ranged between 0.13-0.24 µg/ml and 0.41-0.74 µg/ml. Results: Pharmacokinetic parameters were studied after intravenous bolus administration of Cliv-92 at 10 mg/kg dose in mice. Blood samples were collected at a predefined time up to 24 h post-injection. The Cliv-92 plasma half-life (t1/2) was 2.77 h, and the clearance was estimated as 2.38 L/h/kg. Conclusion: The method is simple, sensitive, and accurate for the determination of plasma concentration of coumarinolignoids. The present preclinical pharmacokinetic study of coumarinolignoids has been anticipated in clinical studies with scaling techniques. [ABSTRACT FROM AUTHOR]

Chemical investigations on the fruits of Zanthoxylum armatum Roxb. (Rutaceae) led to the isolation of two new constituents characterised as 2α-methyl-2β-ethylene-3β-isopropyl-cyclohexan-1β, 3α-diol (1) and phenol-O-β-D-arabinopyranosyl-4′-(3″, 7″, 11″, 15″-tetramethyl)-hexadecan-1″-oate (2) along with known compounds m-methoxy palmityloxy benzene (3), acetyl phenyl acetate (4), linoleiyl-O-α-D-xylopyranoside (5), m-hydroxyphenoxy benzene (6) and palmitic acid (7). The chemical structures were established with the help of physical, chemical and spectroscopic methods. The anti-inflammatory potential of isolated compounds 1 and 2 was evaluated using in vitro target-based anti-inflammatory activity in LPS-stimulated primary peritoneal macrophages isolated from mice. Production of pro-inflammatory cytokines (TNF-α and IL-6) was significantly inhibited by the treatment of isolated compounds 1 and 2 in a dose-dependent manner. [ABSTRACT FROM AUTHOR]

Background: Long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) increases risk of having a range of gastrointestinal problems. Therefore, new anti-inflammatory, analgesic, antipyretic drugs having lesser side effects are being searched all over the world as alternatives to NSAIDs. Aims: To evaluate the anti-inflammatory, analgesic and antipyretic profile of Ocimum sanctum root extracts. Materials and Methods: Anti-inflammatory profile of hexane (STH), chloroform (STC), ethyl acetate (STE), butanol (STB) and water (STW) extracts of OS was carried out by using carrageenan induced paw edema. STE a most active extract was further validated in dose dependent manner for anti-inflammatory, analgesic and antipyretic activity as well as oral toxicity profile in small laboratory animals. Identification of bioactives flux and chemical signature of most active fraction STE was developed by using the high-performance liquid chromatography fingerprinting. Results: An ethyl acetate fraction (STE) exhibit most potent anti-inflammatory activity followed by STB, STW, STC and STH. Dose response study of STE showed anti-inflammatory, analgesic and anti-pyretic potential in dose-dependent manner without any toxic effect at dose 2000 mg/kg. Chemical fingerprint revealed the presence of flavanoids. Conclusions: The present research revealed that STE possess anti-inflammatory, analgesic and anti-pyretic properties. However, future research is advocated to evaluate the pharmacological properties of isolated bioactive compounds. [ABSTRACT FROM AUTHOR]