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The genus Cuscuta belonging to the Cuscutaceae family comprises of about 100–170 species spread around the world. Although several species have been studied for their phytochemical characterization and biological activities but still many species are yet unexplored till date. Cuscuta are parasitic plants generally of yellow, orange, red or rarely green color. The Cuscuta species were reported rich in flavonoid and glycosidic constituents along with alkaloids, fatty acids, fixed oil, minerals, essential oil and others phytomolecules also etc. Flavonoids and other molecules of Cuscuta species were reported for different types of biological activities such as antiproliferative activity, antioxidant activity, anti-inflammatory, hepatoprotective, antimicrobial and anxiolytic activity, while some other flavonoids have exhibited potential antiviral and anticancer especially in ovarian and breast cancer activities. This review is an attempt to compile all the available data for the 24 different of Cuscuta species on the basis of different types of phytochemical constituents and biological studies as above. [ABSTRACT FROM AUTHOR]

Abstract: The paper reports an improved pilot scale process technology for the extraction of Cliv-92: a combination of three hepatoprotective coumarinolignoids, cleomiscosins A, B and C from the seeds of Cleome viscosa. The method involved the extraction of the defatted seeds with methanol, which on concentration gave a viscous residue. Trituration of the residue with methanol and keeping it at a low temperature resulted in the precipitation of Cliv-92 which was separated by filtration. Almost half of total yield of Cliv-92 was obtained from the methanolic extract simply by the trituration method. The filtrate obtained was concentrated and adsorbed on celite. The adsorbed material was then partitioned with toluene, ethyl acetate and methanol successively. The fractions obtained from partitioning methods were concentrated and Cliv-92 was isolated from the above fractions by passing through a bed of silica gel. The novelty of the improved process included application of an extrusion device to expel out the fixed oil before extraction, adopting trituration technique to effectively crystallize the coumarinolignoids and using solid-matrix partitioning technique thereby avoiding the use of water for partitioning to isolate the coumarinolignoids. The yield of Cliv-92 obtained was 1.13% carried out at a scale of 100kg/batch level which was about 10 times higher in comparison to previous bench scale process. [Copyright &y& Elsevier]

Citronella (Cymbopogon spp.) essential oil is an important component of various fragrances, cosmetics, and household products. In this study, comparative chemical composition and antimicrobial activity of Java citronella (Cymbopogon winterianus Jowitt ex Bor) essential oil, extracted by different methods, namely hydro-distillation and steam-distillation were determined by GC, GC-MS, and disc diffusion assay and microdilution broth assay. Major constituents of the essential oil were citronellal (2.2–55.4%), geraniol (14.2–53.0%), citronellol (8.2–16.4%), isopulegol (0.3–12.6%), elemol (0.8–8.2%), and limonene (0.2–5.0%). The essential oils showed inhibition of test bacteria with minimum inhibition concentration (MIC) in the range of 250–1000 µg/mL and showed anticandidal activity with MIC in the range of 125–500 µg/mL. In general, the oils were moderately active against Gram-positive and Gram-negative bacterial strains and also showed good activity against Candidal strains. The essential oils extracted from the herbage by different techniques exhibited variations in their yield, chemical composition, and antimicrobial activities. [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]

The present investigation for the first time explains the anti biofilm and anti virulence potential of Kaffir lime oil (KLO) and its major constituent, Citronellal (3,7-dimethyloct-6-enal) against Xanthomonas oryzae pv. oryzae , causal organism of bacterial blight disease of rice. KLO at 500 ppm showed potential activity against X. oryzae pv. oryzae . Among the major components identified, citronellal (CIT) at 75 μM concentration was found to significantly inhibit biofilm along with the swimming and swarming potential of X. oryzae pv. oryzae . In contrary, CIT did not affect the metabolic status and growth kinetics of the bacterial cells. Gene expression analysis showed down regulation in motA, cheD, cheY, flgF, gumC, xylanase, endogluconase, cellulose, cellobiosidase, virulence and rpfF transcript levels by citronellal treatment. However, an insignificant effect of 75 μM CIT treatment was observed on motB, flgE, pilA, estY, pglA , protease and lytic genes expression. Finally, the observations recorded were in confirmity with the virulence leaf clip test as lesion length was significantly decreased (39%) in CIT treatment as compared to the control leaves inoculated with only X. oryzae pv. oryzae . Overall, the findings obtained advocate the use of CIT for promising anti biofilm and anti virulence activity which in turn can be used for managing the blight disease in rice. [ABSTRACT FROM AUTHOR]

Liquiritigenin (LTG) and its bioprecursor isoliquiritigenin(ISL), the main bioactives from roots of Glycyrrhiza genus are progressively documented as a potential pharmacological agent for the management of chronic diseases. The aim of this study was to evaluate the pharmacological potential of liquiritigenin, isoliquiritigenin rich extract of Glycyrrhiza glabra roots (IVT-21) against the production of pro-inflammatory cytokines from activated macrophages as well as further validated the efficacy in collagen-induced arthritis model in rats. We also performed the safety profile of IVT-21 using standard in-vitro and in-vivo assays. Results of this study revealed that the treatment of IVT-21 and its major bioactives (LTG, ISL) was able to reduce the production of pro-inflammatory cytokines (TNF-α, IL-6) in LPS-activated primary peritoneal macrophages in a dose-dependent manner compared with vehicle-alone treated cells without any cytotoxic effect on macrophages. In-vivo efficacy profile against collagen-induced arthritis in Rats revealed that oral administration of IVT-21 significantly reduced the arthritis index, arthritis score, inflammatory mediators level in serum. IVT-21 oral treatment is also able to reduce the NFкB-p65 expression as evidence of immunohistochemistry in knee joint tissue and mRNA level of pro-inflammatory cytokines in paw tissue in a dose-dependent manner when compared with vehicle treated rats. Acute oral toxicity profile of IVT-21 demonstrated that it is safe up to 2000 mg/kg body weight in experimental mice. This result suggests the suitability of IVT-21 for further study in the management of arthritis and related complications. [ABSTRACT FROM AUTHOR]

The needle powder of Taxus wallichiana is in use for the management of diabetes and inflammation-related complications in the Indian and Chinese Systems of Traditional Medicine but the lack of proper pharmacological intervention has prompted us to investigate the pharmacological mechanism against inflammation-induced insulin resistance in high-fat diet-fed C57BL/6 mice. Hexane (Tw-H), chloroform (Tw-C), and ethyl acetate (Tw-EA) extracts were prepared from a needle of T. wallichiana and its effect on glucose uptake against TNF-α-induced insulin resistance in skeletal muscle cells was studied. Among all, Tw-EA extract has shown promising glucose uptake potential. Tw-EA treatment is also able to decrease the lipid accumulation in adipocytes. Chemical signature of Tw-EA using HPLC showed the presence of taxoids. Efficacy of taxoids-rich extract from T. wallichiana (Tw-EA) was further validated in in vivo system against high-fat diet (HFD)-induced insulin resistance in C57BL/6 mice. Oral treatment of Tw-EA showed significant reduction in blood glucose, pro-inflammatory cytokine production and body weight gain when compared with vehicle-treated HFD-induced insulin resistance in C57BL/6 mice. Histopathology and immunohistochemistry study in skeletal muscle and adipose tissue revealed that oral treatment of Tw-EA is able to reduce the infiltration of inflammatory cells in skeletal muscles, ameliorate the hypertrophy in adipose tissue and upregulate the GLUT4 protein expression. Treatment with Tw-EA significantly up-regulated mRNA expression of insulin signaling pathway (IRS-1, PI3K, AKT, GLUT 4). This study suggested the beneficial effect of taxoids-rich extract from Taxus wallichiana against the inflammation-associated insulin resistance condition. [ABSTRACT FROM AUTHOR]

Aloe barbadensis popularly known as Aloe vera is an extensively cultivated medical herb that is significantly affected by phytopathogenic fungal infestations worldwide. Huge economic losses occur due to leaf spot disease caused by Alternaria spp. The use of different fungicides to manage this disease has harmful impacts on both the environment and the pharmacologically valuable components of Aloe vera. In this study, the antifungal activities and mechanism of 1,8-cineole, a major component of Eucalyptus globulus essential oil (EGO) was investigated as the potential substitute for synthetic fungicides against Alternaia tenuissima. 1,8-cineole at a minimum inhibitory concentration (MIC) of 5 µL mL−1 significantly reduced the ergosterol biosynthesis, along with weak cellular membrane, stunted germ tube development with hampered cell wall rigidity. At the gene level, the elevated expression of NADPH oxidase A (NoxA) gene in fungus treated with 1,8-cineole resulted in an increased production of reactive oxygen species (ROS) that triggered cellular damage, leading to the successful mitigation of the phytopathogen. Furthermore, 1,8-cineole downregulated genes related to chitin synthase, ergosterol synthase, cellulase production, glycosyl hydrolase, RhO1 G protein (Rho1), cyclic AMP-dependent protein kinase subunit 1 (AAPK1), and glyceraldehyde-3-phosphate dehydrogenase (GADPH) which validated its detrimental effect on A. tenuissima. To further confirm the proposed antifungal mechanism, docking simulations were run between 1,8-cineole and a potential antifungal target glucosamine-6-phosphate synthase that revealed an efficient interaction with the designed protein model. Consequently, this research offers promising prospects for developing sustainable methods for safeguarding crops through the use of bioactive phyto compounds. [Display omitted] • First report on antifungal effect of Eucalyptus globules oil against Alternaria tenuissima. • 1, 8-cineole identified as a major bioactive molecule of the oil through GC-MS analysis. • 1, 8-cineole effects the expression of virulence and structural genes of A. tenuissima. • Glucosamine-6-phosphate synthase was found as potential target of 1,8-cineole through docking. [ABSTRACT FROM AUTHOR]

Artemisia pallens Wall. ex DC, commonly known as davana, is cultivated in India for extraction of its essential oil (DO). In this study, DO collected from thirteen locations (DO1-DO13) and those extracted from six different phenophases and different plant parts were investigated using GC-FID and GC-MS. Altogether, 84 constituents were identified, forming 81.0–96.2% of the total oil composition. Major components of the oils were cis-davanone (17.4–65.1%), bicyclogermacrene (4.0–22.0%), cis-methyl jasmonate (0.4–8.5%), β-eudesmol (0.3–6.6%), davana ether isomer (0.5–6.1%), trans-ethyl cinnamate (1.4–6.1%), and germacrene D (0.1–4.7%). Among all tested oils, the DO10, having low cis-davanone content (27.5%), was found more potent against test microorganisms. The oils collected from different locations showed variations in their physical properties, chemical composition, and antimicrobial activity. Based on the yield and cis-davanone content, the flower bud and full-flowering stages could be suitable for harvesting good quality oil in north Indian plains. [ABSTRACT FROM AUTHOR]

Abstract: Natural nevirapine (1), a dipyridodiazepinone metabolite has been isolated as a minor constituent with a yield of 0.00397% from the ethyl acetate extract during large scale extraction of Cliv-92 at a level of 100kg/batch from the seeds of Cleome viscosa. Column chromatographic purification of the ethyl acetate extract afforded the molecule which was characterized as nevirapine through spectral analysis and confirmed by single crystal X-ray crystallography. The molecule also has been re-isolated from the same batch of seeds to confirm its presence in the seeds of C. viscosa. The molecule nevirapine has been fully characterized by co-TLC, prep-TLC-MS/MS and chiral HPLC analysis. Isotope Ratio Mass Spectrometric (IRMS) analysis of natural nevirapine and the synthetic drug revealed it to be different. It is an interesting discovery to find out that the natural nevirapine exists as an endogenous metabolite of the plant. This paper also reports the isolation of salicylic acid from the same batch of seeds which afforded nevirapine which may have been due to some plant–pathogenic interaction. [Copyright &y& Elsevier]

Abstract: Large scale extraction of the fruits of Garcinia indica was conducted with water extracted hydroxyl citric acid. The marc left after water extraction was extracted exhaustively with methanol and concentrated methanol. The concentrated methanol extract was adsorbed with celite and dried. The dried celite containing the methanol extract was successively extracted with hexane, chloroform and ethyl acetate to get hexane, chloroform and ethyl acetate extract respectively. Column chromatographic separation of hexane extract afforded two new molecules, one polyisoprenylated benzophenone and a new acylphloroglucinol derivative and two known molecule garcinol and isogarcinol. Likewise, chromatographic separation of the chloroform and ethyl acetate extract also yielded extra quantity of garcinol and isogarcinol respectively. Garcinol was isolated as a major compound among all the four molecules isolated from the fruits G. indica. [Copyright &y& Elsevier]

Abstract: The optically active nevirapine, a natural analogue of the previously designed and synthesized optically inactive nevirapine, a non-nucleoside inhibitor of HIV-1 reverse transcriptase, has been isolated and fully characterized from the seeds of Cleome viscosa. The structure of natural nevirapine has been confirmed by X-ray crystallography. It is an interesting discovery to find out that optically inactive nevirapine was designed and synthesized before the isolation of optically active nevirapine from the seeds of C.viscosa. [Copyright &y& Elsevier]

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]

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]

Highlights • Treatment of palmarosa and ajwain oils inhibited sprouting of potato tubers. • Treatments of lemon grass and clove oils induced sprouting of potato tubers. • Selected oils treatments modulated accumulation of reducing sugars and ethylene. • Selected oils treatments modulated expression of key genes of tuber-sprouting. • Selected oils can be used for reducing post-harvest losses of potato crop. Abstract Use of harmful chemicals and expensive maintenance of cold-storage conditions for controlling sprouting are among the major problems in potato storage. Here, 20 essential oils (EOs) were tested for their sprouting-inhibiting and sprouting-inducing activities. Overall, treatments of lemon grass (LG) and clove (CL) oils could induce sprouting whereas palmarosa (PR) and ajwain (AZ) oils could inhibit sprouting of potato tubers at normal-room-temperature (25 ± 2 °C) storage. Selected-EOs treatments affected sprouting by modulation of accumulation of reducing sugars, ethylene, and expression of genes involved in tuber-sprouting such as ARF , ARP , AIP and ERF. Surprisingly, 7-days AZ-treatments could inhibit sprouting for 30-days which was mediated via damaging apical meristem. However, LG- and CL-treated tubers could produce enhanced potato yield as well. Present work clearly demonstrates that selected-EOs can be used as a promising eco-friendly approach for inducing/inhibiting sprouting of potato tubers during potato storage and those enhancing sprouting can be used for enhancing productivity. [ABSTRACT FROM AUTHOR]

Abstract Ethnopharmacological relevance Tejovati (Zanthoxylum armatum DC; Family- Rutaceae) popularly known as toothache tree is widely distributed in sub-tropical Himalaya region. Traditionally, The Southeast Asian population of Indo-Nepal origin uses it to treat asthma, gout, pain, and inflammation. The Ayurvedic action of the plant includes the balancing of Vata-Kapha in the body. Which lead to various ailments related to the circulation of blood and water, digestion, immunity, and skin. Therefore, in-vitro xanthine oxidase (XO) inhibition potential of the extract could be worth to explore prospect in the prevention/treatment of gouty affections of the joints and other diseases. Aim of study Anti-inflammatory and antioxidant potential of Z. armatum fruit (ZAF) has been reported. To date, no scientific study to validate the claim for gout treatment/management has been attempted so far. The present study deals with the xanthine oxidase inhibitory potential of a various extract of ZAF and marker-based high-performance liquid chromatography (HPLC) standardization of most active fraction. Materials and methods Liquid-liquid partioning of crude methanol extract of the ZAF followed by repeated column chromatography of most active fraction has resulted in the isolation of seven compounds. Five distinct groups of compounds were isolated, purified, and identified. We have investigated the therapeutic action of ZAF in the management of gout through in-vitro assay of XO, a key enzyme involved in gout pathogenesis. Results Phytochemical investigation of ZAF has resulted in the isolation of seven compounds of diverse nature. It is noteworthy to mention that out of seven, five compounds have shown the xanthine oxidase inhibitory action. The ethyl acetate fraction was most potent to inhibit XO. The XO inhibitory activity (IC 50 values) of isolated marker chemical was ranging from 5.62 to 41.21 µM. Three compounds viz. acetyl phenyl acetate (ZA-2), prudomestin (ZA-6), and tambulin (ZA-7) showed the most potent XO inhibitory activity (IC 50 ≈ 6 µM) comparable with a positive control (Allopurinol, IC 50 , 3.38 µM). This is the first validated HPLC-PDA method for simultaneous analysis and accurate quantification of seven compounds (phenolic acid, acetyl phenyl acetate, xylopyranoside, diphenyl ether and three flavones) in ZAF as well as their distribution in other tissues of the plant. Conclusion Most potent three chemicals (ZA-2, 6 and 7) could be considered as bioactive to ensure the robust quality of the enriched fraction of ZAF with defined XO inhibition potential. Therefore, either single purified component or their enriched fraction could be a better choice for the management of gout than the crude extract of ZAF. Developed HPLC method is suitable for quality assurance analysis and process control of ZAF derived product intended for gout management. XO inhibitory potential exhibited by the characterized compounds validate the traditional use of this ZAF for the treatment of gout. Further, a detailed study is required to assess the effect of ZAF chemicals on serum uric acid and mechanism of XO inhibition. Graphical abstract fx1 [ABSTRACT FROM AUTHOR]

A practical and novel approach has been developed for the synthesis of oleanolic acid based chromene analogues. Different α,β-unsaturated carbonyl and chromene derivatives of oleanolic acid were synthesized and evaluated for their anticancer activity. Compounds 6e, 6k, 7e and 7g showed significant anticancer activity within the IC50 range of 12.23–39.04 μg mL−1. The promising derivatives 7e and 7g were further analyzed for their effects on the cell cycle and apoptosis in A-549 and MDA-MB-231 cells, and it was depicted that 7e and 7g triggered apoptosis in A-549 and MDA-MB-231 cells and arrested the cell population in the G2/M phase. The anticancer activity of the most active analogue 7g occurred through microtubule destabilization (IC50: ∼3.6 μg mL−1), and it was found to be non-toxic against human erythrocytes. The compounds 7e and 7g significantly inhibited the proinflammatory cytokines TNF-α and IL-6. [ABSTRACT FROM AUTHOR]

Background: Curcuma longa L. is an important industrial crop used by medicinal and cosmetic industries in the world. Its leaves are a waste material after harvesting rhizomes. The aim of the study was to evaluate the chemical and pharmacological profile of essential oil from waste leaves of Curcuma longa (EOCl) against skin inflammation.Methods: EOCl was subjected to gas chromatography (GC) analysis for identification of essential oil constituents and its anti-inflammatory evaluation through in vitro and in vivo models.Results: Chemical fingerprinting using GC and GC-MS analysis of EOCl revealed the presence of 11 compounds, representing 90.29% of the oil, in which terpinolene (52.88%) and α-phellandrene (21.13%) are the major components. In the in vitro testing EOCl inhibited the production of pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) in lipopolysaccharide (LPS) and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in the human keratinocyte cell line (HaCaT). Topical application of EOCl produced anti-inflammatory effects by reducing ear thickness, ear weight and ameliorating the level of pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) at protein and mRNA levels as well as regulating the overproduction of oxidative markers and restoring the histopathological damage in a TPA-induced mouse model of inflammation.Conclusion: These findings of topical anti-inflammatory properties of EOCl provide a scientific basis for medicinal use of this plant material against inflammatory disorders.Graphical Abstract: [ABSTRACT FROM AUTHOR]

To create your abstract, type over the instructions in the template box below. Fonts or abstract dimensions should not be changed or altered. [Display omitted] Braylin (10b) is a 8,8-dimethyl chromenocoumarin present in the plants of the family Rutaceae and Meliaceae and possesses vasorelaxing and anti-inflammatory activities. In this study, six 6-alkoxy (10b , 15 – 19), and twelve 6-hydroxy-alkyl amine (20a - 20l) derivatives of braylin (11 and 12) were synthesized to delineate its structural requirement for vasorelaxing activity. The synthesized compounds were evaluated for vasorelaxation response in preconstricted intact rat Main Mesenteric Artery (MMA). The compounds showed l -type VDCC channel blockade depended and endothelium-independent vasorelaxation within the range of Emax < 50.00–96.70 % at 30 µM. Amongst all, 6-alkoxy derivatives were more active than 6-hydroxy-alkyl amine derivatives. The structural refinements about braylin showed that deletion of its methoxy group or homologation beyond ethoxy group presented deleterious effect on vasorelaxation response of braylin. Interestingly, substituting the ethoxy group in 10b presented the best activity and selectivity towards l -type VDCC channel blockade, a specific target cardiovascular function. [ABSTRACT FROM AUTHOR]

Zanthoxylum armatum or Timoor has been used in different traditional system of medicine due to its aromatic properties and also in the treatment of cancer, diarrhea and cholera. In the present investigation, four chemically distinct compounds namely Tambulin (6), Prudomestin (7), Ombuin (8) and 3, 4, 5, 3′, 4′, 5′-hexahydroxydiphenyl ether (9) have been isolated and quantified from the fruits. To explore the biological activities, we have further studied the antiproliferative, antimicrobial and antioxidant efficacy. Tambulin which was also found in maximum amount (0.125%) in fruits revealed significant antiproliferative activity (IC 50 37.96 ± 0.36 to 48.7 ± 0.21 μg/mL) against breast, liver, colon and skin cancer cell lines corroborated by resilient binding interaction with SDH (−6.76 Kcal/mol) and inhibition constant (Ki: 11.02 μM). Hexane and ethyl acetate fraction exhibited moderate antibacterial efficacy (MIC: 250–1000 μg/mL) against selected pathogenic microbes while Ombuin displayed broad spectrum antibacterial effect with MIC ranges from 125 to 500 μg/mL. Total phenolic content (5.27 ± 0.06 to 46.12 ± 0.40 mg/g of gallic acid equivalents), total flavonoids content (6.05 ± 0.24 to 14.46 ± 0.73 mg/g of quercetin equivalents), ferric reducing power (42.35 ± 0.85 to 62.52 ± 0.66 mg/g of ferrous sulfate equivalents) and percent free radical scavenging activity (59.56 ± 0.38 to 64.85 ± 1.78) were also estimated. Our findings infer that Tambulin exhibited significant antiproliferative activity whereas Ombuin was found to display broad spectrum antibacterial activity which adds one more positive attribute to its traditional usage. [ABSTRACT FROM AUTHOR]

Background: Pyrethrins are monoterpenoids and consist of either a chrysanthemic acid or pyrethric acid with a rethrolone moiety. Natural pyrethrins are safe and eco-friendly while possessing strong insecticidal properties. Despite such advantages of commercial value coming with the eco-friendly tag, most enzymes/genes involved in the pyrethrin biosynthesis pathway remain unidentified and uncharacterized. Since the flowers of Tanacetum cinerariifolium are rich in major pyrethrins, next generation transcriptome sequencing was undertaken to compare the flowers and the leaves of the plant de novo to identify differentially expressed transcripts and ascertain which among them might be involved in and responsible for the differential accumulation of pyrethrins in T. cinerariifolium flowers. Results: In this first tissue specific transcriptome analysis of the non-model plant T. cinerariifolium, a total of 23,200,000 and 28,500,110 high quality Illumina next generation sequence reads, with a length of 101 bp, were generated for the flower and leaf tissue respectively. After functional enrichment analysis and GO based annotation using public protein databases such as UniRef, PFAM, SMART, KEGG and NR, 4443 and 8901 unigenes were identified in the flower and leaf tissue respectively. These could be assigned to 13344 KEGG pathways and the pyrethrin biosynthesis contextualized. The 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway was involved in the biosynthesis of acid moiety of pyrethrin and this pathway predominated in the flowers as compared to the leaves. However, enzymes related to oxylipin biosynthesis were found predominantly in the leaf tissue, which suggested that major steps of pyrethrin biosynthesis occurred in the flowers. Conclusions: Transcriptome comparison between the flower and leaf tissue of T. cinerariifolium provided an elaborate list of tissue specific transcripts that was useful in elucidating the differences in the expression of the biosynthetic pathways leading to differential presence of pyrethrin in the flowers. The information generated on genes, pathways and markers related to pyrethrin biosynthesis in this study will be helpful in enhancing the production of these useful compounds for value added breeding programs. Related proteome comparison to overlay our transcriptome comparison can generate more relevant information to better understand flower specific accumulation of secondary metabolites in general and pyrethrin accumulation in particular. [ABSTRACT FROM AUTHOR]

Different alkyl amide ( 15a – l ) and alkyl amine ( 16a – e ) derivatives of 7,8-dimethoxy-3-hydroxy-2-(4-methoxyphenyl)benzopyran-4-one were synthesized and evaluated for their anticancer activity against five different cancer cell lines using SRB assay. Compounds 15e , 15i , 15j and 16a – e showed significant anticancer activity within the range of IC 50 2.58–34.86 μM. The most promising molecule, 1 6c , was further analyzed for its effect on cell cycle and apoptosis of estrogen receptor positive cancer cells (MCF-7 cells) which showed that 16c triggered apoptosis in MCF-7 cells and arrested cells population at sub-G 0 (apoptotic) and G 2 M phase. In tubulin polymerization assay, 16c interfered with kinetics of tubulin polymerization. [ABSTRACT FROM AUTHOR]

Quorum sensing modulatory effect of linalool was tested for the first time against Pseudomonas syringae pv. tomato DC 3000, a bacterial plant pathogen responsible for causing huge losses worldwide. DC 3000 extensively regulates its virulence traits through quorum sensing mechanism involving expression of psyI, an acyl–homoserine lactone (AHL) synthase gene and psyR, a luxR-type regulator. In this study, exposure of DC 3000 to 80 ppm linalool concentration resulted in reduced biofilm formation, hampered motility, decreased AHL production, and reduced secretion of plant cell wall-degrading enzymes followed by negligible effect on the bacterial count and its metabolic activity. Extracellular polymeric substances (EPS), which play a crucial role in the development of biofilm and subsequent infection was significantly reduced which was further confirmed by Fourier Transform Infrared Spectroscopy. The qRT PCR analysis of the gene expression analysis of virulence genes (syringafactin production gene syfA, type III secretion system gene hrpA, flagellar genes fleQ and fliC, and coronatine production gene cfl unveiled significant downregulation of the same under Lin 80 ppm concentration. To further confirm the aforementioned possibilities, docking simulations run between PsyR and linalool suggested a strong interaction with the developed protein model. Overall, the treatment of DC 3000 with Lin 80 ppm affected the phenotypic and genotypic expressions associated with quorum sensing, thereby significantly reducing the infection rate as observed in in-vivo plant assay. [Display omitted] • Linalool suppresses the Quorum Sensing mechanism and production of AHL in Pseudomonas syringae DC 3000. • Linalool interferes with the biofilm formation and hinders virulence mechanism of the pathogen at 80 ppm. • Docking of PsyR and linalool suggests interactivity of linalool with QS mechanism. [ABSTRACT FROM AUTHOR]

[Display omitted] • Marigold petals are the primary industrial source of lutein. • An efficient green process described for isolating high purity lutein from marigold petals. • The process does not require recrystallization for further purification of free lutein. • The process does not use toxic solvents, high temperatures, acid, etc. • 2-MeTHF appears as a potential alternative solvent to hexane for lutein extraction. Marigold (Tagetes erecta L.) petals are the primary industrial source of lutein, which is used as a colouring agent and nutrient supplement to foods. This research extracted marigold petals using different solvents, covering conventional and non-toxic green solvents. The oleoresin, free lutein, and recrystallized lutein yields varied from 8.47–16.67%, 2.56–9.62%, and 1.11–1.61%, respectively. The purity of lutein was achieved up to 92.57% and 97.64% in conventional and newly established green methods, respectively. The present study described an efficient green process to isolate lutein with significantly improved yield (2.56%) and purity (97.33%) over the conventional methods. Based on the results, 2-methyltetrahydrofuran could be a practical green alternative to the traditional toxic solvents for the processing of lutein. Further, the chemical analysis of the essential oil of the residual receptacles obtained after removing petals revealed the presence of important organic volatiles, including piperitone (54.7%) and piperitenone oxide (6.5%), indicating its usefulness for value-addition. [ABSTRACT FROM AUTHOR]

Rose-scented geranium (Pelargonium graveolens L'Herit. ex Aiton), belonging to the family Geraniaceae, has gained considerable attention because of its fragrance and high economic value. The compositional complexity of rose-scented geranium essential oil (GEO) has been challenging for quality control. In this study, the chemical profiles of GEOs extracted from Indian cultivars/genotypes were developed using polarity-based fractionation, followed by characterization using a combination of gas chromatography (GC-FID), gas chromatography-mass spectrometry (GC-MS), and nuclear magnetic resonance spectroscopy (NMR). The analysis led to the identification of 121 compounds. Major components of the GEOs were citronellol (22.4–42.2 %), geraniol (5.7–30.5 %), linalool (2.1–9.8 %), citronellyl formate (4.0–9.5 %), isomenthone (5.3–7.5 %), geranyl formate (2.0–5.1 %), 6,9-guaiadiene (0.0–4.3 %), 10- epi - γ -eudesmol (0.2–6.4 %), 2-phenyl ethyl tiglate (1.0–2.1 %), geranyl tiglate (1.4–2.7 %), germacrene D (0.8–1.7 %) and geranial (0.4–1.6 %). This study identified effective markers which could help determine the authenticity of Indian cultivars/genotypes. Physical properties and chromatographic profiles of GEOs and terpeneless GEOs (TLOs) derived from Indian cultivar/genotype were compared. The two-step chromatographic separation coupled with principal component analysis allowed the identification of possible markers. The presence or absence of the sesquiterpenes, namely 10- epi - γ -eudesmol, 6,9-guaiadiene, and some other minor constituents, physical, and organoleptic properties, could effectively distinguish and define the quality of Indian cultivars/genotypes. Besides, the GEOs and TLOs prepared from different cultivars exhibited significant antimicrobial activity against Staphylococcus aureus and Candida albicans. [Display omitted] • Rose-scented geranium essential oil is known for its chemical complexity. • Chemical characterization and quality control of Indian genotypes were done. • Fractionation followed by GC-MS analysis led to the separation of co-eluting components. • The compounds identified could be viable tools for genotypes authentication. • Indian genotypes meet international standards. [ABSTRACT FROM AUTHOR]

This paper reports comparative extraction efficiencies and enrichment methods for natural insecticidal compounds pyrethrins from the dried flowers of Chrysanthemum cinerariaefolium using different techniques and solvent systems. Four different extraction techniques viz. percolation, agitation with heat, sonication and soxhlet using five different solvent systems hexane, ethyl acetate, acetone, acetonitrile and methanol were evaluated. In these studies, it was observed that maximum extract yield was obtained using methanol as extracting solvent by soxhlet technique, although the content of total pyrethrins was higher in the hexane extract than in methanol. The successive and maximum enrichment of the total pyrethrins was achieved by solid-matrix partitioning of the extract using acetonitrile as extracting solvent followed by treatment with activated charcoal, subsequent chilling and filtration by which enrichment of total pyrethrins up to 60.37% content was obtained. The quantitative analysis of the extraction and enrichment development protocol was validated by a simple, accurate, reproducible RP-HPLC-UV method using a binary gradient elution comprising of acetonitrile and water. The separation was achieved on a Waters-symmetry C 18 column (150 mm × 3.9 mm i.d., 5 μm) that achieved a greater degree of linearity within an overall concentration range of 5–500 μg mL −1 and higher degree of correlation (0.9842 ≤ r 2 ≤ 0.9987) for all the pyrethrin esters. [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]

Biotransformation of artemisinin (1) with the selected hairy root clones of three medicinally important plants, i.e ., Atropa belladonna, Hyoscyamus muticus and Ocimum basilicum , yielded two biotransformed products, which were identified as 3-α-hydroxy-1-deoxyartemisinin (2) and 4-hydroxy-9,10-dimethyloctahydrofuro-(3,2-i)-isochromen-11(4 H )-one (3). Their structures were elucidated through spectroscopic analysis (NMR/MS) and X-ray crystallography. The relative transformation efficiencies of the tested hairy root clones differed concerning individual bioconversion reactions. Consequently, the HR clones of H. muticus and A. belladonna accomplished the highest conversion of ( 1 ) to ( 2 ) and ( 3 ) respectively, while that of O. basilicum imparted an intermediate response. In-silico and in-vitro bioactivity analysis of the derivatives revealed promising anti-plasmodial activity profile in tandem with notable TNF level lowering potential of compound ( 2 ), indicating thereby its prospective therapeutic merit in ameliorating the severity of malarial infection. [ABSTRACT FROM AUTHOR]

Experimental activity of a compound on cancer cell line/target is mostly analyzed in the form of percentage inhibition at different concentration gradient and time of incubation. In this study a statistical model has been developed referred as in silico assay using support vector regression model, which can act with change in concentration gradient and time of incubation. This model is a function of concentration gradient, treatment hour and independent components; which calculate the percentage inhibition in combination of above three components. This model is designed to screen tetracyclic triterpenoids active against human breast cancer cell line MCF7. The model has been statistically validated, checked for applicability domain and predicted results were reconfirmed by MTT assay, for example Oenotheranstrol derivatives, OenA & B. Computational SAR, target and docking studies were performed to understand the cytotoxic mechanism of action of Oenotheranstrol compounds. The proposed in silico assay model will work for specific chemical family for which it will be optimized. This model can be used to analyze growth kinetics pattern on different human cancer cell lines for designed compounds. [ABSTRACT FROM AUTHOR]

Highlights: [•] Isolation of new compounds from the roots of Oenothera biennis. [•] Two new compounds identified as dihydroxyprenyl xanthone acetylated and cetoleilyl diglucoside. [•] Study of antioxidant activities of new and previously isolated compounds. [•] The compounds were investigated for the antioxidant effects using several different methods. [ABSTRACT FROM AUTHOR]

The essential oil obtained by hydro distillation of flowers of Bauhinia variegata were analyzed by GC and GC-MS analysis. Fifty one compounds have been identified in the flowers oil, representing 87.3% of total oil. The major components were identified as α-pinene (5.1%), β-pinene (2.2%), β-elemene (2.6%), γ-elemene (19.0%), δ-cadinene (3.6%), occidentalol (2.3%), cis-murrol-5-en-4-α-ol (24.4%) and α-cadinol (4.4%). This is the first report on chemical composition of B. variegata flowers essential oil of north Indian origin. [ABSTRACT FROM AUTHOR]

4-chloro eugenol (4CE), a semisynthetic analog of phytomolecule eugenol exhibited potent antiplasmodial activity with IC 50 in the range of 1.5–5 μM against sensitive as well as drug resistant strain of P. falciparum. This analog also showed synergy with a clinically used antimalarial drug artesunate and was able to curtail the IC 50 of artesunate up to 4–5 folds. Although, 4CE did not show any effect on heme polymerization, the most common drug target in the malaria parasite, it could increase the level of reactive oxygen species (ROS) and reactive nitrogen species (RNS) alone as well as in combination with artesunate. Further, 4CE induced oxidative stress was observed to affect the macromolecules in terms of DNA damage, protein carbonylation and lipid peroxidation. At the physiological level, cellular organelles like mitochondria and endoplasmic reticulum were observed to be get affected by 4CE in terms of membrane depolarization and calcium ion leakage respectively. These observations could be validated by expression analysis of oxidative stress responsive genes and proteins. Further, in in vivo assay, 4CE showed significant chemo-suppression of parasitemia as well as an increase in mean survival time in the murine malaria model. Interestingly, in combination with artesunate, 4CE showed higher chemo-suppression as well as enhanced mean survival time at a much lower concentrations of both the partners as compared to an individual dose of artesunate and 4CE. A combination of 4CE and artesunate was also observed to attenuate cerebral malaria pathogenesis. [ABSTRACT FROM AUTHOR]

Lavender oil (LO) is an aromatic/essential oil extracted from Lavandula angustifolia and traditionally used as an aromatherapy massage oil due to its anti-inflammatory and wound healing property and also for providing the relief in other skin conditions such as psoriasis, dermatitis and eczema. However, LO has not been evaluated scientifically for psoriasis like skin inflammation. This study was aimed to investigate the LO and its major components linalool (L) and linalyl acetate (LA) against psoriasis like skin inflammation. Anti-psoriatic activity was done using Imiquimod (IMQ) induced psoriasis like skin inflammation in BALB/c mice. Assessment of anti-psoriatic effect of LO, L and LA was done on the basis of change in ear thickness, psoriasis area severity index (PASI) scoring at alternative day, CosCam scoring using skin analyzer equipped with SkinSys software, biochemical, immunohistochemical and histological investigations. Level of effectiveness against psoriasis was investigated by percent reduction in PASI scores, CosCam scores and level of Th-1 and Th-17 cell expressing cytokines, as compared to the diseased mice. Topical application of LO 10% showed 73.67% recovery in PASI and 87% in Th-17 cell-specific cytokines towards normal as compared to disease group. L and LA were identified as the major components of LO and favoured ligands for selected psoriasis targets. At 2% topical dose, L and LA showed 64% and 47.61% recovery in PASI scores, respectively. Both, L and LA showed significant recovery in Th-1 specific TNF-α and IL-1β however, only L showed significant recovery of Th-17 cytokines (IL-17 and IL-22). In contrast to LA (which restored granulosis), L restored epidermal hyperplasia and parakeratosis toward the normal condition. On the other hand, L also reduced the expression of NF-κβ, ccr6 and IL-17, while LA reduced the expression of NF-κβ only. At 10% topical dose, LO was observed to be slight irritant while at 2% topical dose, L and LA were found non-irritant to the skin. This study proves the effectiveness of LO and its major phytoconstituents linalool and linalyl acetate against IMQ induced psoriasis like skin inflammation and provides the scientific evidence for topical use of lavender oil. Image 1 [ABSTRACT FROM AUTHOR]

A series of substituted 8,8-dimethyl-8 H -pyrano[2,3- f ]chromen-2-ones (chromeno-coumarin hybrids) was synthesized from scopoletin (11) as vasorelaxing agents. The synthesized compounds 21a-f, 22, 23a-e and scopoletin (11) were evaluated for vasorelaxation in endothelium intact rat main mesenteric artery (MMA). Compounds 11 , 21a , 21c - f and 22 showed significant vasorelaxation in precontracted MMA within the range of EC 50 value 1.58–5.02 µM. These derivatives presented 29.40–70.89 fold increased sensitivity for experimental tissue compared to scopoletin (11), the parent molecule. Among others, 22 was found to be the most active compound which had EC 50 1.58 µM with 70.89 fold increased sensitivity. The mechanistic evaluation of 22 showed that it exerted vasorelaxation through Ca2+-activated K+ (BKca) channel and the effect was endothelium-independent. [ABSTRACT FROM AUTHOR]