Neuroinflammation and acetylcholinesterase inhibition potentials of acyclic monoterpenoids isolated from Cymbopogon distans (Nees ex Steud.) Will. Watson.

Cymbopogon distans (Nees ex Steud.) Will. Watson (Poaceae) is a promising aromatic plant distributed in the Himalayas. In this study, five acyclic monoterpenoids, namely geranyl acetate (RS1), neral (RS2), geranial (RS3), citral (RS4) and geraniol (RS5) were isolated from the essential oil of C. distans. The isolated compounds were tested for in-vitro neuroinflammation inhibitory potential in LPS-stimulated BV2 microglial cells. RS1-RS4 exhibited significant neuroinflammation inhibition without any cytotoxic effect at the dose of 10 µM. RS4, the most active anti-neuroinflammatory compound (TNF-α 31.48 ± 1.00%; IL-6 24.02 ± 0.63%; IL-1ß 42.15 ± 1.76%) was also able to inhibit acetylcholinesterase (AChE) in a dose-dependent manner. The results showed that RS4 (an isomeric mixture of neral and geranial) has the potential to inhibit neuroinflammation and AChE, which are the biomarkers of neurodegenerative disorders.

Cu-catalyzed click reaction in synthesis of eugenol derivatives as potent antimalarial agents.

Eugenol(1), a terpenoid found in Ocimum, has various biological activities. The present study aims at extraction, isolation of the plant secondary metabolite eugenol (1), it's derivatisation and structure identification as bioactive molecules. Synthesis and antiplasmodial activity (in-vitro and in-vivo), of a series of fourteen novel eugenol-based 1,2,3-triazole derivatives was done in the present study. Derivatives 5a-5n showed good antimalarial activity against the strain Plasmodium falciparum NF54. Derivative 5 m, IC50 at 2.85 µM was found to be several times better than its precursor 1 (106.82 µM) whereas the derivative 5n showed three fold better activity than compound 1, in vitro. The structure-activity relationship of the synthesised compounds indicated that the presence of triazole ring in eugenol analogues is responsible for their good activity. Compound 5m, was further evaluated for in-vivo antimalarial activity which showed about 79% parasitemia suppression. It is the first report on antimalarial activity of triazole eugenol derivatives.

An Updated Insight into Phytomolecules and Novel Approaches used in the Management of Breast Cancer.

Breast cancer is a widespread condition that kills more women from cancer-related causes than any other type of cancer globally. Women who have estrogen-dependent, initial metastatic breast cancer frequently receive treatment with surgery, radiation therapy, and chemotherapy. They may also get more specialized treatments like tamoxifen or aromatase inhibitors (anastrozole or letrozole). The World Health Organisation reported in 2012 that by 2030, breast cancer will be more common worldwide. There are several phytochemicals, such as isoflavones, coumestans, lignans, and prenylflavonoides. Isoflavones have been shown in studies to prevent the spread of breast cancer and to trigger apoptosis. Targeting BCs in metastatic breast cancer may be made possible by combining well-formulated phytochemicals in nanoparticles or other novel drug delivery agents with currently accepted endocrine and/or conventional chemotherapies. Cell signaling, regulation of cell cycles, oxidative stress action, and inflammation could be positively impacted by phytoconstituents. They have the ability to alter non-coding RNAs, to prevent the proliferation and regeneration of cancer cells. The availability of novel approaches helps in disease targeting, safety, effectiveness and efficacy. The current literature helps to know the available drugs i.e. phytoconstituents or novel drug delivery like nanoparticle, microsphere, micelles, liposomes and neosomes. The literature has been taken from PubMed, Google Scholar, SciFinder, or other internet sites.

An Insight of Naturally Occurring Phytoconstituents and Novel Approaches Towards the Treatment of Diabetes.

BACKGROUND: The rising in diabetes incidents has clearly become one main worldwide health problem. Individuals suffering from diabetes are still more susceptible to many long-term and short-term side effects, which most often cause fatalities. Even though chemically synthesized anti-diabetic entities are capable of helping manage and treat, there has been significant risks related with their prolong and repetitive use. Hence, there is a requirement for safer and novel approaches that might be formed and utilized. OBJECTIVE: Aim of the present review is to explain the naturally occurring phytochemicals and novel approach as anti-diabetic agents in the treatment of diabetes and its related issues. METHOD: A survey of Google scholar, Research Gate, Pubmed, Science Direct, NCBI database was carried out conducted to determine a most hopeful phytochemicals and novel drug delivery systems in the management of diabetes. RESULT: The study stressed the significance of phytomolecules and some novel approaches researched or reported in the literature for the management and cure of diabetes. It is suggested that changes in lifestyle can help patients and like nutritional support, assessment and lifestyle guidance must be individualized based on physical and functional capacity. Further evaluations and improved preventative medicine were the result of improving patient outcomes. CONCLUSION: Conventional or synthetic drugs provide relief for short time but nanoformulations of phytomolecules offer an improved therapeutic with fewer negative side effects. Herbal medicines are rich in phytoconstituents and possess variety of health benefits. This review is compilation of phytoconstituents and novel drug delivery system of phytomolecules i.e. nanoparticles, niosomes, microsphere, microparticle and others.

Synthesis of 6-alkoxy and 6-hydroxy-alkyl amine derivatives of braylin as vasorelaxing agents.

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.

Liquiritigenin, isoliquiritigenin rich extract of glycyrrhiza glabra roots attenuates inflammation in macrophages and collagen-induced arthritis in rats.

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.

Taxoids-rich extract from Taxus wallichiana alleviates high-fat diet-induced insulin resistance in C57BL/6 mice through inhibition of low-grade inflammation.

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.

Pharmacological and Toxicological Study of Coumarinolignoids from Cleome viscosa in Small Animals for the Management of Rheumatoid Arthritis.

This study aims to explore the possible pharmacological potential of Cleome viscosa Linn (Cleomaceae), an annual weed, into therapeutic value-added products. In the present study, we have explored the pharmacological and toxicological profile of coumarinolignoids isolated from Cleome viscose for the management of rheumatoid arthritis and related complications in a small animal model. To avoid the biasness during experiments on animals, we have coded the isolated coumarinolignoids as CLIV-92 to perform the experimental pharmacological study. CLIV-92 was orally administrated (30,100, 300 mg/kg) to animal models of collagen-induced arthritis (CIA), carrageenan-induced acute inflammation, thermal and chemical-induced pain, and Brewer's yeast-induced pyrexia. Oral administration of CLIV-92 significantly decreases the arthritis index, arthritis score, and increases the limb withdrawal threshold in the CIA model in experimental rats. The anti-arthritis studies revealed that the anti-inflammatory effect of CLIV-92 was associated with inhibition of the production of inflammatory mediators like TNF-α, IL-6, IL-17A, MMP-1, MMP-9, Nitric oxide, and C-RP in CIA rat's serum, and also reduced the NFкB-p65 expression as evidence of immunohistochemistry in knee joint tissue of CIA rats, in a dose-dependent manner. Further individual experiments related to arthritis-related complications in experimental animals demonstrated the analgesic, anti-inflammatory, and antipyretic potential of CLIV-92 in a dose-dependent manner. Further, an in-vivo acute oral toxicity study concluded that CLIV-92 is safe in experimental animals up to 2,000 mg/kg dose. The results of this study suggested that the oral administration of CLIV-92 may be a therapeutic candidate for further investigation in the management of rheumatoid arthritis and related complications.

Corrigendum: Calliterpenone, a natural plant growth promoter from a medicinal plant Callicarpa macrophylla, sustainably enhances the yield and productivity of crops.

[This corrects the article DOI: 10.3389/fpls.2022.960717.].

Linalool reduces the virulence of Pseudomonas syringae pv. tomato DC 3000 by modulating the PsyI/PsyR quorum-sensing system.

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.

Towards the development of phytoextract based healthy ageing cognitive booster formulation, explored through Caenorhabditis elegans model.

The positive effect of herbal supplements on aging and age-related disorders has led to the evolution of natural curatives for remedial neurodegenerative diseases in humans. The advancement in aging is exceedingly linked to oxidative stress. Enhanced oxidative stress interrupts health of humans in various ways, necessitating to find stress alleviating herbal resources. Currently, minimal scientifically validated health and cognitive booster resources are available. Therefore, we explored the impact of plant extracts in different combinations on oxidative stress, life span and cognition using the multicellular transgenic humanized C. elegans, and further validated the same in Mus musculus, besides testing their safety and toxicity. In our investigations, the final product-the HACBF (healthy ageing cognitive booster formulation) thus developed was found to reduce major aging biomarkers like lipofuscin, protein carbonyl, lipid levels and enhanced activity of antioxidant enzymes. Further confirmation was done using transgenic worms and RT-PCR. The cognitive boosting activities analyzed in C. elegans and M. musculus model system were found to be at par with donepezil and L-dopa, the two drugs which are commonly used to treat Parkinson's and Alzheimer's diseases. In the transgenic C. elegans model system, the HACBF exhibited reduced aggregation of misfolded disease proteins α-synuclein and increased the health of nicotinic acetylcholine receptor, levels of Acetylcholine and Dopamine contents respectively, the major neurotransmitters responsible for memory, language, learning behavior and movement. Molecular studies clearly indicate that HACBF upregulated major genes responsible for healthy aging and cognitive booster activities in C. elegans and as well as in M. musculus. As such, the present herbal product thus developed may be quite useful for healthy aging and cognitive boosting activities, and more so during this covid-19 pandemic. Supplementary Information: The online version contains supplementary material available at 10.1007/s13237-022-00407-1.

Calliterpenone, a natural plant growth promoter from a medicinal plant Callicarpa macrophylla, sustainably enhances the yield and productivity of crops.

The global population is rising at an alarming rate, which is threatening food and nutritional security. Although chemical fertilizers and pesticides are important for achieving food security, their excessive usage critically affects soil health and adds up residues in the food chain. There is an increasing interest in identifying eco-friendly farm inputs that can improve crop productivity through sustainable agricultural practices. One of the most common approaches to reducing chemical inputs in agriculture is the use of plant growth regulators (PGRs). Here, we demonstrate the benefits of a natural and novel plant growth enhancer "calliterpenone," isolated from Callicarpa macrophylla, a medicinal plant, for increasing crop productivity in six crops, viz., rice, wheat, potato, tomato, chickpea, and onion. Results revealed that the application of calliterpenone (foliar spraying or seed soaking) enhanced the yield of rice (28.89%), onion (20.63%), potato (37.17%), tomato (28.36%), and chickpea (26.08%) at 0.001 mM and of wheat (27.23%) at 0.01 mM concentrations in comparison to control. This enhancement in yield was reflected through improvements in its growth attributes, viz., spike length, tillers plant-1, seeds spike-1, plant height, and biomass. Furthermore, the exogenous application of calliterpenone could increase the endogenous level of indole-3-acetic acid (IAA) in all tested crops and decrease the content of abscisic acid (ABA) in a few. Trials conducted at farmers' fields showed an overall ~12% increase in rice yield (mean of 11 farmers' fields ranging from 3.48 to 19.63%) and ~10% increase in wheat yield (ranging from 3.91 to 17.51%). The 0.001 mM of calliterpenone was the best effective dose for most crops except wheat, where a concentration of 0.01 mM was found to be the most optimal. This study indicates that calliterpenone is a natural plant growth promoter that can be used in boosting the yields of multiple crops and would be an important input component of organic farming.

An efficient process for the extraction of lutein and chemical characterization of other organic volatiles from marigold (Tagetes erecta L.) flower.

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-methyltetrahydrofurancould 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.

Chemical composition and antimicrobial activity of the leaf essential oil of Ravenia spectabilis Engl. (Rutaceae).

Ravenia spectabilis Engl. belongs to the family Rutaceae is known to possess several biologically active phytomolecules. This study was planned to investigate the chemical composition and antimicrobial activity of the leaf essential oil of R. spectabilis. The hydrodistillation of fresh leaves of R. spectabilis gave 0.19 ± 0.02% essential oil. The resulting essential oil was analysed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Altogether, thirty-one constituents forming 97.6 ± 1.72% of the total oil composition were identified. Major components of the oil were sabinene (60.8 ± 0.36%), α-pinene (5.4 ± 0.30%), myrcene (4.8 ± 0.25%), δ-3-carene (4.7 ± 0.62%) and ß-pinene (4.3 ± 0.17%). The in-vitro antimicrobial potential of the oil was examined against eight human pathogenic bacterial and fungal strains. The essential oil showed significant activity against Staphylococcus aureus, Staphylococcus epidermidis, methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Candida albicans, and Candida kefyr. This is the first report on R. spectabilis leaf essential oil composition and its antimicrobial activity. The essential oil could be a promising natural source of sabinene and antimicrobial for developing new phytotherapeutics.

New Insights into the Chemical Composition, Pro-Inflammatory Cytokine Inhibition Profile of Davana (Artemisia pallens Wall. ex DC.) Essential Oil and cis-Davanone in Primary Macrophage Cells.

Artemisia pallens Wall. ex DC., popularly known as davana, has gained considerable attention because of its unique fragrance, high economic value, and pharmacological properties. The compositional complexity of davana essential oil (DO) has been a challenge for quality control. In this study, the chemical profile of DO was developed using polarity-based fractionation and a combination of gas chromatographic (GC-FID), hyphenated chromatographic (GC/MS), and spectroscopic (Fourier-Transform Infra-Red, 1D, 2D-Nuclear Magnetic Resonance) techniques. The analysis led to the identification of ninety-nine compounds. Major components of the DO were cis-davanone (D3, 53.0 %), bicyclogermacrene (6.9 %), trans-ethyl cinnamate (4.9 %), davana ether isomer (3.4 %), spathulenol (2.8 %), cis-hydroxy davanone (2.4 %), and trans-davanone (2.1 %). The study led to identifying several co-eluting novel minor components, which could help determine the authenticity of DO. The rigorous column-chromatography led to the isolation of five compounds. Among these, bicyclogermacrene, trans-ethyl cinnamate, and spathulenol were isolated and characterized by spectroscopic methods for the first time from DO. Pharmacological profile revealed that the treatment of DO and D3 inhibited the production of pro-inflammatory cytokines (TNF-α, IL-6) induced by lipopolysaccharide (LPS) in primary macrophages without any cytotoxic effect after administration of their effective concentrations. The result of this study indicates the suitability of DO and D3 for further investigation for the treatment of chronic skin inflammatory conditions.

Cliv-92-Loaded Glycyrrhetinic Acid-Modified Chitosan Nanoparticles for Enhanced Hepatoprotection-Preparation, Characterization, and In Vivo Evaluation.

Cliv-92 is a mixture of three structurally similar coumarinolignoids and a proven hepatoprotective agent. Low aqueous solubility and poor bioavailability are notable hindrances for its further use. Therefore, glycyrrhetinic acid-linked chitosan nanoparticles loaded with Cliv-92 were prepared for active targeting to the liver. The nanoparticles were prepared by the ionic gelation method to avoid the use of toxic solvents/rigorous agitation. The method of preparation was optimized using a central composite design with independent variables, namely polymer: drug ratio (3:1, w/w), crosslinker concentration (0.5%), and stirring speed (750 rpm). The optimized nanoparticles had a mean particle size of 185.17 nm, a polydispersity index of 0.41, a zeta potential of 30.93 mV, and a drug loading of 16.30%. The prepared formulation showed sustained release of approximately 63% of loaded Cliv-92 over 72 h. The nanoparticles were freeze-dried for long-term storage and further characterized. The formulation was found to be biocompatible for parenteral delivery. In vivo imaging study showed that optimized nanoparticles were preferentially accumulated in the liver and successfully targeting the liver. The present study successfully demonstrated the improved pharmacokinetic properties (≈12% relative bioavailability) and efficacy profile (evidenced by in vivo and histopathological studies) of fabricated Cliv-92 nanoparticles.

4-Chlorothymol Exerts Antiplasmodial Activity Impeding Redox Defense System in Plasmodium falciparum.

Malaria remains one of the major health concerns due to the resistance of Plasmodium species toward the existing drugs warranting an urgent need for new antimalarials. Thymol derivatives were known to exhibit enhanced antimicrobial activities; however, no reports were found against Plasmodium spp. In the present study, the antiplasmodial activity of thymol derivatives was evaluated against chloroquine-sensitive (NF-54) and -resistant (K1) strains of Plasmodium falciparum. Among the thymol derivatives tested, 4-chlorothymol showed potential activity against sensitive and resistant strains of P. falciparum. 4-Chlorothymol was found to increase the reactive oxygen species and reactive nitrogen species level. Furthermore, 4-chlorothymol could perturb the redox balance by modulating the enzyme activity of GST and GR. 4-Chlorothymol also showed synergy with chloroquine against chloroquine-resistant P. falciparum. 4-Chlorothymol was found to significantly suppress the parasitemia and increase the mean survival time in in vivo assays. Interestingly, in in vivo assay, 4-chlorothymol in combination with chloroquine showed higher chemosuppression as well as enhanced mean survival time at a much lower concentration as compared to individual doses of chloroquine and 4-chlorothymol. These observations clearly indicate the potential use of 4-chlorothymol as an antimalarial agent, which may also be effective in combination with the existing antiplasmodial drugs against chloroquine-resistant P. falciparum infection. In vitro cytotoxicity/hemolytic assay evidently suggests that 4-chlorothymol is safe for further exploration of its therapeutic properties.

4-chloro eugenol interacts synergistically with artesunate against drug resistant P. falciparum inducing oxidative stress.

4-chloro eugenol (4CE), a semisynthetic analog of phytomolecule eugenol exhibited potent antiplasmodial activity with IC50 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 IC50 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.

New chemical constituent from the stem of Cuscuta reflexa Roxb. and its biological activities.

Chemical investigations on the stem of Cuscuta reflexa Roxb. (Convolvulaceae) led to the isolation of one new compound characterised as 3',4'-dimethoxy-1-phenyl-1α, 2-ethanediol (1), along with eight known compounds as tridecanyl palmitate, palmitic acid, n-pentatriacontane, n-triacont-21, 27-dien-1-ol, kaempherol, chlorogenic acid, 5,7-dimethoxyapigenin and quercitin. The chemical structures were established with the help of physical, chemical and spectroscopic methods. The antimicrobial potential of the new compound (1) was evaluated against three bacterial and three fungal pathogenic strain and showed significant activities.

Chemical composition, bactericidal kinetics, mechanism of action, and anti-inflammatory activity of Isodon melissoides (Benth.) H. Hara essential oil.

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.