Chemical composition and mosquitocidal properties of essential oil from Indian indigenous plants Ocimum tenuiflorum L. and Ocimum americanum L. against three vector mosquitoes.

Mosquitoes stand out as the most perilous and impactful vectors on a global scale, transmitting a multitude of infectious diseases to both humans and other animals. The primary objective of the current research was to assess the effectiveness of EOs from Ocimum tenuiflorum L. and Ocimum americanum L. in controlling Anopheles stephensi Liston. Culex quinquefasciatus Say and Aedes aegypti L. mosquitoes. The larvae, pupae and eggs of the mosquitoes were exposed to four different concentrations (6.25-50 ppm). The tested EOs resulted in >99-100 % mortality at 120 h for the eggs of all examined mosquito species. It also showed robust larvicidal and pupicidal activity with LC50 and LC90 values of 17-39, 23-60 ppm and 46-220, and 73-412 ppm against Aedes, Culex and Anopheles mosquito species, respectively, at 24 h of treatment. The Suitability Index or Predator Safety Factor demonstrated that the EOs extracted from O. tenuiflorum L. and O. americanum L. did not cause harm to P. reticulata, D. indicus (water bug), G. affinis and nymph (dragonfly). GC-MS analysis identified the major probable constituents of the oil, including Phenol, 2-Methoxy-4-(1-Propenyl)- (28.29 %); 1-Methyl-3-(1'-Methylcyclopropyl) Cyclopentene (46.46 %); (E,E,E)-3,7,11,15-Tetramethylhexadeca-1,3,6,10,14-Pentaene (18.91 %) and 1,3-Isobenzofurandione, 3a,4,7,7a-Tetrahydro-4,7-Dimethyl (33.02 %). These constituents may play a significant role in the mosquitocidal activity of the oil. The same results were identified in the formulation prepared from the EOs. This marks the first report confirming the successful utilization of EOs derived from O. tenuiflorum L. and O. americanum L. in mosquito population control initiatives.

Role of Polyphenols in Alleviating Alzheimer's Disease: A Review.

Alzheimer's Disease (AD) is a successive neurodegenerative disorder in the aged population. Many chemicals and phytochemicals are used to treat AD. Polyphenols which occur widely in various fruits, vegetables, beverages, and some other plant sources are gaining importance in AD treatment. Polyphenols comprise various subcategories, such as phenolic acids, lignans, tannins, stilbenes, hydroxybenzoic acid, hydroxycinnamic acid, and flavonoids. These compounds, as sole entities or in combination, can be used for treating AD because they have an abundance of antioxidants that are reported to be effective in free radical scavenging, metal ion chelating, and anti-inflammatory activities. Polyphenols of various plant origins have been studied, and these have been supported by in vitro assays and in vivo studies in rodents. These molecules protect neurons against oxidative stress and deposition of amyloid-ß (Aß) and tau proteins which play a vital role in the pathogenesis of AD. Consumption of wine and other foods rich in polyphenols has a beneficial effect on the neuronal signaling pathways, playing a vital role in shielding neuronal cells from neurodegeneration. Their ability to reduce free radicals and chelate metals are of great advantage. In this review, we highlight the various polyphenols that inhibit neuronal damage and progression of AD while also providing a cure. Some of the polyphenols covered are hesperidin, resveratrol, curcumin, catechin, kaempferol, and quercetin. The mechanisms of the actions of three polyphenols are also elaborated.

The Anticancer Efficacy of Thiourea-Mediated Reduced Graphene Oxide Nanosheets against Human Colon Cancer Cells (HT-29).

The current research focuses on the fabrication of water-soluble, reduced graphene oxide (rGO) employing thiourea (T) using a simple cost-effective method, and subsequently examining its anticancer characteristics. The cytotoxicity caused by graphene oxide (GO) and T-rGO is investigated in detail. Biological results reveal a concentration-dependent toxicity of GO and T-rGO in human colon cancer cells HT-29. A decrease in cell viability alongside DNA fragmentation is observed. Flow cytometry analysis confirms the cytotoxic effects. The novelty in this work is the use of raw graphite powder, and oxidants such as KMNO4, NaNO3, and 98 percent H2SO4 to produce graphene oxide by a modified Hummers method. This study demonstrates a simple and affordable procedure for utilising thiourea to fabricate a water-soluble reduced graphene oxide, which will be useful in a variety of biomedical applications.

Computational analysis of single nucleotide polymorphisms (SNPs) in PPAR gamma associated with obesity, diabetes and cancer.

The single nucleotide polymorphisms (SNPs) are the common genetic variations in human genomes and act as markers for molecular susceptibility of complex traits and diseases in humans. Amino acid variations in the non-synonymous SNPs (nsSNPs) in coding and non-coding regions affect the function/structure of the proteins. The Peroxisome proliferator-activated receptor gamma (PPARγ or PPARG) is a nuclear receptor that plays a significant role in lipid metabolism and insulin production and is associated with diabetes, obesity, and cancer. In this study, the PPARG sequence was retrieved from the NCBI database (dbSNP: NP_619726.2), and an analysis was done to predict the damaged/harmful mutated amino acids. We identified five mutated variants (C162S, R166W, Q286P, or Q314P and P467L), which were mostly expressed in cancer tissues and associated with insulin resistance and partial lipodystrophy. The identified mutations were induced, and the analysis of molecular dynamics simulation was established to determine the dynamic stability/flexibility of PPARG. The dynamic trajectories were analyzed by RMSD, RMSF, and Radius of Gyration (Rg) analysis; a vast difference was noticed in each of the protein structure when compared with the PPARG wild-type, and the mutations in PPARG impaired its functions, leading to more significant problems in humans.Communicated by Ramaswamy H. Sarma.

Antidiabetic with antilipidemic and antioxidant effects of flindersine by enhanced glucose uptake through GLUT4 translocation and PPARγ agonism in type 2 diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants have been used by the people of developing countries to treat various diseases. WHO also recommends the use of medicines from plants source. In that, diabetes also one of the diseases that have been treated traditionally by several people all over the world. In India, Toddalia asiatica (L.) Lam. (Rutaceae) is also a medicinal plant used traditionally for the treatment of diabetes in Ayurveda. Moreover, T. asiatica is also used in a polyherbal formulation to treat diabetes. AIM OF THE STUDY: This study examined the antidiabetic with antilipidemic and antioxidant effects of flindersine isolated from T. asiatica leaves. MATERIALS AND METHODS: Diabetes was induced in Wistar rats by feeding a high-fat diet (HFD) for 15 days and injecting a single dose of 40 mg/kg b. wt. of Streptozotocin (STZ). Five days post-injection, the grouped diabetic rats were treated with 20 and 40 mg/kg of flindersine. RESULTS: Flindersine resulted in a clear decline of blood glucose levels during 28 days of treatment in two different doses. Flindersine also significantly (P ≤ 0.05; P ≤ 0.005) reduced the body weight gain, plasma insulin concentration, urea, creatinine, total cholesterol (TC), triglycerides (TG) and free fatty acids (FFA) levels and significantly increased (P ≤ 0.05; P ≤ 0.005) the total protein level, superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) activities compared to the standard drug, pioglitazone. Additionally, flindersine restored the glucose transporter protein 4 (GLUT4), adenosine monophosphate protein kinase (AMPK) and peroxisome proliferator-activated receptor γ (PPARγ) expressions in adipose tissues and skeletal muscles. CONCLUSION: It has been found that flindersine has potent antilipidemic and antidiabetic activities by improving insulin sensitivity by enhancing the phosphorylation of AMPK, GLUT4 translocation, and PPARγ agonism on adipose tissue and skeletal muscles of diabetic rats.

Karyomorphological effects of two new oil formulations on Helicoverpa armigera (Hübner) (Lepidoptera: Noctuidae).

The cotton bollworm Helicoverpa armigera is a serious pest of many economically important crops. Since this pest has become resistant to the conventional synthetic insecticides, newer compounds and formulations are being developed against this insect pest. Many natural compounds isolated from the plants were tested against this pest. Among them Hyptis suaveolens and Melochia corchorifolia showed insecticidal properties against H. arnigera. Based on bioefficacy studies, caryophyllene and ß-sitosterol were isolated from H. suaveolens and M. corchorifolia respectively. The isolated natural compounds were further developed as formulations in various combinations with neem (Azadirachta indica) and karanj (Pongamia pinnata) oils. The present study indicated that the formulations influenced the karyomorphology of H. armigera.

Hepatoprotective effect of selected isoandrographolide derivatives on steatotic HepG2 cells and High Fat Diet fed rats.

Non-alcoholic Fatty Liver Disease (NAFLD) is one of the growing epidemics of the globe. This study was aimed to evaluate the anti-NAFLD effect of selected IAN derivatives using in silico, in vitro and in vivo models. In silico tools viz., DataWarrior, SwissADME and Gaussian 09 were used to predict the pharmacokinetic properties and electronic distribution patterns of the derivatives; docking analysis was done with Autodock against PPARα. Toxicities of the derivatives were assessed in HepG2 cells using MTT assay. Anti-NAFLD efficacies of the derivatives were assessed in free fatty acid induced steatotic HepG2 cells. In vivo anti-NAFLD effect of active isoandrographolide (IAN) derivative, 19-propionyl isoandrographolide (IAN-19P) was assessed in High Fat Diet fed rats. In silico and in vitro studies indicated that IAN-19P showed improved drug-likeness and drug score. The toxicity of IAN-19P to HepG2 cells was comparatively less than IAN and other derivatives. In free fatty acid induced steatotic HepG2 cells, treatment with IAN-19P significantly lowered intracellular triglyceride content and leakage of LDH and transaminases. Treating High Fat Diet fed animals with IAN-19P significantly lowered plasma lipids, transaminases, LDH and GGT levels. The treatment with IAN-19P upregulated the expressions of PPARα and CPT-1. IAN-19P did not produce any noticeable adverse effect till 2 g/kg concentration in acute and 250 mg/kg concentration in subacute toxicity studies. This study indicated the beneficial effect of IAN-19P for the treatment of NAFLD; however robust investigations are needed to establish the potential of IAN-19P to treat NAFLD.

Fucoidan serves a neuroprotective effect in an Alzheimer's disease model.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder that causes memory and cognitive deficits. The present study was carried out to evaluate the protective effects of fucoidan in monocrotophos induced AD in Drosophila melanogaster. In silico studies showed that fucoidan exhibited binding energy of -9.3 kcal with proteins. Consistent with this, fucoidan, in a dose and time-dependent fashion, had inhibitory activity against cholinergic and monoamine-metabolized enzymes in vitro. Fucoidan inhibited the increase in total mRNA and protein in monocrotophos fed flies and prevented changes in biochemicals, neurochemicals and latency time of locomotor, learning and memory induced by monocrotophos. Together, the findings show that fucoidan serves a neuroprotective effect in Alzheimer's disease model in D. melanogaster.

Roles of microRNA in prostate cancer cell metabolism.

MicroRNAs are non-coding RNA which functions as regulators of genes expression. MicroRNAs have shown their biological functions in cell proliferation, cell cycle, cell metabolism, apoptosis, invasion and metastasis. Cancer cells have the ability to grow in the absence of growth factors by increased metabolic activity. MicroRNAs regulate cell metabolic processes by targeting the key enzymes or transporters and change the metabolic activities by interfering with oncogenes/tumor suppressors, hypoxia, signalling pathways and cell adhesion. This review mainly explains the roles of microRNAs in prostate cancer cell metabolism, such as glucose uptake, glycolysis and lactate secretion, lipid metabolism and interaction with signalling pathways. The relation of microRNAs with hypoxia and cell adhesion in cell metabolism is also highlighted. Therefore, miRNAs help in regulating the metabolism of survived tumor cells, understanding such miRNA-mediated interaction could lead to new avenues in therapeutic application to treat PCa.

Larvicidal, Ovicidal, and Histopathological Effects of the Sulphur Polypore Mushroom, Laetiporus sulphureus (Agaricomycetes), Collected from Tamil Nadu, India against Mosquitoes.

This study was conducted to determine the mosquitocidal activity of 6 species of higher Basidiomycetes collected from various places in the state of Tamil Nadu, India. The mushrooms were identified using MycoKey MMI software. We used morphological characteristics such as size, color, height, width (of the cap, lamellae, stipe, and fruiting body), spore deposits, and the presence or absence of ring to identify species. Eggs and larvae of Culex quinquefasciatus and Anopheles stephensi were exposed to various concentrations (62.5, 125.0, 250.0, and 500.0 ppm) of extracts from the 6 mushrooms. The extracts were dissolved in dimethyl sulfoxide. Among the 6 mushrooms, the methanol extract of Laetiporus sulphureus showed high toxicity toward mosquitoes at different life stages, with 96% larvicidal activity against A. stephensi and 76% activity against C. quinquefasciatus. After 24 hours, we found half-maximal lethal concentrations of 155.862 ppm for A. stephensi and 227.225 ppm for C. quinquefasciatus, and 90% lethal concentrations of 424.128 ppm for A. stephensi and 1011.663 ppm for C. quinquefasciatus. The extracts also showed strong ovicidal activity against mosquito eggs: 100% activity against A. stephensi and 91% activity against C. quinquefasciatus were observed at an extract concentration of 500 ppm 120 hours after treatment. The methanol extract of L. sulphureus was tested for toxicity against a nontarget organism, but we found none. Histopathological studies of the treated larvae revealed serious damage to cells in the midgut. These results suggest that the methanol extract of L. sulphureus is a good natural source for controlling mosquitoes.

Comparative studies of tripolyphosphate and glutaraldehyde cross-linked chitosan-botanical pesticide nanoparticles and their agricultural applications.

A nanopesticide formulation was developed using chitosan and a botanical pesticide PONNEEM® and its antifeedant, larvicidal and growth regulating activities were screened against Helicoverpa armigera, a major lepidopteran pest. Chitosan nanoparticles (CSNs) were prepared by using two different cross-linking agents namely glutaraldehyde (GLA) and tripolyphosphate (TPP). The effects of cross linking agents on CSNs and the biological properties against the insect pest were also studied. Cross linking of chitosan with either TPP or GLA was confirmed through Fourier Transform Infrared (FTIR) spectroscopy. Electron micrograph revealed that the size of CSNs varied from 32 to 90nm. The stability of nanoparticles lasted for 9days in CSNs-TPP-PONNEEM. In CSNs-GLA-PONNEEM, the stability of nanoparticles was higher. CSNs-TPP-PONNEEM treatment recorded 88.5% antifeedant activity and 90.2% larvicidal activity against H. armigera. Weights of H. armigera pupae in CSNs-TPP-PONNEEM treatment were significantly low. Chitosan-based nano-pesticide formulation holds great promise in H. armigera management.

Toxic effect of Atalantia monophylla essential oil on Callosobruchus maculatus and Sitophilus oryzae.

The hydrodistillated essential oil of Atalantia monophylla was subjected to GC-MS. Forty compounds were presented in the essential oil. Eugenol (19.76 %), sabinene (19.57 %), 1,2-dimethoxy-4-(2-methoxyethenyl) benzene (9.84 %), beta-asarone (7.02 %) and methyl eugenol (5.52 %) were found the predominant compounds. The oil was tested for fumigant toxicity and repellent activity against Callosobruchus maculatus and Sitophilus oryzae. The development stage of C. maculatus fecundity, adult emergence and also ovicidal activities were studied by the treatment of A. monophylla oil. The oil exhibited considerable fumigation toxicity (70.22 %), repellent activity (85.24 %) and ovicidal activity (100 %) against C. maculatus. The oil significantly reduced the protein, esterase, acetylcholinesterase and glutathione S-transferase on C. maculatus and S. oryzae. It can be considered that A. monophylla has a potential insecticide against stored product pests.

Biocontrol Properties of Basidiomycetes: An Overview.

In agriculture, there is an urgent need for alternate ecofriendly products to control plant diseases. These alternate products must possess preferable characteristics such as new modes of action, cost effectiveness, biodegradability, and target specificity. In the current scenario, studies on macrofungi have been an area of importance for scientists. Macrofungi grow prolifically and are found in many parts of the world. Basidiomycetes (mushrooms) flourish ubiquitously under warm and humid climates. Basidiomycetes are rich sources of natural antibiotics. The secondary metabolites produced by them possess antimicrobial, antitumor, and antioxidant properties. The present review discusses the potential role of Basidiomycetes as anti-phytofungal, anti-phytobacterial, anti-phytoviral, mosquito larvicidal, and nematicidal agents.

Isolation and characterization of 2-hydroxy-9,10-anthraquinone from Streptomyces olivochromogenes (ERINLG-261) with antimicrobial and antiproliferative properties

Abstract Currently Streptomyces is one of the most important antibiotic producing microorganisms against several diseases. In the present study Streptomyces olivochromogenes ERINLG-261 was isolated from the soil samples of the Mudumalai hills, Western Ghats, India. Morphological, physiological, biochemical and 16S rRNA studies strongly suggested that this isolate belonged to the genus Streptomyces. ERINLG-261 showed good antimicrobial activity against different bacteria and fungi in Micromonospora fermentation medium. The active ethyl acetate extract was packed in column chromatography over silica gel which led to the isolation of 2-hydroxy-9,10-anthraquinone as the active principle. The isolated compound showed good antimicrobial activity against tested bacteria and fungi in minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) studies. The compound showed moderate in vitro antiproliferative activity against A549 and COLO320 cells. The compound was subjected to molecular docking studies for the inhibition of Topoisomerase, TtgR and Beta-lactamase enzymes which are targets for antimicrobials. Docking results of the compound showed low docking energy with these enzymes indicating its usefulness as antimicrobial agent. This is the first report of antimicrobial and antiproliferative activity of 2-hydroxy-9,10-anthraquinone isolated from Streptomyces olivochromogenes along with molecular docking studies.

MicroRNA in prostate cancer.

In the United States of America male prostate cancer (PCa) is the most dominant malignancy and the second highest cause of cancer-related mortality risk compared to lung and colon cancers. MicroRNAs (miRNAs) are a class of endogenously expressed small, non-coding, single-stranded RNA which function as regulators of gene expression. They influence various physiological and pathophysiological processes. In this review, we focus on the regulation of miRNAs in prostate cancer and their mechanisms which contribute to prostate carcinogenesis. The relation of miRNAs with androgen signaling is highlighted and the prospects of miRNAs for clinical therapies are discussed.

Bioefficacy of flindersine against Helicoverpa armigera Hübner, Spodoptera litura Fabricius, Anopheles stephensis Liston. and Culex quinquefasciatus Say.

Flindersine, an alkaloid isolated from Toddalia asiatica, was evaluated for their antifeedant, larvicidal and growth inhibitory activities against Helicoverpa armigera, Spodoptera litura and larvicidal activity against vector mosquitoes Anopheles stephensi and Culex quinquefasciatus. For this, leaf disc no choice method was used for agricultural pests; larvicidal activity was tested on second and fourth instar larvae for mosquitoes at different concentrations. Flindersine showed antifeedant, larvicidal and growth inhibitory activities against H. armigera and S. litura and larvicidal activity against vector mosquitoes An. stephensi and Cx. quinquefasciatus. It showed high regression (R2) values of 0.91 and 0.87 against H. armigera and S. litura, respectively for antifeedant activity. Flindersine exhibited more than 65% larvicidal activity against both the pests with LC50 values of 443.04 and 568.88 ppm and R2 values of 0.87 and 0.90 against H. armigera and S. litura, respectively. The larval and pupal duration of tested insects increased to more than five days at 1000 ppm when compared with the control. The adult emergence was reduced when the concentration of flindersine was increased. At 1000 ppm, no adult emergence was observed in both the pests. Flindersine exhibited 100% larvicidal activity against both the tested mosquitoes at 20 ppm concentration, which showed LC50 values of 2.90, 4.19, 1.68 and 2.71 ppm for 2nd and 4th instar larvae of Cx. quinquefasciatus and An. Stephensi, respectively. High regression values were observed for antifeedant, larvicidal and growth inhibitory activities. Flindersine could be used to develop an ecofriendly pesticide formulation to control the agricultural pests and vector mosquitoes.

Feeding Deterrent and Genotoxicity Analysis of a novel Phytopesticide by using Comet Assay against Helicoverpa armigera (HÜbner) (Lepidoptera: Noctuidae)

Newly developed Phytopesticidal formulations from pongam and neem oils were evaluated for their feeding deterrent activity using leaf disc choice and no-choice methods, and genotoxic study using comet assay against Helicoverpa armigera at different concentrations of 5, 10, 15, and 20 ppm. Among various phytopesticidal formulations, neem and pongam oils at 1:1 ratio, called PONNEEM showed significant feeding deterrent activity against H. armigera at 20 ppm concentration and wasgenotoxic to H. armigera (P>0.001). The comet parameters, namely tail moment (arbitrary units), tail length (µm) and tail DNA (%) were observed at all the concentrations of PONNEEM. Statistically significant changes in all the comet parameters of H. armigera were observed at 20 ppm (P<0.001). Feeding deterrent and genotoxicity effect of PONNEEM could be applied as phytopesticide for controlling the lepidopteran insect pests.

Bioefficacy of pectolinaringenin from Clerodendrum phlomidis Linn. F. against Anopheles stephensi and bhendi fruit borer, Earias vittella fab.

Larvicidal activity of pectolinaringenin from Clerodendrum phlomidis was evaluated against Anopheles stephensi and antifeedant, larvicidal and growth inhibitory activities were evaluated against Earias vittella. Pectolinaringenin exhibited larvicidal activity of 100 and 98.24% against 2nd and 4th instar larvae of Anopheles stephensi at 5ppm concentration. It exhibited LC50 values of 0.35 and 0.55 ppm for 2nd and 4th instar larvae, respectively. At 100 ppm concentration, pectolinaringenin exhibited maximum antifeedant activity of 74.00% and larvicidal activity of 89.98%. The LC50 values were 36.2 and 10.23 ppm for antifeedant and larvicidal, respectively. The compound completely prevented the adult emergence at 50 and 100 ppm concentrations. This is the first report of pectolinaringenin from C. phlomidis evaluated against An. stephensi and E. vittella. The results suggested that the pectolinaringenin from C. philomidis could be used to develop a new botanical formulation to manage vector mosquitoes and agricultural pests.

Evaluation of fractions and 5,7-dihydroxy-4',6-dimethoxy-flavone from Clerodendrum phlomidis Linn. F. against Helicoverpa armigera Hub.

Twelve fractions from chloroform extract of Clerodendrum phlomidis and 5,7-dihydroxy- 4',6-dimethoxy-flavone (pectolinaringenin) were evaluated against Helicoverpa armigera. Maximum antifeedant (89.41%), larvicidal (83.77%) and ovicidal (69.25%) activities were observed in fraction 5. The least LC50 value for antifeedant (178.09 ppm) and larvicidal (198.23 ppm) were observed in fraction 5. No adult emergence was recorded in fractions 4-6 at 1000 ppm. The oviposition deterrent activity was 100% in fraction 5 at all the concentrations. Pectolinaringenin recorded maximum antifeedant (74.68%) and larvicidal (81.11%) activities at 100 ppm; it completely prevented the adult emergence of H. armigera at 100 ppm. Maximum ovicidal activity at 100 ppm concentration was 67.95%. The oviposition deterrent activity was 100% in 100 and 50 ppm concentrations. C. phlomidis could be effectively used to develop a new formulation to control the economically important pests.

Induced resistance to Helicoverpa armigera through exogenous application of jasmonic acid and salicylic acid in groundnut, Arachis hypogaea.

BACKGROUND: Induced resistance to Helicoverpa armigera through exogenous application of jasmonic acid (JA) and salicylic acid (SA) was studied in groundnut genotypes (ICGV 86699, ICGV 86031, ICG 2271 and ICG 1697) with different levels of resistance to insects and the susceptible check JL 24 under greenhouse conditions. Activities of oxidative enzymes and the amounts of secondary metabolites and proteins were quantified at 6 days after JA and SA application/insect infestation. Data were also recorded on plant damage and H. armigera larval weights and survival. RESULTS: Higher levels of enzymatic activities and amounts of secondary metabolites were observed in the insect-resistant genotypes pretreated with JA and then infested with H. armigera than in JL 24. The insect-resistant genotypes suffered lower insect damage and resulted in poor survival and lower weights of H. armigera larvae than JL 24. In some cases, JA and SA showed similar effects. CONCLUSION: JA and SA induced the activity of antioxidative enzymes in groundnut plants against H. armigera, and reduced its growth and development. However, induced response to application of JA was greater than to SA, and resulted in reduced plant damage, and larval weights and survival, suggesting that induced resistance can be used as a component of pest management in groundnut.