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.

Zinc supply influenced the growth, yield, zinc content, and expression of ZIP family transporters in sorghum.

MAIN CONCLUSION: Zinc deficiency altered shoot and root growth, plant biomass, yield, and ZIP family transporter gene expression in sorghum. Zinc (Zn) deficiency affects several crop plants' growth and yield, including sorghum. We have evaluated the sorghum under various concentrations of Zn supply for phenotypic changes, Zn content, and expression of Zn-regulated, iron-regulated transporter-like proteins (ZIP) family genes. Zn deficiency reduced the shoot and root growth, plant biomass, and yield by > 50%. The length and number of lateral roots were increased by more than 50% under deficient Zn compared to sufficient Zn. Ten SbZIP family transporter genes showed dynamic expression in shoot and root tissues of sorghum under deficient and sufficient Zn. SbZIP2, 5, 6, 7, and 8 were expressed in all tissues under deficient and sufficient Zn. SbZIP2, 4, 5, 6, 7, 8, and 10 were highly induced in shoot tissues by deficient Zn. The expression level of SbZIP6, 7, 8, and 9 was higher in root tissues under deficient Zn. The phylogenetic analysis revealed that most SbZIP family proteins are closely associated with the ZmZIP family of maize. The functional residues His177 and Gly182 are fully conserved in all SbZIP family transporters, as revealed by homology modeling and multiple sequence alignment. This study may provide a foundation for improving the Zn-use efficiency of sorghum.

Phylogenomics including the newly sequenced mitogenomes of two moths (Noctuoidea, Erebidae) reveals Ischyja manlia (incertae sedis) as a member of subfamily Erebinae.

We sequenced the mitogenomes of two Erebid species, namely Ischyja manlia (Cramer, 1776) and Rusicada privata (Walker, 1865) to analyse the phylogenetic relationship and to establish the taxonomic position of incertae sedis members of the family Erebidae. The two circular genomes of I. manlia and R. privata were 15,879 bp and 15,563 bp long, respectively. The gene order was identical, containing 13 protein-coding genes (PCGs), 22 tRNA genes, two rRNA genes, and an A + T-rich region. The nucleotide compositions of the A + T-rich region of both mitogenomes were similar: 80.65% for R. privata, and 81.09% for I. manlia. The AT skew and GC skew were slightly positive in I. manlia and negative in R. privata. In I. manlia and R. privata, except for cox1 which started with CGA and TTG codons, all the other 12 PCGs started with ATN codon. The A + T-rich regions of I. manlia and R. privata were 433 and 476 bp long, respectively, and contained common characteristics of Noctuoidea moths. At present, Ischyja is treated as Erebinae incertae sedis. However, phylogenetic analysis conducted in the present study reveals that the genus Ischyja is most likely to be a member of the subfamily Erebinae.

Growth inhibitory effect of selected quinones from Indian medicinal plants against Theileria annulata.

Tropical Bovine Theileriosis, caused by the protozoan parasite Theileria annulata, poses a significant threat to cattle populations. Currently, Buparvaquone is the sole effective naphthoquinone drug commercially available for its treatment. In our research, we delved into the potential of naturally occurring quinones as alternative treatments. We isolated two quinones, emodin and chrysophanol, from Rheum emodi Wall, and two more, embelin and lawsone, from Embelia ribes Burm.f. and Lawsonia inermis L. respectively. We assessed the anti-Theileria efficacy of these quinones in vitro using MTT and flow cytometric assays on T. annulata-infected bovine lymphocytes. Additionally, we evaluated their safety on uninfected bovine Peripheral Blood Mononuclear Cells (PBMC) and Vero cells. Emodin emerged as a promising candidate, exhibiting an IC50 value of 4 µM, surpassing that of buparvaquone. Emodin also displayed relatively low LD50 values of 1.74 mM against uninfected PBMC and 0.87 mM against Vero cells, suggesting potential safety. Remarkably, emodin demonstrated a high cell absorption rate of 71.32%. While emodin's efficacy and bioavailability are encouraging, further research is imperative to validate its safety and effectiveness for treating Tropical Bovine Theileriosis.

Characterization and Molecular Phylogenetic Analysis of Subfamily Erebinae (Lepidoptera: Noctuoidea: Erebidae) Using Five Complete Mitochondrial Genomes.

In this study, the complete mitogenomes of Sympis rufibasis, Lacera noctilio, Oxyodes scrobiculata, Mocis undata, and Artena dotata were newly sequenced to bring up-to-date the database using the next-generation sequencing methods. The gene order of all sequenced mitogenomes was identical consisting of 13 protein-coding genes (PCGs), 22 transfer RNA genes (tRNAs), two ribosomal RNA genes (rRNAs), and a non-coding A+T-rich region, which were common to other Lepidopteran insects. All protein-coding genes (PCGs) initiated with a canonical ATN codon and ended with TAN or an incomplete stop codon, single T. The A+T-rich region of S. rufibasis, L. noctilio, O. scrobiculata, M. undata, and A. dotata are 406 bp, 462 bp, 372 bp, 410 bp, and 406 bp long, respectively, containing number of characteristics that are distinctive to Noctuoidea moths. We analyzed concatenated amino acid sequences of protein-coding genes not including rRNAs, using Maximum Likelihood and Bayesian Inference methods. The phylogenetic analyses indicated that the tribe relationships within Erebinae were reconstructed as (Sypnini+((Erebini 1+Poaphilini 1)+((Euclidiini+Catocalini+(Hypopyrini+Erebini 2))+((Hulodini+(Poaphilini 2+Ophiusini))))). Phylogenetic analyses supported and confirmed the monophyly of the subfamilies' relationships as follows: (Hypeninae+Lymantriinae)+((Scoliopterginae+((Calpinae+Erebinae)+((Herminiinae+Aganainae)+Arctiinae)))) within Erebidae.

Docking studies and thiourea-mediated reduced graphene oxide nanosheets' larvicidal efficacy against Culexquinquefasciatus.

The larvicidalproperty of graphene oxide (GO) and thiourea-reduced graphene oxide (T-rGO)was assessed against Culexquinquefasciatuslarvae. A simple water-soluble material synthesis method was used. The transformation of graphene into graphene oxide was accomplished in a single step. Under mild conditions, grapheneoxidewasdissolved in water to form a solution. Structure, optical, and microstructural features of the synthesized samples wereevaluatedusing a variety of analytical tools to compare the samples. Both GO and RGO, as well as GO, showed strong larvicidal potential when used against the third instar larvae of the Culexquinquefasciatus mosquito, with LC50and LC90values of 1.71 and 5.17 ppm and 1.89 and 5.00 ppm, respectively. As a result, our study showed that all of the GO and T-rGO under investigation create larvicidal compounds that could be employed to support efforts to control mosquito populations. It also offers an alternative method for producing GO and rGO on a big scale, which may be used in the future for a variety of biomedical applications.The binding efficacy of the active compounds against AChE1 was studied using Auto dock and the results were observed to be highly promising.

Synthesis and characterization of magnetite carbon nanocomposite from agro waste as chromium adsorbent for effluent treatment.

The waste water released from industries which contain pollutants like heavy metals, dyes and other toxic chemicals brings numerous harms to the ecosystem and humans. Nowadays the nanocomposites based technologies are effectively used for environmental remediation. In the present study, hexavalent chromium was removed from the industrial effluent using magnetite carbon nanocomposite. The nanocomposite composed of highly porous carbon and iron oxide nanoparticles prepared by using agrowastes (sugarcane bagasse and orange peel extract). Iron oxide nanoparticles (FeONPs) formation was confirmed by UV-visible spectroscopy; incorporation of magnetite with highly porous carbon was established by Fourier Transforms Infrared Spectroscopy and X-ray Diffraction Spectroscopy. Morphological features of magnetite nanoparticles and highly porous carbon were analyzed using Scanning Electron Microscope and Transmission Electron Microscope. Magnetic properties analyzed by Vibrating Sample Magnetometer revealed magnetite carbon nanocomposite exhibited better Ms value than highly porous carbon. The concentration of Cr6+ in treated effluent was determined using Atomic Absorption Spectroscopy. Pseudo-second order equation fitted with kinetics and the Langmuir monolayer favors for isotherm. This study reveals efficiency in Cr6+ removal from effluent using magnetite carbon nanocomposites which extends their application in waste water treatment.

Larvicidal and ovicidal activities of phenyl acetic acid isolated from Streptomyces collinus against Culex quinquefasciatus Say and Aedes aegypti L. (Diptera: Culicidae).

The bio-efficacy of crude ethyl acetate extract, fractions and a compound phenyl acetic acid from the ethyl acetate extract of Streptomyces collinus was evaluated on Culex quinquefasciatus Say and Aedes aegypti L. mosquitoes (Diptera: Culicidae). The larvae were exposed to concentrations of 2.5, 5.0, 7.5 and 10.0 ppm for fractions and 0.5, 1.0, 1.5 and 2.0 ppm for compound. After 24 h, the larval mortality was assessed and the LC50 and LC90 values were calculated. Similarly, per cent ovicidal activity was calculated for eggs after 120 h post treatment for phenyl acetic acid. Among the eleven fractions screened, fraction 7 from the ethyl acetate extract of Streptomyces collinus exhibited good larvicidal activity against both mosquito species. The LC50 and LC90 values of fraction 7 were 4.42, 6.23 ppm against Cx. quinquefasciatus larvae and 5.13, 14.51 ppm against Ae. aegypti larvae, respectively. Further, the isolated compound, phenyl acetic acid from fraction 7 recorded 100% larvicidal activity at 2 ppm concentration with LC50 and LC90 values of 2.07, 4.87 ppm on Cx. quinquefasciatus larvae and 3.81, 9.87 ppm on Ae. aegypti larvae, respectively. Phenyl acetic acid presented 50.3% and 42.0% ovicidal activity against Cx. quinquefasciatus and Ae. aegypti eggs at 2 ppm concentration after 120 h post treatment. The compound, phenyl acetic acid could be used in mosquito control programme.

Synthesis of a 1,2,3-bistriazole derivative of embelin and evaluation of its effect on high-fat diet fed-streptozotocin-induced type 2 diabetes in rats and molecular docking studies.

The embelin derivative 2a was synthesized with the 1,2,3-bistriazole and spectral data confirmed its structural identity. Anti-diabetic and anti-lipidemic effects were evaluated using HFD-STZ induced type 2 diabetic rats. The derivative 2a (30 mg/kg b wt.) supplementation significantly (P ≤ 0.01) normalized the changed biochemical parameters like fasting blood glucose (FBG), body weights, plasma insulin level, total cholesterol (TC), triglycerides (TG) and marker enzymes of carbohydrate metabolism. The derivative 2a (30 mg/kg) also showed a significant effect on oral glucose tolerance test (OGTT) and intraperitoneal insulin tolerance test (ITT). But 15 mg/kg dose of derivative 2a failed to show any significant effects in HFD-STZ induced type2 diabetic rats. Histopathology analysis substantiated the protective effect of this derivative 2a (30 mg/kg b wt.) on the ß-cells of the pancreatic, liver and adipose tissues in diabetic treated rats. Further, the expressions of PPARγ and GLUT4 were significantly enhanced in the epididymal adipose tissue. The HOMO and LUMO energies characterized the molecular stability of the derivative 2a with 6-311G++ (d, p) in DFT/B3LYP/LanL2DZ method using Gaussian09 program package. The molecular docking analysis also confirmed the activity of derivative 2a through hydrogen bond interaction with ARG 288, GLU 343, SER 342 and least energy value (-7.72 kcal/mol). Hence, the embelin-1,2,3-bis triazole derivative 2a (30 mg/kg) enhanced the activity of embelin and might be acting as a suitable drug for type 2 diabetes, obesity and its complications.

Phosphate supply influenced the growth, yield and expression of PHT1 family phosphate transporters in seven millets.

MAIN CONCLUSION: Phosphate starvation altered the root morphology and phosphate uptake with the induction of PHT1 family transporter genes in root and shoot tissues of seven millets. Millets are nutrient-rich cereals majorly cultivated in Asia and Africa. Foxtail millet (FoxM), pearl millet (PeaM), finger millet (FinM), kodo millet (KodM), little millet (LitM), proso millet (ProM), and barnyard millet (BarM) were examined for the influence of external phosphorous (P) supply on phenotypic traits, P uptake, yield, and PHosphate Transporter1 (PHT1) family gene expression. Millet seedlings grown under low Pi condition (LPC) produced significantly lower mean values for all traits except for lateral root length (LRL) and lateral root number (LRN) which were increased under LPC. Under LPC, seed weight (SW) also reduced by > 75% and had significantly lower levels of total P (TP) and Pi contents in leaf and root tissues. Expression dynamics of 12 PHT1 family (PHT1;1-1;12) transporters genes were analyzed in 7 millets. PHT1;2 has been found to be a constitutive transporter gene in all millets. Under LPC, root tissues showed the overexpression of PHT1;2, 1;3, 1;4 and 1;9 in FoxM, PHT1;1, 1;2, 1;3, 1;4, 1;8 and 1;10 in PeaM, PHT1;2 and 1;3 in FinM and ProM and PHT1;3, 1;6 and 1;11 in BarM. In leaf, LPC induced the expression of PHT1;3, 1;4 and 1;6 in FoxM, PHT1;2, 1;3, 1;4 and 1;8 in PeaM, PHT1;2, 1;3 and 1;4 in FinM and KodM, PHT1;2 in LitM and PHT1;4 in ProM and BarnM. This comprehensive study on the influence of P in phenotype, physiology, and molecular responses may help to improve the P uptake and its use efficiency of millets in future.

Biocontrol and non-target effect of fractions and compound isolated from Streptomyces rimosus on the immature stages of filarial vector Culex quinquefasciatus Say (Diptera: Culicidae) and the compound interaction with Acetylcholinesterase (AChE1).

The present study was aimed to check the mosquitocidal activity of intracellular methanol extract fractions and the compound di (2-ethylhexyl) phthalate isolated from Streptomyces rimosus. The isolated compound was also analyzed for its interaction with Acetylcholinesterase (AChE1). The larvae and eggs of Culex quinquefasciatus were exposed to four different concentrations such as 2.5, 5.0, 7.5 and 10 ppm for fractions and 0.5, 1.0, 1.5 and 2.0 ppm for compound. After 24 and 120 h post treatment, the larval mortality and ovicidal activity were recorded. Fractions collected from the intracellular methanol extract were tested for larvicidal activity; among them Fraction 4 was found to be the active fraction. Fraction 4 showed 74% larvicidal activity with LC50 and LC90 values of 6.9 and 17.2 ppm, respectively, in 24 h against the larvae of Cx. quinquefasciatus. Fraction 4 showed 95% ovicidal activity at 10 ppm concentration after 120 h post treatment. The eluted compound di(2-ethylhexyl) phthalate was highly toxic and exhibited promising activity against the eggs of Cx. quinquefasciatus. The compound presented 94% ovicidal activity at 2.0 ppm concentration after 120 h post treatment. The larvae of Cx. quinquefasciatus were exposed to di(2-ethylhexyl) phthalate which showed good activity in a concentration-dependent manner. The compound showed 76% larvicidal activity against the larvae of Cx. quinquefasciatus with LC50 and LC90 values of 1.22 and 3.28 ppm, respectively, at 2 ppm concentration in 24 h. Fraction 4 and the compound were subjected to toxicity study against non-target organism and were found to be nontoxic. The present studies revealed that the treated larvae showed serious damage in the midgut cells. Growth disruption and larval deformities were observed in compound-treated larvae. The compound was highly active and inhibited AChE in a concentration-dependent manner. Computational analysis of the compound had strong interaction with AChE1 of Cx. quinquefasciatus. These results clearly showed that Fraction 4 and the compound isolated from S. rimosus can be used to control the life stages of Cx. quinquefasciatus; it will be a good alternative to synthetic insecticides.

Protective effects of Ficus carica leaves on glucose and lipids levels, carbohydrate metabolism enzymes and ß-cells in type 2 diabetic rats.

CONTEXT: The decoctions of Ficus carica Linn. (Moraceae) leaves are used in the folklore treatment of diabetes. OBJECTIVE: To evaluate the effect of F. carica on glucose and lipids levels, carbohydrate metabolism enzymes and ß-cells protective effects in type 2 diabetes. MATERIAL AND METHODS: Diabetes was induced in 15 days high-fat diet (HFD)-fed Wistar rats by intraperitoneal injection of streptozotocin (STZ) (40 mg/kg). The ethyl acetate extract (250 and 500 mg/kg) of F. carica leaves was administered for 28 days. Oral glucose tolerance (OGTT) and intraperitoneal insulin tolerance tests (ITT) were evaluated on 15th and 25th days, respectively. RESULTS: The ethyl acetate extract (250 and 500 mg/kg) of n F. carica leaves showed significant effect (p < 0.005) in the levels of blood glucose, total cholesterol (TC), triglycerides (TG), body weight and hepatic glycogen. In OGTT, F. carica (250 and 500 mg/kg) significantly (p < 0.005) detained the increase in blood glucose levels at 60 and 120 min and in ITT, F. carica enhanced the glucose utilization significantly (p < 0.005) over 30 and 60 min compared to diabetic control. Further, the altered activities of key carbohydrate metabolizing enzymes such as glucose-6-phosphatase, fructose-1,6-bisphosphatase and hexokinase in the liver tissue of diabetic rats were significantly (p < 0.005) reverted to near normal levels upon treatment with F. carica. Immumohistochemical studies of islets substantiated the cytoprotective effect on pancreatic ß-cells. DISCUSSION AND CONCLUSIONS: F. carica leaves exerted significant effect on carbohydrate metabolism enzymes with promising hypoglycemic and hypolipidemic activities in type 2 diabetic rats.

Insulin sensitization via partial agonism of PPARγ and glucose uptake through translocation and activation of GLUT4 in PI3K/p-Akt signaling pathway by embelin in type 2 diabetic rats.

BACKGROUND: The present study was aimed at isolating an antidiabetic molecule from a herbal source and assessing its mechanism of action. METHODS: Embelin, isolated from Embelia ribes Burm. (Myrsinaceae) fruit, was evaluated for its potential to regulate insulin resistance, alter ß-cell dysfunction and modulate key markers involved in insulin sensitivity and glucose transport using high-fat diet (HFD) fed-streptozotocin (STZ) (40mg/kg)-induced type 2 diabetic rats. Molecular-dockings were performed to investigate the binding modes of embelin into PPARγ, PI3K, p-Akt and GLUT4 active sites. RESULTS: Embelin (50mg/kg b wt.) reduced body weight gain, blood glucose and plasma insulin in treated diabetic rats. It further modulated the altered lipid profiles and antioxidant enzymes with cytoprotective action on ß-cell. Embelin significantly increased the PPARγ expression in epididymal adipose tissue compared to diabetic control group; it also inhibited adipogenic activity; it mildly activated PPARγ levels in the liver and skeletal muscle. It also regulated insulin mediated glucose uptake in epididymal adipose tissue through translocation and activation of GLUT4 in PI3K/p-Akt signaling cascade. Embelin bound to PPARγ; it disclosed stable binding affinities to the active sites of PI3K, p-Akt and GLUT4. CONCLUSIONS: These findings show that embelin could improve adipose tissue insulin sensitivity without increasing weight gain, enhance glycemic control, protect ß-cell from damage and maintain glucose homeostasis in adipose tissue. GENERAL SIGNIFICANCE: Embelin can be used in the prevention and treatment of type 2 diabetes mellitus caused due to obesity.

In vitro antimicrobial, antioxidant and cytotoxic properties of Streptomyces lavendulae strain SCA5.

BACKGROUND: Actinomycetes are Gram-positive, often filamentous, bacteria known for their unsurpassed capacity for the production of secondary metabolites with diverse biological activities. The aim of the present study was to evaluate the antimicrobial, cytotoxic and antioxidant properties of Streptomyces lavendulae strain SCA5. RESULTS: The ethyl acetate extract of SCA5 broth (EA-SCA5) showed antimicrobial activity with MIC value of 31.25 µg/ml. EA-SCA5 showed good antioxidant potential by scavenging 2, 2-diphenyl-picrylhydrazyl (DPPH) (IC50 507.61 ± 0.66 µg/ml), hydroxyl radical (IC50 617.84 ± 0.57 µg/ml), nitric oxide (IC50 730.92 ± 0.81 µg/ml) and superoxide anion radical (IC50 864.71 ± 1.15 µg/ml). The EA-SCA5 also showed strong suppressive effect on rat liver lipid peroxidation (IC50 838.83 ± 1.18 µg/ml). The total phenolic content of SCA5 was 577.12 mg of GAE equivalents/gram extract. EA-SCA5 exhibited cytotoxic activity on A549 adenocarcinoma lung cancer cell line. It showed 84.9% activity at 500 µg/ml with IC50 value of 200 µg/ml. The gas chromatography mass spectrometry (GC-MS) analysis revealed the presence of one major bioactive compound actinomycin C2. CONCLUSIONS: The results of this study indicate that the EA-SCA5 could be probed further for isolating some medically useful compounds.

Effect of Polygonum hydropiper L. against dengue vector mosquito Aedes albopictus L.

The present study aimed to evaluate the essential oil and an isolated compound from the leaves of Polygonum hydropiper L. against dengue vector mosquito Aedes albopictus L. The plant material was macerated and steam distilled using clavenger apparatus for oil extraction. The essential oil was tested at different concentrations of 100, 50, 25, 12.5 and 6.25 ppm concentrations against the larvae of Ae. albopictus. The isolated compound was tested for larvicidal, ovicidal, repellent, oviposition deterrent and adulticidal activities at 10, 5, 2.5, 1.25 and 0.625 ppm concentrations. The essential oil exhibited LC50 values of 194.63 and 199.65 and confertifolin exhibited LC50 values of 2.02 and 3.16 against the second and fourth instar larvae of Ae. albopictus, respectively. The ovicidal activity of 100% on 0- to 6-h-old eggs, repellent activity of 320.6 min, oviposition deterrent activity of 98.51% and adulticidal activity of 100% at 10 ppm concentration of confertifolin were recorded. No mortality of was observed in negative control. To the best of our knowledge, this is the first report on the potential mosquitocidal activities of confertifolin against Ae. albopictus.

Larvicidal and pupicidal activities of ecbolin A and ecbolin B isolated from Ecbolium viride (Forssk.) Alston against Culex quinquefasciatus Say (Diptera: Culicidae).

The mosquitocidal activity of different fractions and isolated compounds from the ethyl acetate extract of Ecbolium viride root was assessed on larvae and pupae of Culex quinquefasciatus Say (Diptera: Culicidae). The larvae and pupae were exposed to concentrations of 6.125, 12.5, 25 and 50 ppm for fractions and 1, 2.5, 5 and 10 ppm for compound. Among the 12 fractions screened, fraction 6 from the ethyl acetate extract of E. viride was recorded to have the highest larvicidal and pupicidal activities against C. quinquefasciatus. The lethal concentration (LC50 and LC90) values of fraction 6 were 4.26 and 9.0 ppm against C. quinquefasciatus larvae and 6.55 and 12.19 ppm against C. quinquefasciatus pupae, respectively, in 24 h. Fraction 7 was recorded to have moderate activity with LC50 and LC90 values of 11.25 and 25.02 ppm against C. quinquefasciatus larvae and 13.33 and 31.15 ppm against C. quinquefasciatus pupae, respectively, in 24 h. Ecbolin A and ecbolin B were identified from fractions 7 and 6, respectively. The structure of the isolated compounds was identified on the basis of spectral data ((1)H NMR and (13)C NMR) and compared with literature spectral data. Further, the isolated compound, ecbolin B, from fraction 6 was recorded to have strong larvicidal and pupicidal activities than ecbolin A. The LC50 and LC90 values of ecbolin B on C. quinquefasciatus larvae were 1.36 and 2.76 ppm, and on pupae, these were 1.54 and 3.51 ppm, respectively. The present results suggest that ecbolin B could be used as a mosquitocidal agent against C. quinquefasciatus.

Gastroprotective activity of violacein isolated from Chromobacterium violaceum on indomethacin-induced gastric lesions in rats: investigation of potential mechanisms of action.

Chromobacterium violaceum, Gram-negative bacteria species found in tropical regions of the world, produces a distinct deep violet-colored pigment called violacein. In the present study, we investigated whether violacein can promote a gastroprotective effect and verified the possible mechanisms involved in this action. For this study, an indomethacin-induced gastric ulcer rat model was used. The roles of biomolecules such as MPO, PGE2, pro- and anti-inflammatory cytokines, growth factors, caspase-3, NO, K(+)ATP channels, and α 2-receptors were investigated. Violacein exhibited significant gastroprotective effect against indomethacin-induced lesions, while pretreatment with L-NAME and glibenclamide (but not with NEM or yohimbine) was able to reverse this action. Pretreatment with violacein also restored cNOS level to normal and led to attenuation of enhanced apoptosis and gastric microvascular permeability. Our results suggest that violacein provides a significant gastroprotective effect in an indomethacin-induced ulcer model through the maintenance of some vital protein molecules, and this effect appears to be mediated, at least in part, by endogenous prostaglandins, NOS, K(+)ATP channel opening, and inhibition of apoptosis and gastric microvascular permeability.

Effect of Mosquitocidal, histopathological alteration and non target effects of Sigesbeckia orientalis L. on Anopheles stephensi Liston, Culex quinquefasciatus say and Aedes aegypti L.

Diseases transmitted by vectors have a significant collision on society and community health, particularly in tropical and subtropical regions, where they can cause large-scale outbreaks shortly after initial transmission. The intent of this investigation was to study the plant extract derived from Sigesbeckia orientalis L. in controlling the immature stages of Anopheles, Culex and Aedes mosquitoes, while also considering its potential toxicity to ecosystems. The immature stages were exposed to different extracts (62.5-500 ppm), and the mortality of larvae and pupae, as well as ovicidal activity, were noted after 24 and 120 h of the experiment. The hexane and ethyl aceate extract of S. orientalis presented 100% ovicidal activity against the eggs of Anopheles, Aedes and Culex at 500 ppm concentration after 5 days of treatment. The hexane and ethylacetate extracts presented strong larvicidal activity with LC50 values of 215.7, 332.0, 197.4 and 212.6, 694.9 and 201.7 ppm against treated mosquitoes at 24 h, respectively. The same extract also presented promising pupicidal activity. The LC50 values of hexane extract were 219.6, 353.6, 194.2 and LC50 values of ethyl acetate were 257.6, 387.8 and 259.07 ppm against early stage pupae of three vector mosquitoes, respectively. The extracts from S. orientalis had strong inhibitory activity against growth and development of mosquitoes. SI/PSF values showed that the extracts of S. orientalis did not harm Poecilia reticulata, Diplonychus indicus (Water bug), Gambusia affinis and dragon fly nymph at tested concentrations. Furthermore, examinations of histopathology and growth disruption revealed significant damage to the midgut cells in the treated larvae. The formulations utilizing hexane and ethyl acetate extracts exhibited potent activity without posing any toxicity towards non-target organisms. This study clearly indicated that hexane and ethylacetate extracts showed promising results against treated mosquitoes. The present study documents the first report of the extracts from S. orientalis and they can be further assessed to identify compounds for application purposes.

Exploring the antiviral inhibitory activity of Niloticin against the NS2B/NS3 protease of Dengue virus (DENV2).

Dengue virus (DENV2) is the cause of dengue disease and a worldwide health problem. DENV2 replicates in the host cell using polyproteins such as NS3 protease in conjugation with NS2B cofactor, making NS3 protease a promising antiviral drug-target. This study investigated the efficacy of 'Niloticin' against NS2B/NS3-protease. In silico and in vitro analyses were performed which included interaction of niloticin with NS2B/NS3-protease, protein stability and flexibility, mutation effect, betweenness centrality of residues and analysis of cytotoxicity, protein expression and WNV NS3-protease activity. Similar like acyclovir, niloticin forms strong H-bonds and hydrophobic interactions with residues LEU149, ASN152, LYS74, GLY148 and ALA164. The stability of the niloticin-NS2B/NS3-protease complex was found to be stable compared to the apo NS2B/NS3-protease in structural deviation, PCA, compactness and FEL analysis. The IC50 value of niloticin was 0.14 µM in BHK cells based on in vitro cytotoxicity analysis and showed significant activity at 2.5 µM in a concentration-dependent manner. Western blotting and qRT-PCR analyses showed that niloticin reduced DENV2 protein transcription in a dose-dependent manner. Besides, niloticin confirmed the inhibition of NS3-protease by the SensoLyte 440 WNV protease detection kit. These promising results suggest that niloticin could be an effective antiviral drug against DENV2 and other flaviviruses.

Mosquitocidal Susceptibility and Non-Target Effects of Tricholoma equestre Mushroom (Agaricomycetes) on the Immature Stages of Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus.

The worldwide scientific community is well aware that mosquitoes are the sole agents responsible for transmitting various dreadful diseases and critical illnesses caused by vector-borne pathogens. The primary objective of this current research was to evaluate the effectiveness of methanol extract from Tricholoma equestre mushroom in controlling the early life stages of Culex quinquefasciatus Say, Anopheles stephensi Liston, and Aedes aegypti (Linnaeus in Hasselquist) mosquitoes. The larvae, pupae and eggs of these mosquitoes were exposed to four different concentrations (62.5 to 500 ppm). After 120 h of treatment, the methanol extract of T. equestre exhibited ovicidal activity ranging from 66% to 80% against the eggs of the treated mosquitoes. It also demonstrated promising larvicidal and pupicidal activity with LC50 values of 216-300 and 230-309 ppm against the early life stages of all three mosquito species. Extensive toxicity studies revealed that the methanol extract from T. equestre had no harmful effects on non-target organisms. The suitability index (SI) or predator safety factor (PSF) indicated that the methanol extract did not harm Poecilia reticulata Peters 1859, (predatory fish), Gambusia affinis S. F. Baird & Girard 1853, dragonfly nymph and Diplonychus indicus Venkatesan & Rao 1871 (water-bug). Gas chromatography-mass spectrometry (GCMS) analysis identified key compounds, including 3-butenenitrile, 2-methyl-(25.319%); 1-butanol, 2-nitro-(18.87%) and oxalic acid, heptyl propyl ester (21.82%) which may be responsible for the observed activity. Furthermore, the formulation based on the methanol extract demonstrated similar effectiveness against all treated mosquitoes at the laboratory level and was found to be non-toxic to mosquito predators. This groundbreaking research represents the first confirmation that methanol extract from T. equestre could be effectively employed in preventing mosquito-borne diseases through mosquito population control programs.