OBJECTIVETo investigate the antioxidant, antibacterial and cytotoxic activity of whole Leucas aspera (Labiatae) (L. aspera) alcoholic extract.

METHODSWhole L. aspera powder was extracted by absolute ethanol (99.50%). The ethanolic extract was subjected to antioxidant, antibacterial and brine shrimp lethality assay.

RESULTSThe extract showed potent radical scavenging effect (antioxidant) with IC50 value of (99.58±1.22) µg/mL which was significant (P<0.01) in comparison to ascorbic acid with IC50 value of (1.25±0.95) µg/mL. In case of antibacterial screening, the extract showed notable antibacterial effect against the tested microbial strains. Significant (P<0.05) zone of inhibitions against Gram positive Bacillus subtilis [(12.00±1.32) mm] and Bacillus megaterium [(13.00±1.50) mm], Staphylococcus aureus [(8.00±0.50) mm] and Gram negative Salmonella typhi [(6.00±0.50) mm], Salmonella paratyphi [(8.00±1.00) mm], Shigella dysenteriae [(9.00±1.32) mm] and Vibrio cholerae [(9.00±0.66) mm] was observed. In brine shrimp lethality bioassay, the extract showed the LC50 value as (181.68±2.15) µg/mL which was statistically significant (P<0.01) compared to positive control vincristine sulfate [LC50=(0.76±0.04) µg/mL].

CONCLUSIONSThe results demonstrate that the ethanolic extract of L. aspera could be used as antibacterial, pesticidal and various pharmacologic actives.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Artemia ; drug effects ; Biphenyl Compounds ; antagonists & inhibitors ; Dose-Response Relationship, Drug ; Inhibitory Concentration 50 ; Lamiaceae ; chemistry ; Microbial Sensitivity Tests ; Phytochemicals ; chemistry ; pharmacology ; Picrates ; antagonists & inhibitors ; Plant Extracts ; chemistry ; pharmacology ; Toxicity Tests

In developing countries threat of cholera is a significant health concern whenever water purification and sewage disposal systems are inadequate. Vibrio cholerae is one of the responsible bacteria involved in cholera disease. The complete genome sequence of V. cholerae deciphers the presence of various genes and hypothetical proteins whose function are not yet understood. Hence analyzing and annotating the structure and function of hypothetical proteins is important for understanding the V. cholerae. V. cholerae O139 is the most common and pathogenic bacterial strain among various V. cholerae strains. In this study sequence of six hypothetical proteins of V. cholerae O139 has been annotated from NCBI. Various computational tools and databases have been used to determine domain family, protein-protein interaction, solubility of protein, ligand binding sites etc. The three dimensional structure of two proteins were modeled and their ligand binding sites were identified. We have found domains and families of only one protein. The analysis revealed that these proteins might have antibiotic resistance activity, DNA breaking-rejoining activity, integrase enzyme activity, restriction endonuclease, etc. Structural prediction of these proteins and detection of binding sites from this study would indicate a potential target aiding docking studies for therapeutic designing against cholera.
Bacteria ; Binding Sites ; Cholera ; Computer Simulation* ; Developing Countries ; DNA ; DNA Restriction Enzymes ; Drug Discovery ; Drug Resistance, Microbial ; Genome ; Humans ; Integrases ; Sewage ; Solubility ; Vibrio cholerae ; Vibrio cholerae O139* ; Water Purification

The plethora of genome sequence information of bacteria in recent times has ushered in many novel strategies for antibacterial drug discovery and facilitated medical science to take up the challenge of the increasing resistance of pathogenic bacteria to current antibiotics. In this study, we adopted subtractive genomics approach to analyze the whole genome sequence of the Fusobacterium nucleatum, a human oral pathogen having association with colorectal cancer. Our study divulged 1,499 proteins of F. nucleatum, which have no homolog's in human genome. These proteins were subjected to screening further by using the Database of Essential Genes (DEG) that resulted in the identification of 32 vitally important proteins for the bacterium. Subsequent analysis of the identified pivotal proteins, using the Kyoto Encyclopedia of Genes and Genomes (KEGG) Automated Annotation Server (KAAS) resulted in sorting 3 key enzymes of F. nucleatum that may be good candidates as potential drug targets, since they are unique for the bacterium and absent in humans. In addition, we have demonstrated the three dimensional structure of these three proteins. Finally, determination of ligand binding sites of the 2 key proteins as well as screening for functional inhibitors that best fitted with the ligands sites were conducted to discover effective novel therapeutic compounds against F. nucleatum.
Anti-Bacterial Agents ; Bacteria ; Binding Sites ; Colonic Neoplasms ; Colorectal Neoplasms ; Computer Simulation* ; Drug Delivery Systems ; Drug Discovery ; Fusobacterium nucleatum* ; Fusobacterium* ; Genes, Essential ; Genome ; Genome, Human ; Genomics ; Humans ; Ligands ; Mass Screening ; Mining* ; Proteome*

Objective: The aim of the current research was to analyze the role of subolesin and enolase in feeding and reproduction of H. longicornis by gene silencing. Methods: In this study, we used RNA interference to silence salivary enolase and subolesin in H. longicornis. Unfed female ticks injected with double-stranded RNA targeting subolesin and enolase were attached and fed normally on the rabbit's ear. Real-time polymerase chain reaction was used to confirm the extent of knockdown. Results: Ticks in the subolesin or enolase dsRNA groups showed knockdown rates of 80% and 60% respectively. Ticks in the combination dsRNA (subolesin and enolase) group showed an 80% knockdown. Knockdown of subolesin and enolase resulted in significant depletion in feeding, blood engorgement weight, attachment rate, and egg laying. Silencing of both resulted in a significant (p < 0.05) reduction in tick engorgement, egg laying, egg hatching (15%), and reproduction. Conclusions and Relevance: Our results suggest that subolesin and enolase are an exciting target for future tick control strategies.

Objective: To investigate the comparative effects of Diospyros blancoi (Ebenaceae) leaves (DBL), root bark (DBRB) and stem bark (DBSB) on free radicals and cancer. Methods: The polyphenol contents, antioxidant and free radical scavenging properties were determined using standard spectrophotometric methods. Cytotoxicity and anticancer activities were performed on brine shrimp nauplii and Ehrlich ascite carcinoma cells, respectively. Results: Among the extracts, DBSB showed the highest total antioxidant capacity and reducing capacity on ferrous ion. Based on 1,1-diphenyl-2-picrylhydrazyl and hydroxyl radical scavenging activities, DBSB showed (95.760 ± 0.343)% and (67.460 ± 2.641)% scavenging with IC

Objective To evaluate the effect of methanolic extract of Syzygium cumini (L.) Skeels (S. cumini) seeds on the major organs in an animal model of diabetes through biochemical and histopathological studies. Methods The methanolic extracts of S. cumini seeds (100 and 200 mg/kg body weight) were administered to alloxan-induced diabetic rats daily, with fasting blood glucose levels being measured by glucometry at one-day interval for a duration of two weeks. Biochemical assays to evaluate changes in the functions of the heart, liver, pancreas and kidney were carried out. Histopathological changes in the diabetic rat organs (pancreas, liver, heart, kidney and spleen) were also observed after the 14 days of treatment with the extracts. Results Oral administration of methanolic extracts of S. cumini seeds (100 and 200 mg/kg body weight), with gliclazide as a positive control (25 mg/kg), showed beneficial effects including lowering blood glucose levels (P < 0.001), improved heart and liver functions, and hyperlipidemia due to diabetes. At 200 mg/kg, the extracts reversed cardiac and liver damage caused by alloxan. Conclusions In addition to the anti-hyperglycemic activity of methanolic extracts of S. cumini seeds, the extracts demonstrates potential to minimize cardiac and hepatic complications.

Objective: To evaluate hydrophilic extracts from edible portions of fifteen plants for total phenolic content (TPC) and anti-oxidant capacity (AC) as an effort to find possible sources for future novel antioxidants. Methods: Folin-Ciocalteau and DPPH radical scavenging assays were employed to determine TPC and AC, respectively. Results: Among the assayed plants, TPC (mean±SD), expressed as gallic acid equivalent, varied from 0.04±0.01 (Amaranthus spinosus) to 6.01±0.04 (Zanthoxylum rhetsa) mg gallic acid equivalent/g fresh weight. AC (mean±SD), expressed as trolox equivalent, ranged from 0.14±0.00 (Alternanthera philoxeroides) to 7.54±0.00 (Zanthoxylum rhetsa) μmol trolox equivalent/g fresh weight. A significant and positive linear relationship (R