Screening of the antioxidant and antibacterial effects of extracted essential oils from Thunbergia coccinea, Acacia polyacantha, Polygonum micrpcephallum, Abies spectabilis and Clerodendrum colebrookianum

During the previous few decades, it has been seen that there is a rapid emergence of pathogens resistant to multiple antibiotics. This has now become a global crisis. Some unexplored or less explored plants also provide some antibacterial, bactericidal and antioxidant properties. The antibacterial, bactericidal effects of extracted essential oils (EEOs) of Thunbergia coccinea, Acacia polyacantha, Polygonum micrpcephallum, Abies spectabilis and Clerodendrum colebrookianum was tested in comparison with standard antibiotics. The methods chosen were disc diffusion and deduction of minimum inhibitory concentration (MIC) by microbroth dilution assays of the EEOs against the bacterial strains.The antioxidant activity was found out utilizing DPPH free radical scavenging assay, MDA, Hydrogen peroxide radical inhibition assay and Superoxide radical inhibition assay (O 2 -). Some commonly used standard antibiotics (metronidazole, amoxicillin, clarithromycin, rifampicin, clindamycin and oxacillin,) were utilized to compare the EEO antibacterial action. Clerodendrum colebrookianum (85.17 ± 3.06 µg MDA/g extract) had a reasonable MDA. Acacia polyacantha in MIC had values of 3.86 ± 0.25 to 6.20 ± 0.16. Polygonum micrpcephallum had excessive H2O2 (48.27 ± 2.4 5%). The antibacterial actions determined by the paper disc‑diffusion technique of the EEO extracted from these plants showed that most had some antibacterial actions. Also, it was seen that the bactericidal action of the EEO extracted from E. alba was most potent against S. pyogenes (4.06 ± 0.15). The extract of the plant at varying concentrations (20, 40, 60, 80 and100 mg/mL) demonstrated noteworthy (P< 0.001) anthelmintic action in an effective change when the dose was adjusted. In conclusion, most of the tested plants contain a medicinal value, which can be utilized in the future to supplement artificial medicines and cure emerging diseases that create havoc for mankind.

Isolation of Chemical Constituents and Invitro Antidiabetic Activity of Mirabilis Jalapa Flower Extracts

Objectives: The present work was designed to investigate the phytochemical and in vitro screening of the flower extracts of Mirabilis jalapa. Materials and Methods: Phytochemical constituents were isolated using column chromatography and characterized of the compounds were carried out using IR, 1H NMR, 13C NMR and mass spectroscopy data. In vitro anti-diabetic activity was evaluated by alpha-amylase inhibition assay and Alpha-glucosidase inhibition assay. Results: Phytochemical investigation of the ethanol extract revealed the presence of a flavonoid Kaempferol and a triterpenoid Lupeol. In vitro investigation indicated that the Mirabilis jalapa flowers extracts has considerable anti-diabetic activity Conclusion: The anti-diabetic activity may due to the presence of phytoconstituents like flavonoids, triterpenoids, steroids.

Disclosing the bioactive metabolites involved in the in vitro anthelmintic effects of salt-tolerant plants through a combined approach using PVPP and HPLC-ESI-MSn

Strategies to reduce dependence on synthetic drugs for the treatment of gastrointestinal nematodes (GIN) infections in ruminants include the search for novel anthelmintic scaffolds on plants, yet salt-tolerant plants remain overlooked. This study aims to evaluate the in vitro anthelmintic properties of selected salt-tolerant plants against GIN, and identify the potential bioactive secondary metabolites involved. For that purpose, 80% acetone/water extracts were prepared from dried biomass of aerial organs of nine salt-tolerant plant species and tested against Haemonchus contortus and Trichostrongylus colubriformis by the Larval Exsheathment Inhibition Assay (LEIA) and Egg Hatching Inhibition Assay (EHIA). Pistacia lentiscus, Limoniatrum monopetalum, Cladium mariscus and Helychrisum italicum picardi were the most active in both GIN and life stages. To investigate the role of polyphenols in the anthelmintic activity, four selected extracts were treated with polyvinylpolypyrrolidone (PVPP), and non-treated and treated samples were further characterized by high-performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC-ESI-MSn). While polyphenols seem responsible for the EHIA properties, they are partially accountable to LEIA results. Several phenolics involved in the anthelmintic effects were identified and discussed. In sum, these species are rich sources of anthelmintic compounds and, therefore, are of major interest for nutraceutical and/or phytotherapeutic applications against GIN in ruminants.

Evaluation of Tuberculosis Vaccine Candidate, pcDNA3.1-rpfD using Mycobacterial Growth Inhibition Assay (MGIA)

Resuscitation-promoting factor D (RpfD) is a protein involved in the resuscitation of dormant bacteria. A new tuberculosis vaccine carrying the rpfD gene has been successfully constructed, pcDNA3.1-rpfD. It was demonstrated that this vaccine exhibits cellular and humoral immune responses. Therefore, within this study, the efficacy of this new vaccine candidate was evaluated using mycobacterial growth inhibition assay (MGIA). MGIA is a functional assay that measures the complex host immune response, peripheral blood mononuclear cell (PBMC) and splenocyte from BALB/c mice against mycobacteria. With BACTECTM MGITTM 960 automated system, the effect of vaccination on bacterial growth was reported as a time to positivity (TTP) in hours. The mean of TTP from the vaccinated group (both pcDNA3.1-rpfD and BCG) was higher than the negative control group. These results suggest that pcDNA3.1-rpfD may be effective in controlling tuberculosis growth and may provide a clue for the development of the tuberculosis vaccine. In addition, despite previous evidence that IFNγ was essential for tuberculosis immunity, IFNγ (interferon gamma) production was found not to be correlated with mycobacterial inhibition. Therefore, these findings offer an alternative method to evaluate vaccine candidates than the assessment using IFNγ only.

Phytochemical Analysis and In-vitro Anti-Diabetic and Anti- Inflammatory study of root extract of Apama siliquosa LAMK.

The demand for herbal medicines in many pharmaceutical sectors is growing at a drastic rate due to their improved pharmacological actions, minimal side effects and cost-effectiveness. Anti-inflammatory phytochemicals are found to be efficacious against the treatment of inflammatory diseases like rheumatoid arthritis, glomerulonephritis, hepatitis, inflammatory bowel disease, etc. Anti-diabetic phytochemicals are found to treat the increasing incidence of diabetes prevalent globally. This work aims to perform the phytochemical screening and to evaluate the antidiabetic and anti-inflammatory activity of crude extract of Apama siliquosa Lamk. The method employed for obtaining the active principles includes soxhlation technique with methanol as solvent. The anti-inflammatory property was studied in vitro using inhibition of albumin denaturation technique as well as heat-induced hemolysis and IC50 value was found to be 39.5μg/ml and 36.30μg/ml respectively. The anti-diabetic activity was estimated using the alpha-amylase inhibition assay and Glucose diffusion inhibitory study. The IC50 value for alpha-amylase inhibition assay was found to be 15.75μg/ml. It also shows a strong inhibition of glucose across the dialysis membrane.

Identification of Novel Antistaphylococcal Hit Compounds Targeting Sortase A

Staphylococcus aureus (S. aureus) is a causative agent of many hospital- and community-acquired infections with the tendency to develop resistance to all known antibiotics. Therefore, the development of novel antistaphylococcal agents is of urgent need. Sortase A is considered a promising molecular target for the development of antistaphylococcal agents. The main aim of this study was to identify novel sortase A inhibitors. In order to find novel antistaphylococcal agents, we performed phenotypic screening of a library containing 15512 compounds against S. aureus ATCC43300. The molecular docking of hits was performed using the DOCK program and 10 compounds were selected for in vitro enzymatic activity inhibition assay. Two inhibitors were identified, N,N-diethyl-N′-(5-nitro-2-(quinazolin-2-yl)phenyl)propane-1,3-diamine (1) and acridin-9-yl-(1H-benzoimidazol-5-yl)-amine (2), which decrease sortase A activity with IC50 values of 160.3 µM and 207.01 µM, respectively. It was found that compounds 1 and 2 possess antibacterial activity toward 29 tested multidrug resistant S. aureus strains with MIC values ranging from 78.12 to 312.5 mg/L. These compounds can be used for further structural optimization and biological research.

In Vitro Studies on Alpha-amylase Inhibitory Activities of Zanthoxylum armatum of Mid-Western Regions of Nepal

The alpha-amylase inhibitors are used as a drug to control hyperglycemia in type II diabetes mellitus. The plant extract is a natural source to minimize toxicity and other side effects. The alpha-amylase inhibition assay shows that the methanol extracts of fruits, seeds, leaves, and barks of Z. armatum exhibit 50% alpha-amylase inhibition activity at concentration 47.73 μg/mL, 50.25 μg/mL, 67.25 μg/mL, 152.6 μg/mL respectively, and hexane extracts of fruits, seeds, leaves and barks of Z. armatum exhibits 50% alpha-amylase inhibition activity at concentration 86.24 μg/mL, 84.02 μg/mL, 98.8 μg/mL, 138.81 μg/mL respectively, whereas the 50% alpha-amylase inhibition activity of Acarbose (standard) was found to be 33.66 μg/mL. Therefore, methanol and hexane extracts of fruits, seeds, and leaves show potential alpha-amylase inhibition activity and can be used as anti-diabetes.

The Toxicity of Wiped Dust and Airborne Microbes in Individual Classrooms Increase the Risk of Teachers’ Work-Related Symptoms: A Cross-Sectional Study

Background: The causes and pathophysiological mechanisms of building-related symptoms (BRS) remain open. Objective: We aimed to investigate the association between teachers’ individual work-related symptoms and intrinsic in vitro toxicity in classrooms. This is a further analysis of a previously published dataset. Methods: Teachers from 15 Finnish schools in Helsinki responded to the symptom survey. The boar sperm motility inhibition assay, a sensitive indicator of mitochondrial dysfunction, was used to measure the toxicity of wiped dust and cultured microbial fallout samples collected from the teachers’ classrooms. Results: 231 teachers whose classroom toxicity data had been collected responded to the questionnaire. Logistic regression analysis adjusted for age, gender, smoking, and atopy showed that classroom dust intrinsic toxicity was statistically significantly associated with the following 12 symptoms reported by teachers (adjusted ORs in parentheses): nose stuffiness (4.1), runny nose (6.9), hoarseness (6.4), globus sensation (9.0), throat mucus (7.6), throat itching (4.4), shortness of breath (12.2), dry cough (4.7), wet eyes (12.7), hypersensitivity to sound (7.9), difficulty falling asleep (7.6), and increased need for sleep (7.7). Toxicity of cultured microbes was found to be associated with nine symptoms (adjusted ORs in parentheses): headache (2.3), nose stuffiness (2.2), nose dryness (2.2), mouth dryness (2.8), hoarseness (2.2), sore throat (2.8), throat mucus (2.3), eye discharge (10.2), and increased need for sleep (3.5). Conclusions: The toxicity of classroom dust and airborne microbes in boar sperm motility inhibition assay significantly increased teachers’ risk of work-related respiratory and ocular symptoms. Potential pathophysiological mechanisms of BRS are discussed.