Aspergillus niger CJ6 extract with antimicrobial potential promotes in-vitro cytotoxicity and induced apoptosis against MIA PaCa-2 cell line.

Nowadays, the increased number of multidrug-resistant strains among pathogens is a severe public health concern and cancer is posing a great threat for humans. These problems should be tackled with the development of novel and broad-spectrum antimicrobials from microbial origin. During the present study, the bioactive secondary metabolites from Aspergillus niger CJ6 were extracted, characterized; their biological properties were evaluated by subjecting them for antimicrobial, antifungal and anticancer activities. The potent isolate Aspergillus niger CJ6 with nucleotide sequence of 959 base pairs showed antagonistic activity against fungal pathogens in dual culture. The chemical profiling of crude ethyl acetate extract indicated the presence of various bioactive molecules belonging to phenolic, hydrocarbons, and phthalate derivative classes. In antimicrobial activity, the crude extract displayed increasing activity with increased concentration; the highest activity observed against Shigella flexneri with 15 ± 1.0, 19 ± 0.5, 20 ± 1.0 and 24 ± 1.0 mm zones of inhibition at 25, 50, 75 and 100 µl concentrations. The MTT assay illustrated deformed cells of MIA PaCa-2 cell line in in-vitro cytotoxic activity; outflow of cell matrix and membrane rupture; the IC50 of 90.78 µg/ml suggested moderate potential of extract to prevent cancer cell growth. The apoptosis/necrosis study by flow cytometer exhibited 8.98 ± 0.85% early and 73 ± 0.7% of late apoptotic population with 3.8 ± 1.1% necrotic cells; only 14.22 ± 0.6% of healthy cells suggested the increased apoptosis inducing capacity of Aspergillus niger CJ6 crude extract. The outcomes of this study persuade further exploration on the identification, purification and development of novel bioactive agents that could help battle fatal diseases in humans.

Phytochemical Analysis, GC-MS Profiling, and In Vitro Evaluation of Biological Applications of Different Solvent Extracts of Leonotis nepetifolia (L.) R.Br. Flower Buds.

Leonotis nepetifolia (L.) R.Br. is a medicinally important herb belonging to the family Lamiaceae. The plant is typically found in tropical regions, and its leaf and root extracts are renowned for their ethno-botanical and therapeutic applications. This study was designed to determine the presence of various bioactive components, and to evaluate antibacterial, antifungal, antioxidant, and anti-proliferative activities. The preliminary phytochemical screening and gas chromatography-mass spectrometry (GC-MS) analysis of different solvent extracts revealed the presence of various bioactive compounds, of which methanol extract showed 24 compounds, petroleum ether extract revealed 26 compounds, and 24 compounds in hexane extracts. The major bioactive components including λ-sitosterol (16.20 %) in methanol extract, 1-nonadecanol (15.48 %) in petroleum extract, and eicosane (13.22 %) in hexane extract have been reported with various bio-therapeutic applications. In addition, the flower bud methanolic extract of L. nepetifolia exhibited inhibitory potential against all tested bacterial and fungal pathogens. The DPPH radical scavenging assay revealed that methanolic extract possessed the highest antioxidant activity. The scavenging activity increased in a concentration-dependent manner, as indicated by a 74 % inhibition rate at 1000 µg/ml. Furthermore, the in vitro cytotoxic effects of the methanolic extract on the HepG2 cell line were evaluated. The IC50 value of methanolic extract against HepG2 cells was determined to be 83.28 µg/ml. The findings reveal that different solvent extracts of L. nepetifolia flower buds contain a significant amount of various bioactive phytochemicals with antioxidant and anticancer activities; and thus, the plant could serve as a potential source of pharmacological applications.

Cardioprotective effects of phytopigments via multiple signaling pathways.

BACKGROUND: Cardiovascular diseases (CVDs) are among the deadliest non-communicable diseases, and millions of dollars are spent every year to combat CVDs. Unfortunately, the multifactorial etiology of CVDs complicates the development of efficient therapeutics. Interestingly, phytopigments show significant pleiotropic cardioprotective effects both in vitro and in vivo. PURPOSE: This review gives an overview of the cardioprotective effects of phytopigments based on in vitro and in vivo studies as well as clinical trials. METHODS: A literature-based survey was performed to collect the available data on cardioprotective activities of phytopigments via electronic search engines such as PubMed, Google Scholar, and Scopus. RESULTS: Different classes of phytopigments such as carotenoids, xanthophylls, flavonoids, anthocyanins, anthraquinones alleviate major CVDs (e.g., cardiac hypertrophy, atherosclerosis, hypertension, cardiotoxicities) via acting on signaling pathways related to AMPK, NF-κB, NRF2, PPARs, AKT, TLRs, MAPK, JAK/STAT, NLRP3, TNF-α, and RA. CONCLUSION: Phytopigments represent promising candidates to develop novel and effective CVD therapeutics. More randomized, placebo-controlled clinical studies are recommended to establish the clinical efficacy of phytopigments.

An expedient synthesis and screening for antiacetylcholinesterase activity of piperidine embedded novel pentacyclic cage compounds.

The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12 ± 0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.

Student-involved demonstration approach to teach the physiology of vestibular apparatus for undergraduate medical students.

BACKGROUND: It is quite difficult to teach complex topics like the physiology of vestibular apparatus to undergraduate students. Understanding the orientation and mode of stimulation of receptors in vestibular apparatus is also quite challenging for the students. As faculty we attempt to use innovative methods to teach physiology and enhance student learning. PURPOSE: This article describes a simple and innovative method (student-involved demonstration approach, or SID) to teach the physiology of the vestibular apparatus to the undergraduate medical students. METHODS: The current study describes a protocol where students engage in role-play sessions in the middle of the regular didactic lectures. Effectiveness of the sessions was later evaluated by using a questionnaire and by comparing the pre-SID and post-SID test results of the students. RESULTS: The posttest score of the students was significantly higher than the pretest score, and this indicates the usefulness of SID sessions on enhancing the student learning in the class. CONCLUSIONS: Students also found this method very interesting and useful in better understanding the physiology of the vestibular apparatus.

Ascorbic acid protects against restraint stress-induced memory deficits in Wistar rats.

OBJECTIVE: Chronic stress has been shown to cause oxidative damage in the central nervous system. Although stress-induced impairments in learning and memory have been studied extensively, very few studies have investigated possible ways to prevent their ill effects. The present work was designed to study the protective effects of ascorbic acid in memory loss induced by chronic restraint stress. METHODS: Adult male Wistar rats were designated into the following groups: (i) Normal control, (ii) Ascorbic acid treatment, (iii) Vehicle control, (iv) Restraint stress, (v) Restraint stress + vehicle, and (vi) Restraint stress + ascorbic acid treatment. At the end of 21 days, animals of all groups were subjected to memory tests using Morris water maze and passive avoidance apparatus. Then, the results obtained were compared between the experimental groups. RESULTS: Rats exposed to restraint stress alone and those pretreated with vehicle solution before restrained stress showed deficits in learning and impaired memory retention in the memory tests when compared to animals in other experimental groups. Animals pretreated with ascorbic acid before restraining showed significant improvement in memory retention in the same memory tests. CONCLUSIONS: Results of this study suggest the possibility of using ascorbic acid as a dietary supplement to prevent stress-induced memory impairments.

Anti-arthritic potential of the plant Justicia gendarussa Burm F.

OBJECTIVE: To evaluate the anti-arthritic potential of the plant Justicia gendarussa using two different rat models. MATERIALS AND METHOD: The anti-arthritic potential of the alcoholic extract of the plant Justicia gendarussa was evaluated using the Freund's adjuvant-induced and collagen-induced arthritic rat models. The rats were treated with the ethanolic extract of Justicia gendarussa and with standard aspirin. RESULTS: The ethanolic extract of Justicia gendarussa showed significant anti-arthritic activity that was statistically similar to that of aspirin. Our results suggest that the alcoholic extract of Justicia gendarussa exhibits significant anti-arthritic potential.

Anti-arthritic potential of the plant Justicia gendarussa Burm F

OBJECTIVE: To evaluate the anti-arthritic potential of the plant Justicia gendarussa using two different rat models. MATERIALS AND METHOD: The anti-arthritic potential of the alcoholic extract of the plant Justicia gendarussa was evaluated using the Freund's adjuvant-induced and collagen-induced arthritic rat models. The rats were treated with the ethanolic extract of Justicia gendarussa and with standard aspirin. RESULTS: The ethanolic extract of Justicia gendarussa showed significant anti-arthritic activity that was statistically similar to that of aspirin. Our results suggest that the alcoholic extract of Justicia gendarussa exhibits significant anti-arthritic potential.

Ascorbic acid protects against restraint stress-induced memory deficits in wistar rats

OBJECTIVE: Chronic stress has been shown to cause oxidative damage in the central nervous system. Although stress-induced impairments in learning and memory have been studied extensively, very few studies have investigated possible ways to prevent their ill effects. The present work was designed to study the protective effects of ascorbic acid in memory loss induced by chronic restraint stress. METHODS: Adult male Wistar rats were designated into the following groups: (i) Normal control, (ii) Ascorbic acid treatment, (iii) Vehicle control, (iv) Restraint stress, (v) Restraint stress + vehicle, and (vi) Restraint stress + ascorbic acid treatment. At the end of 21 days, animals of all groups were subjected to memory tests using Morris water maze and passive avoidance apparatus. Then, the results obtained were compared between the experimental groups. RESULTS: Rats exposed to restraint stress alone and those pretreated with vehicle solution before restrained stress showed deficits in learning and impaired memory retention in the memory tests when compared to animals in other experimental groups. Animals pretreated with ascorbic acid before restraining showed significant improvement in memory retention in the same memory tests. CONCLUSIONS: Results of this study suggest the possibility of using ascorbic acid as a dietary supplement to prevent stress-induced memory impairments.