In Silico Computational Studies of Bioactive Secondary Metabolites from Wedelia trilobata against Anti-Apoptotic B-Cell Lymphoma-2 (Bcl-2) Protein Associated with Cancer Cell Survival and Resistance.

In the present study, the binding affinity of 52 bioactive secondary metabolites from Wedelia trilobata towards the anti-apoptotic B-cell lymphoma-2 (Bcl-2) protein (PDB: 2W3L) structure was identified by using in silico molecular docking and molecular dynamics simulation. The molecular docking results demonstrated that the binding energies of docked compounds with Bcl-2 protein ranged from -5.3 kcal/mol to -10.1 kcal/mol. However, the lowest binding energy (-10.1 kcal/mol) was offered by Friedelin against Bcl-2 protein when compared to other metabolites and the standard drug Obatoclax (-8.4 kcal/mol). The molecular dynamics simulations revealed that the Friedelin-Bcl-2 protein complex was found to be stable throughout the simulation period of 100 ns. Overall, the predicted Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) properties of Friedelin are relatively better than Obatoclax, with the most noticeable differences in many parameters where Friedelin has no AMES toxicity, hepatotoxicity, and skin sensitization. The ADMET profiling of selected compounds supported their in silico drug-likeness properties. Based on the computational analyses, the present study concluded that Friedelin of W. trilobata was found to be the potential inhibitor of the Bcl-2 protein, which merits attention for further in vitro and in vivo studies before clinical trials.

In vitro hypoglycemic potential of spices: Cinnamon and Cumi.

Present study evaluates the anti-hyperglycemic potential of two Indian spices Cinnamomum zeylanicum(CZ) and Cumin cyminum(CC) (whole powder and aqueous extracts) using in vitro techniques like glucose adsorption assay, amylolysis kinetics and ex vivo assays like amylase, Sucrase and α-glucosidase assay. CZ displayed higher glucose adsorption and glucose diffusion retardation than CC, as shown by glucose adsorption and amylolysis kinetics assay. CZ showed lower inhibition of α-amylase and sucrase where as CC has no effect on both the enzymes. In case of α-glucosidase, CC had better inhibition than CZ. Further research is needed to understand the mechanism through which both the spices act to regulate the hyperglycemia.

In vitro hypoglycemic effects and starch digestibility characteristics of wheat based composite functional flour for diabetics.

The associations between chronic feeding of high level of soluble/insoluble fibers and low serum glucose levels have been well documented. In the present study, composite flours were formulated using psyllium, barley and oat at two different levels [WPOB-I = wheat flour (75 %), psyllium (5 %), oat (10 %) and barley (10 %), WPOB-II = wheat flour (60 %), psyllium (10 %), oat (15 %) and barley (15 %)]. Chapaties were prepared from all formulations and various starch fractions were analyzed using controlled enzymatic digestion. The digestibility characteristics were studied using amylolysis kinetics employing porcine pancreatic α-amylase in vitro. Results showed that both the variations (WPOB-I & WPOB-II) had acceptable sensory qualities and had significantly lower (p ≤ 0.05) values for total starch (TS), rapidly digestible starch (RDS), resistant starch (RS), starch digestibility index (SDI) and rapidly available glucose (RAG) compared to control. Between the two variations, WPOB-I showed better starch digestibility characteristics with significantly lower (p ≤ 0.05) starch digestibility index (SDI). In case of amylolysis kinetics, both the variations significantly (p ≤ 0.05) inhibited α-amylase as reflected by lower glucose diffusion and significantly higher (p ≤ 0.05) glucose dialysis retardation index (GDRI) compared to control. It is inferred that, consumption of the composite flours might be helpful in establishing stable blood glucose pattern due to the redistribution of nutritionally important starch fractions and inhibition of carbohydrate digestion in the gastrointestinal tract.

In vitro hypoglycemic effects of Butea monosperma Lam. leaves and bark.

The present study evaluated the antidiabetic potential of Butea monosperma Lam. Kuntze (Fabaceae) leaves and the stem bark using various in vitro techniques. The samples were studied for their effects on glucose adsorption, diffusion, amylolysis kinetics, enteric enzymes and glucose transport across yeast cells. Both the samples adsorbed glucose and the adsorption of glucose increased with increase in glucose concentration. The samples also inhibited movement of glucose across the dialysis membrane to varying degree in both glucose diffusion and amylolysis kinetic experiment models. B. monosperma leaves inhibited α-amylase, α-glucosidase and sucrase enzymes in succession to varying degrees, whereas the bark inhibited only α-amylase to a significant extent and slightly activated α-glucosidase and sucrase enzymes. The extracts of both leaves and bark promoted glucose uptake by yeast cells compared to control. Enhancement of glucose uptake was dependent on both the sample and glucose concentration. It was directly proportional to the sample concentration and inversely proportional to the molar concentration of the glucose. From the results of the study, it is inferred that, B. monosperma leaves and bark possesses antidiabetic activity. However, these effects need to be confirmed using in vivo models and clinical trials for its effective utilization as therapeutic agents.

Survivability and behavior of probiotic bacteria encapsulated by internal gelation in non-dairy matrix and In Vitro GIT conditions.

The primary objective of this investigation was to assess the viability of free and encapsulated Lactobacillus plantarum probiotics in mango juice and under simulated gastrointestinal conditions. Specifically, the probiotics were encapsulated using sodium alginate and alginate-soy protein isolate through the internal gelation method, and the obtained probiotics were characterized for various attributes. Both free and encapsulated probiotics were exposed to challenging conditions, including thermal stress, low temperature, and simulated gastrointestinal conditions. Additionally, both types of probiotics were incorporated into mango juice, and their survival was monitored over a 28-day storage period. Following viability under simulated gastrointestinal conditions, the count of free and encapsulated probiotic cells decreased from initial levels of 9.57 log CFU/mL, 9.55 log CFU/mL, and 9.53 log CFU/mL, 9.56 log CFU/mL to final levels of 6.14 log CFU/mL, 8.31 log CFU/mL, and 6.24 log CFU/mL, 8.62 log CFU/mL, respectively. Notably, encapsulated probiotics exhibited a decrease of 1.24 log CFU and 0.94 log CFU, while free cells experienced a reduction of 3.43 log CFU and 6.24 log CFU in mango juice over the storage period. Encapsulated probiotics demonstrated higher viability in mango juice compared to free probiotics throughout the 28-day storage period. These findings suggest that mango juice can be enriched with probiotics to create a health-promoting beverage.

Isolation and characterization of pepsin-solubilized collagen from the integument of sea cucumber (Stichopus vastus).

BACKGROUND: Sea cucumber (Stichopus vastus) is considered an underutilized resource, since only its stomach and intestines are eaten raw as salad in a few countries and the remaining parts, especially the integument rich in collagen, is discarded. Hence a valuable by-product having potential nutraceutical and pharmaceutical applications is wasted. In the present investigation, pepsin-solubilized collagen (PSC) from the integument of S. vastus was isolated, purified and characterized. RESULTS: Sodium dodecyl sulfate-polyacrylamide gel electrophoretic analysis showed that the purified collagen was of type I, consisting of three α1 chains of approximately 122 kDa each. The peptide map of PSC digested by V8 protease was different from that of calf skin type I collagen. Fourier transform infrared spectroscopy revealed that the triple helical structure was well preserved in isolated collagen. The denaturation temperature of PSC was 21.23 °C and showed good gel-forming capability at pH 6.5 and 300 mmol L⁻¹ NaCl. CONCLUSION: It is inferred that the collagen isolated from S. vastus integument has potential for use as an alternative to land-based mammalian collagen in food, nutraceuticals and pharmaceutical industries.

Effect of Various Intermittent Fasting Protocols on Hyperglycemia-Induced Cognitive Dysfunction in Rats.

Diabetes mellitus is a highly prevalent metabolic disorder that causes cognitive decline. Here, we investigated the impact of various intermittent fasting protocols on type 2 diabetes mellitus (T2DM)-induced cognitive dysfunction in a rodent model. Male Sprague-Dawley rats (aged 3 months) were randomly assigned to five groups (n = 6 per group) and T2DM was induced by streptozotocin (60 mg/kg, IM). The control group was untreated. Cognitive function was tested (Y-maze, novel object recognition, and elevated plus maze tests) and glucose was assessed. The T2DM rats exhibited significantly higher blood glucose, which is associated with cognitive dysfunction. Compared to the validated animal model of T2DM in rats, various intermittent fasting protocols decreased blood glucose and improved cognitive function. These results indicate that various intermittent fasting protocols may be a potential strategy for managing the hyperglycemia-associated cognitive dysfunction.

Exploration of CviR-mediated quorum sensing inhibitors from Cladosporium spp. against Chromobacterium violaceum through computational studies.

An opportunistic human pathogenic bacterium, Chromobacterium violaceum resists the potency of most antibiotics by exploiting the quorum sensing system within their community to control virulence factor expression. Therefore, blocking the quorum sensing mechanism could help to treat several infectious caused by this organism. The quorum sensing receptor (CviR) of C. violaceum was used as a model target in the current investigation to identify potentially novel quorum sensing inhibitors from Cladosporium spp. through in silico computational approaches. The molecular docking results confirmed the anti-quorum sensing potential of bioactive compounds from Cladosporium spp. through binding to CviR with varying docking scores between - 5.2 and - 9.5 kcal/mol. Relative to the positive control [Azithromycin (- 7.4 kcal/mol)], the top six metabolites of Cladosporium spp. had higher docking scores and were generally greater than - 8.5 kcal/mol. The thermodynamic stability and binding affinity refinement of top-ranked CviR inhibitors were further studied through a 160 ns molecular dynamic (MD) simulation. The Post-MD simulation analysis confirmed the top-ranked compounds' affinity, stability, and biomolecular interactions with CviR at 50 ns, 100 ns, and 160 ns with Coniochaetone K of the Cladosporium spp. having the highest binding free energy (- 30.87 kcal/mol) and best interactions (two consistent hydrogen bond contact) following the 160 ns simulation. The predicted pharmacokinetics properties of top selected compounds point to their drug likeliness, potentiating their chance as a possible drug candidate. Overall, the top-ranked compounds from Cladosporium spp., especially Coniochaetone K, could be identified as potential C. violaceum CviR inhibitors. The development of these compounds as broad-spectrum antibacterial medicines is thus possible in the future following the completion of further preclinical and clinical research.

Cardioprotective activity of standardized extract of Ficus racemosa stem bark against doxorubicin-induced toxicity.

CONTEXT: Ficus racemosa Linn. (Moraceae) bark is a rich source of phenolic compounds having diverse biological properties including antioxidant activity. The present study evaluated the cardioprotective activity of sequential acetone extract of Ficus racemosa bark against doxorubicin-induced cardiotoxicity in rats. MATERIALS AND METHODS: The extract was standardized by high-performance liquid chromatography (HPLC) and subjected to acute toxicological evaluation in mice. Cardiotoxicity was induced by administration of doxorubicin (10 mg kg(-1) i.v.) to the extract pretreated rats (250 and 500 mg kg(-1)) and compared with that of Arjuna, a standard cardiotonic. Biochemical parameters included CK-MB, LDH, AST, ALT, troponin I, thiobarbituric acid reactive substances (TBARS), and glutathione. RESULTS: The HPLC fingerprinting of the extract indicated the presence of bergenin (0.89%) and bergapten (0.07%). In an acute toxicity study, the extract at a dose of 2 g kg(-1) did not cause any adverse changes and no mortality was observed. Administration of doxorubicin significantly increased (p ≤ 0.05) serum levels of creatine kinase, lactate dehydrogenase, aspartate aminotransferase, and alanine aminotransferase, which were decreased to an extent of 68, 63, 41, and 65%, respectively, in extract pretreated group (500 mg kg(-1)). Troponin I was undetected in control group, while it was found in serum of all the experimental groups. The extract pretreatment significantly decreased (p ≤ 0.05) TBARS and increased glutathione levels in serum and cardiac tissue. These observations were further substantiated by the histopathological studies. CONCLUSION: The acetone extract of F. racemosa bark possesses potential cardioprotective activity against doxorubicin-induced cardiotoxicity in rats by scavenging free radicals generated by the administration of the drug.

Recent Advances in Unmanned Aerial Vehicles: A Review.

In recent decades, aerial robots especially small UAVs and drones have witnessed tremendous improvements in terms of their structure, working methodology, flying features and navigation control. UAVs are highly utilized in a wide range of services such as photography, path planning, search and rescue, inspection of power lines and civil constructions, etc. This manuscript reports a wide overview and comprehensive survey of recent developments in commercially available UAV's and gives a brief note on the progress and research covered in last 10 years. The research presents a roadmap to understand the successive development of advanced drones/ UAVs in terms of their geometric structure, flying mechanism, sensing and vision ability, aviation quality, path planning, intelligent behaviour and adoptability. A literature survey is conducted systematically on 254 retrieved articles published in the last 10 years and scaled down to 96 relevant articles. In these shortlisted articles, path planning, neural network, artificial intelligence, inspection, surveillance, tracking and identification, etc. are the most relevant methodologies or applications presented. The current research is concerned about the growth and impact of UAVs/drones in the society and also inspires the newbies to carry research in this field and propose new methods to select or equip the flying robot for a specific application in various fields. This article also assists researchers in understanding and evaluating their research work in the context of existing solutions. It also helps newcomers and pilots/practitioners to quickly gain an overview of the existing vast literature in the related fields.

Salicornia bigelovii, S. brachiata and S. herbacea: Their Nutritional Characteristics and an Evaluation of Their Potential as Salt Substitutes.

Excessive sodium (salt) intake in our diet is a main contributor to hypertension and a major risk factor for cardiovascular illnesses. As a result, research has made great efforts to develop salt alternatives, and Salicornia spp. offers a very high potential in the food industry for its promising functional characteristics. This review focuses on the nutritional profile, health effects and commercial potential of three specific species of the Salicornia genus: S. bigelovii, S. brachiata and S. herbacea. It also addresses the methods that are used to produce them as salt substitutes. Owing to the antinutritional and anti-inflammatory effects of its bioactive compounds, Salicornia spp. can serve as an organic biological preservative in foods with better consumer appeal when compared with chemical preservatives that are common in the food industry. Overall, the commercial use of these underutilized species will help to improve food security.

In vitro hypoglycemic effects of selected dietary fiber sources.

The physiological functions of dietary fiber and its role in health promotion and risk reduction of some chronic diseases has been well documented. In the present investigation, the effect of three dietary fiber sources, oats (OA), barley (BA) and psyllium husk (PH) on glucose adsorption, diffusion and starch hydrolysis were studied using in vitro techniques by simulating gastrointestinal conditions and compared with the commercial dietary fiber sources wheat bran (WB), acarbose (ACB) and guar gum (GG). The glucose binding capacity of all the samples was higher than WB and ACB at 5 mM concentration. In all the samples, the diffusion of glucose was directly proportional to the time and diffusion rate was significantly lower (p ≤ 0.01) in the system containing various samples compared to control. Glucose dialysis retardation index (GDRI) was 100 for OA, BA and PH at 60 min, at 120 min the maximal GDRI was in PH. Whereas; WB and ACB exhibited maximal GDRI at 180 and 240 min. All of these mechanisms might create a concerted function in lowering the rate of glucose absorption and as a result, decrease the postprandial hyperglycemia.

Ganoderma lucidum: A potential source to surmount viral infections through ß-glucans immunomodulatory and triterpenoids antiviral properties.

Ganoderma lucidum (G. lucidum) polysaccharides and triterpenoids are the major bioactive compounds and have been used as traditional medicine for ancient times. Massive demands of G. lucidum have fascinated the researchers towards its application as functional food, nutraceutical and modern medicine owing to wide range of application in various diseases include immunomodulators, anticancer, antiviral, antioxidant, cardioprotective, hepatoprotective. G. lucidum polysaccharides exhibit immunomodulatory properties through boosting the action of antigen-presenting cells, mononuclear phagocyte system, along with humoral and cellular immunity. ß-Glucans isolated from G. lucidum are anticipated to produce an immune response through pathogen associated molecular patterns (PAMPs). ß-Glucans after binding with dectin-1 receptor present on different cells include macrophages, monocytes, dendritic cells and neutrophils produce signal transduction that lead to trigger the mitogen-activated protein kinases (MAPKs), T cells and Nuclear factor-κB (NF-κB) that refer to cytokines production and contributing to immune response. While triterpenoids produce antiviral effects through inhibiting various enzymes like neuraminidase, HIV-protease, DENV2 NS2B-NS3 protease and HSV multiplication. Polysaccharides and triterpenoids adjunct to other drugs exhibit potential action in prevention and treatment of various diseases. Immunomodulators and antiviral properties of this mushroom could be a potential source to overcome this current pandemic outbreak.

Radical scavenging and angiotensin converting enzyme inhibitory activities of standardized extracts of Ficus racemosa stem bark.

The present study evaluated the radical scavenging and angiotensin converting enzyme (ACE) inhibitory activity of cold and hot aqueous extracts of Ficus racemosa (Moraceae) stem bark. The extracts were standardized using HPLC. Radical scavenging activity was determined using 1,1-diphenyl-2-picrylhydrazyl radical and angiotensin converting enzyme inhibitory activity using rabbit lung and partially purified porcine kidney ACE. HPLC profiles of cold aqueous extract (FRC) showed the presence of bergenin, an isocoumarin, while hot aqueous extract (FRH) was found to contain ferulic acid, kaempferol and coumarin in addition to bergenin. FRH showed significantly higher (p ≤ 0.01) radical scavenging activity than FRC and butylated hydroxytoluene (BHT), consequently resulting in a significantly lower (p ≤ 0.01) IC50 value than FRC and BHT. Both the extracts exhibited a dose dependent inhibition of porcine kidney and rabbit lung ACE. FRH showed significantly higher (p ≤ 0.01) activity than FRC with lower IC(50) values of 1.36 and 1.91 µg/mL respectively, for porcine kidney and rabbit lung ACE, compared with those of FRC (128 and 291 µg/mL). Further, a significant correlation (r = 0.893; p ≤ 0.05) was observed between radical scavenging activity and ACE-inhibitory activity. This is the first report on the ACE-inhibitory activity of F. racemosa stem bark suggesting its potential to be utilized as a therapeutic alternative for hypertension.

In vitro studies on the hypoglycemic potential of Ficus racemosa stem bark.

BACKGROUND: Medicinal plants have been reported to play an important role in modulating glycemic responses and have preventive and therapeutic implications. Several mechanisms have been proposed for the antidiabetic effect of medicinal plants such as inhibition of carbohydrate-metabolizing enzymes, manipulation of glucose transporters, beta-cell regeneration and enhancing insulin-releasing activity. The present investigation evaluated the possible mechanism of action through which Ficus racemosa stem bark (Moraceae) exerts its hypoglycemic effect using suitable in vitro techniques. RESULTS: Ficus racemosa bark (FRB) exhibited significantly higher (P < or = 0.01) glucose-binding capacity than wheat bran (WB) and acarbose (ACB) consequently showed significantly higher (P < or = 0.01) retardation of glucose diffusion compared to WB and ACB. In case of amylolysis kinetics the liberation of glucose was greatly inhibited by FRB, as reflected by a significantly lower (P < or = 0.01) glucose diffusion rate in the system containing FRB compared to the control and acarbose. Furthermore, FRB significantly increased (P < or = 0.01) the rate of glucose transport across the yeast cell membrane and also in isolated rat hemi-diaphragm. CONCLUSION: The findings indicate F. racemosa bark to possess strong hypoglycemic effect and hence can be utilized as an adjunct in the management of diabetes mellitus.

Traditional uses, medicinal properties, and phytopharmacology of Ficus racemosa: a review.

Ficus racemosa Linn. (Moraceae) is a popular medicinal plant in India, which has long been used in Ayurveda, the ancient system of Indian medicine, for various diseases/disorders including diabetes, liver disorders, diarrhea, inflammatory conditions, hemorrhoids, respiratory, and urinary diseases. F. racemosa is pharmacologically studied for various activities including antidiabetic, antipyretic, anti-inflammatory, antitussive, hepatoprotective, and antimicrobial activities. A wide range of phytochemical constituents have been identified and isolated from various parts of F. racemosa. In this review, a comprehensive account of its traditional uses, phytochemical constituents, and pharmacological effects is presented in view of the many recent findings of importance on this plant.

Effect of Ficus racemosa stem bark on the activities of carbohydrate hydrolyzing enzymes: an in vitro study.

Herbal medicines have been used since prehistoric times by different cultures worldwide for the treatment of diabetes. The present investigation evaluated the effect of Ficus racemosa Linn. (Moraceae) stem bark on carbohydrate hydrolyzing enzymes, viz., porcine pancreatic alpha-amylase, rat intestinal alpha-glucosidase, sucrase, and almond beta-glucosidase, using in vitro model systems. In addition, the effect of heat treatment was also studied. Untreated F. racemosa bark (FRB) significantly inhibited (p < or = 0.05) alpha-amylase, alpha-glucosidase, beta-glucosidase, and sucrase in a dose-dependent manner. Heat treatment of the sample comparably increased alpha-amylase, alpha-glucosidase, and sucrase inhibitory activities, while a marginal decrease in beta-glucosidase inhibitory activity was observed; however, no statistical differences were noted. Untreated FRB showed IC(50) values of 0.94% and 280, 212, and 367 microg/mL for alpha-amylase, alpha-glucosidase, beta-glucosidase, and sucrase, respectively, while the IC(50) values for heat treated FRB were 0.58% and 259, 223, and 239 microg/mL, respectively. Further, a significant correlation (p < or = 0.01; r = 0.791) was observed between alpha-amylase, alpha-glucosidase, beta-glucosidase, and sucrase inhibitory activities of both untreated and heat treated FRB. The results clearly demonstrate that inhibition of carbohydrate hydrolyzing enzymes is one mechanism through which F. racemosa stem bark exerts its hypoglycemic effect in vivo. Therefore, the potential exists to explore the utilization of F. racemosa stem bark in the development of nutraceuticals and functional foods for the management of diabetes and related symptoms/disorders.

Hepatoprotective effects of Ficus racemosa stem bark against carbon tetrachloride-induced hepatic damage in albino rats.

In the present study, the hepatoprotective effects of petroleum ether (FRPE) and methanol (FRME) extract of Ficus racemosa Linn. (Moraceae) stem bark were studied using the model of hepatotoxicity induced by carbon tetrachloride (CCl(4)) in rats. CCl(4) administration induced a significant decrease in serum total protein, albumin, urea and a significant increase (P

Antimicrobial efficacy of nanosilver and chitosan against Streptococcus mutans, as an ingredient of toothpaste formulation: An in vitro study.

CONTEXT: Dental caries is the most prevalent oral infection affecting the humankind worldwide, and Streptococcus mutans is the major microrganism involved in its pathology. Mechanical plaque control in children is not performed efficiently and thus necessitates the inclusion of certain antimicrobial agents in the toothpaste. AIM: To analyze the antibacterial efficacy of nanosilver, chitosan, and fluoride as an ingredient in the dentifrices against S. mutans strains and comparing them with each other. SUBJECTS AND METHODS: Pure culture of S. mutans strain (MTCC 890) was obtained from the Institute of Microbial Technology, Chandigarh, India. Nanosilver (Group 1)- and chitosan (Group 2)-containing toothpastes were obtained from the respective dealers, and fluoride (Group 3) toothpaste was obtained from the local market. The antimicrobial activity of the three toothpastes was determined by modified agar well diffusion method. Saline was kept as the control. STATISTICAL ANALYSIS USED: Unpaired t-test was done for intergroup comparisons. RESULTS: Statistically significant differences between Groups 1 and 2, Groups 1 and 3, and Groups 2 and 3 were seen. CONCLUSIONS: Nanosilver-containing toothpaste has the highest antibacterial efficacy against S. mutans, followed by fluoride- and chitosan-containing toothpaste.