Insights into the radioprotective efficacy of Pterocarpus santalinus L. aqueous extract.

In the present study, we have attempted a comprehensive assessment of the possible radioprotective efficacy of Pterocarpus santalinus aqueous extract (PSAE). All the studied models were gamma-irradiated with prior treatment with PSAE. First, the content of total phenols (4.061 µg/mg gallic acid equivalents), flavonoids (6.616 µg/mg quercetin equivalents), and tannins (0.008 mg/L of PSAE) were determined spectrophotometrically. Second, UHPLC-HRMS analysis was performed to identify the possible radioprotectors. Of those, santalins A & B are known for their usage as natural color in foods and alcoholic beverages identified in PSAE. Treatment was well tolerated with no side effects from PSAE. Later, it was shown that radiation-induced lethality significantly amended in PSAE-treated spleen lymphocytes as evidenced by reduced elevated levels of ROS and lipid peroxidation, restored total thiols and GSH: GSSG, inhibited DNA DSBs and cell death. Furthermore, an immunomodulation study was carried out because radiation exposure induces an inflammatory response. Our study shows that PSAE suppressed concanavalin A-induced T-cell proliferation as evidenced by CFSE dye dilution and CD69 antibody staining methods. Taken together, the current study explored the protective efficacy of PSAE from gamma radiation-inflicted injuries and hence we recommend PSAE as a potent radioprotective formulation.

Thymoquinone mitigates obesity and diabetic parameters through regulation of major adipokines, key lipid metabolizing enzymes and AMPK/p-AMPK in diet-induced obese rats.

The present study was designed to evaluate the anti-obesity and anti-hyperglycemic activity of Thymoquinone (ThyQ) isolated from Nigella sativa seeds. Male Wistar rats were randomly divided into five groups and fed either normal pellet diet or high-fat diet (HFD) for 18 weeks and water ad-libitum. Group I: normal pellet diet (NPD)-fed, Group II: high-fat diet (HFD)-fed, Group III: HFD-fed-ThyQ (20 mg)-treated, Group IV: HFD-fed-ThyQ (40 mg)-treated and Group V: HFD-fed-Orlistat (5 mg)-treated group. Intervention with ThyQ started from 12th week onwards to HFD-fed rats of group III and IV. ThyQ administration significantly (p < 0.01) mitigated body weight gain, blood glucose, insulin level, serum and liver lipids (except HDL) and improved glucose tolerance and insulin sensitivity as evaluated by oral glucose tolerance test (OGTT), homeostasis model assessment-insulin resistance (HOMA-IR) and insulin tolerance test (ITT). Furthermore, ThyQ significantly (p < 0.01) diminished serum aspartate transaminase (AST), alanine transaminase (ALT), acetyl-CoA carboxylase (ACC), plasma leptin, resistin and visfatin levels but enhanced lipoprotein lipase (LPL) and adiponectin levels. RT-PCR analysis demonstrated down-regulated mRNA expression of sterol regulatory element-binding proteins-1c (SREBP-1c), CCAAT/enhancer-binding protein-α (C/EBP-α) and fatty acid synthase (FAS) but upregulation of Insulin receptor substrate-1 (IRS-1).Western blot analysis displayed phosphorylation of adenosine monophosphate activated protein kinase (AMPK) in ThyQ-treated rats. Liver microtome sections of HFD-fed rats showed degenerated hepatocytes with high lipid stores while that of adipose tissue sections displayed large, fat-laden adipocytes, however, these histological changes were considerably attenuated in ThyQ-treated groups. Together these findings demonstrate that ThyQ can be a valuable therapeutic compound to potentially alleviate diet-induced obesity, hyperglycemia and insulin resistance. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-023-03847-x.

Ursolic acid regulates key EMT transcription factors, induces cell cycle arrest and apoptosis in MDA-MB-231 and MCF-7 breast cancer cells, an in-vitro and in silico studies.

Epithelial-mesenchymal transition (EMT) is a vital process in tumorigenesis and metastasis of breast cancer. In our quest to explore effective anticancer alternatives, ursolic acid (UA) was purified from Capparis zeylanica and investigated for its anticancer activity against MDA-MB-231 and MCF-7 breast cancer cells. The apparent anticancer activity of UA on MDA-MB-231 and MCF-7 cells was evident from IC50 values of 14.98 and 15.99 µg/mL, respectively, in MTT assay and also through enhanced generation of ROS. When MDA-MB-231 and MCF-7 cells were treated with 20 µg/mL UA, an absolute decrease in cell viability of 47.6% and 48.6%, enhancement of 1.35% and 1.10% in early apoptosis, and 21.90% and 21.35% in late apoptosis, respectively and G0 /G1 phase, S phase, G2 /M phase cell cycle arrest was noticed. The gene expression studies revealed that UA could significantly (p < 0.001) downregulate the expression of EMT markers such as snail, slug, and fibronectin at molecular level. Further, the obtained in vitro results of snail, slug, and fibronectin were subjected to quantum-polarized-ligand (QM/MM) docking, which predicted that the in silico binding affinities of these three markers are in good correlation with strong hydrogen and van der Waal interactions to UA with -53.865, -48.971 and -40.617 MMGBSA (ΔGbind ) scores, respectively. The long-range molecular dynamics (50 ns) simulations have showed more consistency by UA. These findings conclude that UA inhibits breast cancer cells growth and proliferation through regulating the expression of key EMT marker genes, and thus UA is suggested as a potential anticancer agent.

Quercetin-3-O-rutinoside from Moringa oleifera Downregulates Adipogenesis and Lipid Accumulation and Improves Glucose Uptake by Activation of AMPK/Glut-4 in 3T3-L1 Cells.

Natural product-based therapeutic alternatives have drawn immense interest to deal with growing incidence of metabolic disorders. Rutin (quercetin-3-O-rutinoside) is found in a variety of fruits, vegetables, and plant beverages. In the present study, rutin was isolated from Moringa oleifera Lam., leaves and its anti-lipidemic and anti-adipogenic activity was evaluated through inhibition of key digestive enzymes and in vitro cell culture experiments using 3T3-L1 adipocytes. Rutin treatment substantially reduced α-glucosidase and pancreatic lipase activities with IC50 values of 40 and 35 µg/ml, respectively. MTT assay with 3T3-L1 cells demonstrated the non-toxic effect of rutin up to 160 µg/ml. Oil Red O-stained images of rutin-treated 3T3-L1 cells depicted that rutin considerably reduced lipid content and adipogenesis (79.9%), and enhanced glycerol release in 3T3-L1 cells when compared to untreated cells. Rutin significantly (p < 0.05) enhanced glucose uptake in 3T3-L1 adipocytes and also led to reduced levels of leptin but enhanced levels of adiponectin. Western blot analysis of rutin-treated (40 µg/ml) adipocytes showed phosphorylation of AMPK, upregulated expression of Glut-4 (1.31-fold) and UCP-1 (1.47-fold), but downregulated expression of PPAR-γ by 0.73-fold. At transcriptional level, similar trends were observed in the mRNA expression of the above genes, except AMPK. Our results demonstrate that rutin isolated from M. oleifera significantly alleviates lipid content and adipogenesis, and improves glucose uptake through regulating PPAR-γ and AMPK signaling pathways; thus, rutin can be considered as a potential therapeutic agent against adiposity and glucose intolerance.

Capparis zeylanica L. root extract promotes apoptosis and cell cycle arrest, inhibits epithelial-to-mesenchymal transition and triggers E-cadherin expression in breast cancer cell lines.

Capparis zeylanica L. is a climbing shrub distributed in Indian subcontinent and Mediterranean region. Almost all parts of the plant are used in folk medicine and traditional practices to treat several human ailments. The present study was aimed to investigate the role of C. zeylanica L. root extract in preventing cancerous cells growth and proliferation, as well as promoting apoptosis and cell cycle arrest in MDA-MB-231 and MCF-7 breast cancer cells. Methanolic extract of C. zeylanica L. (MECz) was prepared and characterized by LC-ESI-MS/MS analysis. In vitro cytotoxicity and anti-proliferative activity of MECz was evaluated by MTT assay, while cell viability, apoptosis and cell cycle progression by Muse Cell analyzer. Furthermore, the mRNA and protein expressions of EMT markers were assessed using qRT-PCR and western blotting techniques, respectively. The MECz was found to be rich in phenolic compounds including chlorogenic acid, 6-gingerol, and certain triterpenes like ursolic acid etc. The apparent anti-metastasis activity of MECz was evident from IC50 value of 19.12 and 24.22 µg/mL, respectively, on MDA-MB-231 and MCF-7 cells in MTT assay. An absolute decrease in cell viability (78.1-53.4% and 89.9-49.0%), augmented apoptosis (90.98-48.25% and 88.25-47.70%) and S phase, G2/M phase cell cycle arrest was found by MECz treatment on MDA-MB-231 and MCF-7 cells. The gene expression studies revealed that MECz could significantly (p < 0.001) regulate the expression of EMT markers such as snail, slug, zeb-1, twist-1, fibronectin, vimentin and E-cadherin at molecular level. These findings demonstrate that C. zeylanica L. root extract inhibits breast cancer cells growth and proliferation through regulating the expression of key EMT marker genes and proteins. Thus, MECz may be suggested as a potential anti-metastasis agent in the treatment of breast cancer.

Anti-adipogenic and lipid-lowering activity of piperine and epigallocatechin gallate in 3T3-L1 adipocytes.

The present study was aimed to evaluate the anti-adipogenic activity of piperine (PIP) and epigallocatechin gallate (EGCG) in 3T3-L1 cells. In cytotoxicity studies, PIP and EGCG showed IC50 values of 260 and 218 µM respectively and in combination (20 µM each) did not show cytotoxicity. Treatment with PIP and EGCG (20 µM each) significantly (p<.01) inhibited cell differentiation, lipid droplets deposition and enhanced glycerol release in 3T3-L1 cells. The secreted level of leptin was decreased but adiponectin level was increased in treated 3T3-L1 cells than untreated cells. In molecular expression studies, key adipogenic genes PPAR-γ, SREBP-1c, FAS, Fab-4, C/EBP-α and HMG-CoA reductase were markedly down-regulated but UCP-1 was up-regulated intreated 3T3-L1 cells and the same trend was observed in expression levels of selected proteins. In conclusion, our results demonstrated a combination of PIP and EGCG exhibited strong anti-adipogenic and lipid lowering effect than individual treatments due to synergism.

Astragalin, (3-O-glucoside of kaempferol), isolated from Moringa oleifera leaves modulates leptin, adiponectin secretion and inhibits adipogenesis in 3T3-L1 adipocytes.

Inhibition of adipogenesis is crucial and is a key area of research to develop antiobesity drugs. In this study, 3-O-glucoside of kaempferol (astragalin) was isolated from Moringa oleifera leaves and evaluated for its lipolytic and antiadipogenic activity in 3T3-L1 adipocytes. Astragalin has substantially reduced the triglycerides content and lipid accumulation in 3T3-L1 adipocytes and enhanced the glycerol release in a dose dependent manner. The assay for secreted adipocytokines confirmed that, astragalin at a concentration of 20 µg/mL significantly (p < .01) increased the secretion of adiponectin, but decreased leptin secretion in 3T3-L1 adipocytes. In molecular studies, both the mRNA expression and corresponding protein expression of PPAR-γ, C/EBP-α, FAS, and leptin genes were downregulated while that of adiponectin was upregulated in astragalin treated groups. Taken together, astragalin of M. oleifera promotes lipolysis, suppresses adipogenesis in 3T3-L1 adipocytes, and may be considered as an effective candidate to treat obesity aliments.

A bioactive fraction of Pterocarpus santalinus inhibits adipogenesis and inflammation in 3T3-L1 cells via modulation of PPAR-γ/SREBP-1c and TNF-α/IL-6.

Pterocarpus santalinus has huge demand owing to its commercial and medicinal value. However, there are limited research studies on its therapeutic activity against obesity and obesity-induced inflammation and underlying mechanism of action. Therefore, in the present study, chloroform bioactive fraction of P. santalinus (CFP) was isolated and evaluated for its activity against adipogenesis and adipogenesis-induced inflammation in 3T3-L1 cell culture model. LC-MS/MS analysis of CFP was performed to identify the compounds present. CFP-treated 3T3-L1 cells (50, 100 and 200 µg/ml) have significantly (p < 0.01 or < 0.05) enhanced glycerol release and adiponectin level, but reduced lipid accumulation and leptin, and MTT assay demonstrated CFP was non-toxic till a dose of 300 µg/ml at 24 and 48 h. A considerable reduction in tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels was witnessed in lipopolysaccharide (LPS)-induced 3T3-L1 cells with CFP treatment in dose-dependent manner. Gene expression studies demonstrated down-regulation of mRNA expression of peroxisome proliferator-activated receptor-γ (PPAR-γ), sterol regulatory element-binding protein-1c (SREBP-1c), leptin, TNF-α and IL-6 but up-regulation of adiponectin and uncoupling protein-1 (UCP-1) and the same trend was observed in protein expression also. In conclusion, it is suggested that CFP could be beneficial to treat obesity and associated inflammation.

Plant Polyphenolic Compounds Potentiates Therapeutic Efficiency of Anticancer Chemotherapeutic Drugs: A Review.

BACKGROUND: Scientific research continues to develop more efficacious drugs to treat and cure cancer, the dreadful disease threatening the human race. Chemotherapy is an essential means in cancer therapy, however, plant drugs having pharmacological safety, can be used alone or as additions to current chemotherapeutic agents to enhance therapeutic efficacy and minimize chemotherapyinduced adverse effects. OBJECTIVE: A combination therapy where the synergistic effect on multiple targets is possible has gained significance because a one-drug one-target approach fails to yield the desired therapeutic effect. Therefore, a detailed description of important plant polyphenolic compounds with anticancer activity and their role in potentiating chemotherapeutic efficiency of existing anticancer drugs is provided in this review. Systematically screening combinations of active pharmaceutical ingredients for potential synergy with plant compounds may be especially valuable in cancer therapy. METHODS: We extensively have gone through reviews and research articles available in the literature. We made use of databases such as Google Scholar, Research Gate, PubMed, Science Direct, etc. The following keywords were used in our literature search: "Chemotherapy, drug development, cancer drugs, plant-derived polyphenolics, synergistic studies, combination therapy, diagnosis and genetics." CONCLUSION: Systematic research studies on screening combinations of plant phytochemicals with potential chemotherapeutic pharmaceuticals shed light on their synergistic effects, mechanisms of actions paving the way to develop more efficient anticancer therapeutics to treat and cure the cancer menace, to nullify chemotherapy-induced adverse effects and our review substantially contributes in this direction.

Antiobesity efficacy of asiatic acid: down-regulation of adipogenic and inflammatory processes in high fat diet induced obese rats.

In the current study, we evaluated the effects of Asiatic acid (AA) on lipid metabolic markers in HFD-induced obese Sprague-Dawley rat model. AA (20 mg/kg BW) was administered orally to HFD-fed rats for 42 days. Changes in body composition, glucose, insulin resistance (IR) and lipid profiles of tissues, plasma and the pattern of gene expression of peroxisome proliferator-activated receptor-γ (PPAR-γ) and its target genes fatty-acid synthase (FAS), adipocyte protein-2 (aP2) and uncoupling protein-2 (UCP-2) and pro-inflammatory factor tumor necrosis factor (TNF)-α were observed in experimental rats. Oral administration of AA exerts therapeutic effects similar to orlistat in attenuating body weight gain, glucose, IR, plasma and tissue lipids and mRNA levels of PPAR-γ, FAS, aP2 and inflammatory factor TNF-α and increasing UCP-2 expression in HFD-fed rats. Hence, these findings concluded that AA attenuate HFD-induced obesity by modulating PPAR-γ and its target genes and regulate lipid metabolism, suggesting their possible antiobesity effects.

Sensitivity of glutathione S-transferases to high doses of acrylamide in albino wistar rats: Affinity purification, biochemical characterization and expression analysis.

The main objectives of this study were to purify the glutathione S-transfereses (GSTs) and assess the effect of high doses of acrylamide (ACR) on male albino Wistar rat liver, kidney, testis and bran GST activities, and expression analysis of GST. ACR (50 mg/300 ml) was ingested for 40 days (20 doses) in drinking water on alternative days, on 40 day post ingestion the control and treated tissues were collected for GST purification by affinity column and biochemical characterization of GSTs by substrate specificities, and GST expression by immuno dot blots. In the analysis of the purified GSTs, we observed that liver GSTs were resolved in to three bands known as Yc, Yb and Ya; kidney GSTs were resolved in to two bands known as Yc and Ya; testis and brain GSTs were resolved as four bands known as Yc, Yb, Yß and Yδ on 12.5% sodium dodecyl sulfate polyacrylamide gel (SDS PAGE). In the analysis of biochemical characterization, we observed a significant decrease (p < 0.05) in the specific activities of liver GST isoforms with the substrates 1-chloro 2,4-dinitrobenzene (CDNB), bromosulfophthalein (BSP), p-nitrophenyl acetate (pNPA), p-nitrobenzyl chloride (pNBC) and cumene hydroperoxide (CHP), but showed no activity with ethacrynic acid (ECA) and significant decrease (p < 0.05) in the specific activities of kidney GST isoforms with the substrates CDNB, pNPA, pNBC and CHP, but showed no activity with BSP and ECA, and a significant decrease (p < 0.05) in the specific activities of testis and brain GST isoforms with the substrates CDNB, BSP, pNPA, pNBC, ECA and CHP. In the analysis of immuno dot blots, we observed a decreased expression of liver, kidney, testis and brain GSTs. Through the affinity purification and biochemical characterization, we observed a tissue specific distribution of GSTs that is liver GSTs possess Yc, Yb and Ya sub units known as alpha (α) and mu (µ) class GSTs; kidney GSTs possess Yc and Ya sub units known as (α) alpha class GST; testis and brain GSTs possess Yc, Yb, Yß and Yδ sub units known as alpha (α), mu (µ) and pi (π) class GSTs. Purification studies, biochemical characterization and immuno dot blot analysis were revealed the GSTs were sensitive to high doses of ACR and the high level exposure to ACR cause the damage of detoxification function of GST due to decreased expression and hence lead to cellular dysfunction of vital organs.

Role of glutathione S-transferases in detoxification of a polycyclic aromatic hydrocarbon, methylcholanthrene.

Glutathione S-transferases (GSTs), the versatile phase II biotransformation enzymes, metabolize and detoxify a wide variety of toxic chemical compounds like carcinogens, chemotherapeutic drugs, environmental pollutants and oxidative stress products. GSTs are currently of great interest in drug discovery, nanotechnology and biotechnology because of their involvement in many major cellular processes. GSTs, which are either homo or hetero dimeric proteins mediate catalytic binding between glutathione (GSH) and an array of either endogenous or exogenous toxic compounds to form a highly soluble detoxified complex which is then eliminated. Polycyclic aromatic hydrocarbons (PAHs) which are composed of two or more benzene rings bonded as linear, cluster or angular arrangements are used as intermediaries in pharmaceuticals, agricultural products, photographic products, thermosetting plastics, lubricating materials and other chemical products. Foods those cooked at high temperatures by grilling, roasting, frying and smoking are the main sources for the persistent bio-accumulation of PAHs in food chain. The carcinogenic, mutagenic and immunosuppressive effects of PAHs are well established. A well-known polycyclic aromatic hydrocarbon, methylcholanthrene is a potential carcinogenic, neurotoxic, mutagenic and tumour causing agent that is used as an experimental carcinogen in biological research. Methylcholanthrene converts into reactive metabolites when it enters living cells and those reactive metabolites oxidize DNA, RNA, proteins and lipids and form DNA and protein adducts as well. GSTs play major role in the detoxification of reactive metabolites of methylcholanthrene by mediating catalytic binding with GSH to form a highly soluble detoxified complex which is then eliminated. This review summarizes the role of GSTs in the detoxification of a polycyclic aromatic hydrocarbon, methylcholanthrene.

Genetic polymorphism of glutathione S-transferases: Relevance to neurological disorders.

Glutathione S-tranferases (GSTs) are phase II drug metabolizing enzymes, they play crucial role in detoxification of environmental pollutants, carcinogens, drugs, xenobiotics and oxidative stress products. Genetic differences in expression and activity of GSTs are due to the existence of polymorphic alleles which encode them. Because of genetic polymorphism the GST activity has altered that lead to the increased susceptibility for toxic chemical compounds. GST genetic polymorphism is the main reason for many neurological dysfunctions. GST has over expressed in epileptic brain and pi (π) GST has used to predict stroke; mu (µ) and pi (π) GST are over expressed in Alzheimer's disease (AD). Null and single nucleotide polymorphism of GST has associated with many neurodisorders. Over all, it can be concluded that the GST genetic polymorphism has associated with neurodegenerative diseases.

The effects of Ficus carica on the activity of enzymes related to metabolic syndrome.

The present study aimed to investigate the effects of the various parts of Ficus carica L. (figs) on antioxidant, antidiabetic, and antiobesogenic effects in vitro. Fruit, leaves, and stembark of the F. carica plant were sequentially extracted using organic and inorganic solvents and their total polyphenol and flavonoid contents were estimated. The effects of the extracts on antioxidative, antidiabetic (inhibition of α-amylase and α-glucosidase enzymes), and antiobesogenic (antilipase) activities were measured using several experimental models. The fruit ethanolic extract contained a high quantity of polyphenols and flavonoids (104.67±5.51 µg/mL and 81.67±4.00 µg/mL) compared with all other extracts. The activity of the ethanolic extract of F. carica fruit was significantly (p<0.05) higher than all other extracts and parts of the plant in terms of antioxidative, antidiabetic, and antiobesogenic effects. The IC50 values of the fruit ethanolic extract in terms of antioxidative (134.44±18.43 µg/mL), and inhibition of α-glucosidase (255.57±36.46 µg/mL), α-amylase (315.89±3.83 µg/mL), and pancreatic lipase (230.475±9.65 µg/mL) activity indicate that the activity of fruit ethanolic extract is better than all other extracts of the plant. The gas chromatography-mass spectroscopy analysis of the fruit ethanolic extract showed the presence of a number of bioactive compounds such as butyl butyrate, 5-hydroxymethyl furfural, 1-butoxy-1-isobutoxy butane, malic acid, tetradecanoic acid, phytol acetate, trans phytol, n-hexadecanoic acid, 9Z,12Z-octadecadienoic acid, stearic acid, sitosterol, 3,5-dihydroxy-6-methyl-2,3-dihydro-4H-pyran-4-one, and 2,4,5-trimethyl-2,4-dihydro-3H-pyrazol-3-one. The results of this study suggest that the ethanolic extract of the fruit of F. carica may have potential antidiabetic and antiobesogenic agents.

Glutathione S-transferase is a good biomarker in acrylamide induced neurotoxicity and genotoxicity.

Glutathione S-transferases (GSTs) are major defence enzymes of the antioxidant enzymatic system. Cytosolic GSTs are more involved in the detoxification than mitochondrial and microsomal GSTs. GSTs are localized in the cerebellum and hippocampus of the rat brain. Acrylamide (AC) is a well assessed neurotoxin of both animals and humans and it produces skeletal muscle weakness and ataxia. AC is extensively used in several industries such as cosmetic, paper, textile, in ore processing, as soil conditioners, flocculants for waste water treatment and it is present in daily consumed food products, like potato chips, French fries, bread, breakfast cereals and beverages like coffee; it is detected on tobacco smoking. GST acts as a biomarker in response to acrylamide. AC can interact with DNA and therefore generate mutations. In rats, low level expression of glutathione S-trasferase (GST) decreases both memory and life span. The major aim of this review is to provide better information on the antioxidant role of GST against AC induced neurotoxicity and genotoxicity.

Radioprotective Properties of Pterocarpus santalinus Chloroform Extract in Murine Splenic Lymphocytes and Possible Mechanism.

Background: Pterocarpus santalinus popularly known as Red Sanders is an endemic species confined to Southern part of Eastern Ghats of India especially in Andhra Pradesh and has high demand for its economical importance for its use in treatment of human ailments. Materials and Methods: In the present study, the authors have examined the presence of various phytochemicals in the chloroform extract of P. santalinus heartwood (PSCE, Pterocarpus santalinus chloroform extract) by qualitative and quantitative assays. PSCE was further used to evaluate its antioxidant and metal reducing capacity. Radioprotective property was also evaluated in various subcellular and cellular model systems. Results: The phytochemical screening study showed that the extract was positive for carbohydrates, cardiac glycosides, flavonoids, phenols, tannins, saponins, and terpenoids and was negative for alkaloids, steroids, and phlobatannins. Contents of total phenol, total flavonoids, total anthocyanin, and total tannin in the PSCE are 404 µg/mg in terms of gallic acid equivalents, 22.6 µg/mg in terms of quercetin equivalents, 0.066 mg in terms of cyanidin-3-glucoside (cyn-3-glu) equivalents, and 12.477 g/L, respectively. This extract exhibited significant radical scavenging activity against model free radical 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) radical (ABTS•+), 1,1-diphenyl picrylhydrazyl, and biologically important nitric oxide. It has significant metal reducing capacity as monitored by ferric and molybdenum reduction assay. PSCE showed a concentration dependent radioprotection to plasmid pBR322 DNA and lipids of the mitochondrial membranes. Their study also showed that PSCE protected splenic lymphocytes against radiation induced cell death, DNA double strand breaks, and lipid peroxidation as monitored by propidium iodide staining, γ-H2AX assay, neutral comet assay, and TBARS assay, respectively. Addition of PSCE to lymphocytes scavenged radiation derived reactive oxygen species, restored loss of thiol content, and inhibited cellular apoptosis. Conclusions: PSCE possesses high antioxidant activity and exhibited very good radioprotective property in cell free and cellular model systems.

Correction to: Antiobesity potential of Piperonal: promising modulation of body composition, lipid profiles and obesogenic marker expression in HFD-induced obese rats.

[This corrects the article DOI: 10.1186/s12986-017-0228-9.].

Antiobesity potential of Piperonal: promising modulation of body composition, lipid profiles and obesogenic marker expression in HFD-induced obese rats.

Background: Black pepper or Piper nigrum is a well-known spice, rich in a variety of bioactive compounds, and widely used in many cuisines across the world. In the Indian traditional systems of medicine, it is used to treat gastric and respiratory ailments. The purpose of this investigation is to study the antihyperlipidemic and antiobesity effects of piperonal in high-fat diet (HFD)-induced obese rats. Methods: Piperonal, an active constituent of Piper nigrum seeds, was isolated and confirmed by HPLC, 1H and 13C NMR spectroscopy. Male SD rats were fed on HFD for 22 weeks; Piperonal was supplemented from the 16th week as mentioned in the experimental design. Changes in body weight and body composition were measured by TOBEC, bone mineral composition and density were measured by DXA, and adipose tissue distribution was measured by 7 T-MRI. Plasma levels of glucose, insulin, insulin resistance and lipid profiles of plasma, liver and kidney, adipocyte hormones and liver antioxidants were evaluated using standard kit methods. Expression levels of adipogenic and lipogenic genes, such as PPAR-γ, FAS, Fab-4, UCP-2, SREBP-1c, ACC, HMG-COA and TNF-α were measured by RT-PCR. Histopathological examination of adipose and liver tissues was also carried out in experimental rats. Results: HFD substantially induced body weight, fat%, adipocyte size, circulatory and tissue lipid profiles. It elevated the plasma levels of insulin, insulin resistance and leptin but decreased the levels of adiponectin, BMC and BMD. Increased expression of PPAR-γ, FAS, Fab-4, UCP-2, SREBP-1c, ACC, and TNF-α was noticed in HFD-fed rats. However, supplementation of piperonal (20, 30 and 40 mg/kg b.wt) for 42 days considerably and dose-dependently attenuated the HFD-induced alterations, with the maximum therapeutic activity being noticed at 40 mg/kg b.wt. Conclusions: Piperonal significantly attenuated HFD-induced body weight and biochemical changes through modulation of key lipid metabolizing and obesogenic genes. Our findings demonstrate the efficacy of piperonal as a potent antiobesity agent, provide scientific evidence for its traditional use and suggest the possible mechanism of action.

Phytocompounds as Potential Agents to Treat Obesity-Cardiovascular Ailments.

Obesity is no longer considered as a cosmetic issue as it is a potential risk factor to develop hypertension, type-2 diabetes, cardio vascular diseases (CVDs), infertility, arthritis etc. Apart from genetic factors, changes in life styles, food and work habits have lead to alarming raise in obesity ailments in both developed and developing countries. The excess and unutilized food takenin is converted into lipid components, primarily triglycerides and is stored in the liver, adipose and other tissues; if the positive energy balance extends a longer period it will lead to overweight, obesity and CVDs. Cardiovascular diseases are a group of disorders of the heart and blood vessels and cause greater mortality rate worldwide. Although a number of drugs have been developed to contain these diseases, most of them suffer from significant side effects and some of them have been even withdrawn from markets. In view of this, there is a growing emphasis for natural product based drugs. In this book chapter, the present scenario of obesity-CVDs and their causative factors are described besides mentioning currently available medications to treat them. The role of phytochemicals in treating obesity-CVDs and their possible mode of action is also highlighted. This study strengthens our understanding on obesity-CVDs and paves the way to develop novel and cost-effective plant based drugs/formulations with minimum side effects to treat these lifestyle based diseases.

Ethanolic Fraction of Terminalia tomentosa Attenuates Biochemical and Physiological Derangements in Diet Induced Obese Rat Model by Regulating Key Lipid Metabolizing Enzymes and Adipokines.

The prevalence of overweight-obesity and associated comorbidities have reached alarming levels necessitating the need to explore effective therapeutics. In the present work, we demonstrated the promising antiobesity activity of ethanolic fraction of Terminalia tomentosa bark (EFTT) in diet induced obese rat model. High Fat Diet (HFD)-fed obese rats were orally administered with EFTT (50, 100 and 200 mg/kg body weight). Changes in body weight, body composition, bone mineral concentration, bone mineral density, plasma glucose, insulin, leptin, adiponectin, circulatory and tissue lipid profiles, and the activities of liver antioxidant enzymes, key lipid metabolic enzymes and mRNA expressions of fatty acid synthase (FAS), peroxisome proliferator-activated receptor gamma (PPAR-γ), leptin and tumor necrosis factor alpha (TNF-α) were assessed in experimental rats in the presence and absence of EFTT. At a dose of 200 mg/kg b.wt, EFTT has substantially attenuated body weight and related patho-physiological alterations in HFD-induced obese rats. These findings were correlated with histological observations of adipose tissue. The therapeutic activity of EFTT could be possibly through restoration of antioxidants status, regulation of key lipid metabolizing enzymes, expression of FAS, leptin, PPAR-γ and by synchronized control of energy metabolism in liver and adipose tissue.