Chemopreventive effects of Melastoma malabathricum L. extract in mammary tumor model via inhibition of oxidative stress and inflammatory cytokines.

The objective of this study was to evaluate the anticancer effects of Melstoma malabathricum L. (MM) MDA-MB-231 human breast cancer and in vivo mammary tumor model and decipher the potential mechanism. The phyto-constituents in the extract have been identified by liquid chromatography-mass spectrometry (LC-MS). The anti-cancer activity of MM extract was tested on MDA-MB-231 human breast cancer cells. Chemical carcinogen 7,12-dimethylbenz(a)anthracene (DMBA) was used for the induction of breast cancer in rodents. Burden, volume, tumor incidence, pro-inflammatory cytokines, antioxidant parameters and mitochondrial parameters were estimated. Histological analysis was determined in mammary gland, vagina, uterus, heart, liver, lung and renal tissues. LC-MS showed the 21 phyto-constituents present in the extract of MM. MM extract showed the potent cytotoxicity against MDA-MB-231 cells and exhibited the IC50 value (14.6 µM). MM extract significantly decreased the body weight and altered the organ weight such as ovary, uterus, liver, spleen, lungs, renal, adrenal and brain tissue. MM extract significantly down-regulated the tumor incidence, tumor burden and average tumor weight at dose dependently manner. MM extract significantly altered the antioxidants activity in term of augmented the level of superoxide dismutase (SOD), catalase (CAT) and suppressed the level of malonaldehyde (MDA); pro-inflammatory cytokines levels such as reduced the level of tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß), interleukin-6 (IL-6) in the serum, hepatic and mammary gland tissue in DMBA induced mammary gland tumor rats. MM extract significantly (P < 0.001) enhanced the activity of mitochondrial parameters include Isocitrate dehydrogenase (ICDH), succinate dehydrogenase (SDH), Malate dehydrogenase (MDH) and alpha-keto glutaraldehyde dehydrogenase (α-KGDH). The histopathological finding exhibited that MM extract has a marked reduced effect on mammary glands, mammary gland, vagina, uterus, heart, liver, lung and renal.These data provide the scientific evidence that MM extract might be used as a traditional medicine to cure the breast cancer.

A cross-talk between gut microbiome, salt and hypertension.

Cardiac disorders contribute to one of the major causes of fatality across the world. Hypertensive patients, even well maintained on drugs, possess a high risk to cardiovascular diseases. It is, therefore, highly important to identify different factors and pathways that lead to risk and progression of cardiovascular disorders. Several animals and human studies suggest that taxonomical alterations in the gut are involved in the cardiovascular physiology. In this article, with the help of various experimental evidences, we suggest that the host gut-microbiota plays an important in this pathway. Short chain fatty acids (SCFAs) and Trimethyl Amine -n-Oxide (TMAO) are the two major products of gut microbiome. SCFAs present a crucial role in regulating the blood pressure, while TMAO is involved in pathogenesis of atherosclerosis and other coronary artery diseases, including hypertension. We prove that there exists a triangular bridge connecting the gap between dietary salt, hypertension and gut microbiome. We also present some of the dietary interventions which can regulate and control microbiota that can prevent cardiovascular complications.We strongly believe that this article would improve the understanding the role of gut microbiota in hypertension, and will be helpful in the development of novel therapeutic strategies for prevention of hypertension through restoring gut microbiome homeostasis in the near future.

Prunus amygdalus extract exert antidiabetic effect via inhibition of DPP-IV: in-silico and in-vivo approaches.

Prunus amygdalus (PA) is a popular invasive seed utilized in the management of diabetes in Jammu and Kashmir, India. The objective of the current study was to scrutinize the antidiabetic effect of Prunus amygdalus (PA) against Streptozotocin (STZ) induced diabetic rats and explore the possible mechanism of action at cellular and sub-cellular levels. Box Benkan Design (BBD) was performed to determine the effect of PA powder to methanol, extraction time and extraction temperature on DPPH and ABTS free radical scavenging activity of decoction. In-silico study was performed on GLUT1 (5EQG) and dipeptidyl peptidase IV (DPPIV) (2G63) protein. Type II diabetes mellitus was initiated by single intra-peritoneal injection of STZ. The Blood Glucose Level (BGL) and body weight were estimated at regular interval of time. The different biochemical parameters such as hepatic, antioxidant, and lipid parameters were estimated. At end of the study, pancreas was used for histopathological observation. The variation in DPPH antiradical scavenging activity 40.0-90.0% and ABTS antiradical scavenging activity 34-82%, were estimated respectively. STZ induced DM rats showed increased BGL at end of the experimental study. PA treatment significantly (p < 0.001) down-regulated the BGL level. PA significantly (p < 0.001) altered the biochemical, hepatic and antioxidant parameters in a dose-dependent manner. Histopathological examination demonstrated the constructive mass of ß-cells in pancreas. Overall, the current study indicates that the PA treatment down-regulated the hyperglycemic, oxidative stress and hyperlipidaemia in diabetic rats, due to inhibition of enzymes or amelioration of oxidative stress. [Formula: see text] Communicated by Ramaswamy H. Sarma.

Amelioration of neurodegeneration and cognitive impairment by Lemon oil in experimental model of Stressed mice.

Citrous lemon (Rutaceae) an Indian folk medicine has been used for the treatment of various pathological diseases viz., diabetes, cardiovascular, inflammation, hepatobiliary dysfunction and neurodegenerative disorder. Can lemon oil altered the memory of unstressed and stressed mice, a basic question for which the present work was put on trial. The present investigation was intended to assess the impact of Lemon oil on memory of unstressed and Stressed Swiss young Albino mice. Lemon oil (50 and 100 mg/kg o.r.) and donepezil (10 mg/kg) were guided for three weeks to different groups of stressed and unstressed mice. The nootropic movement was assessed utilizing elevated plus maze and Hebbs Williams Maze. Cerebrum acetylcholinesterase (AChE), plasmacorticosterone, decreased glutathione, lipid per oxidation alongside superoxide dismutase and catalase was surveyed as marker for disease. Histopathology was performed for estimation of drug effects. Acute immobilized stress was induce, lemon oil (100 mg/kg) and donepezil together indicated memory enhancing movement both in stressed and unstressed mice. Lemon oil significantly (p < 0.001) altered and lowered brain AChE activity both in stressed and unstressed mice. Scopolamine induced amnesia was also significantly altered and reversed both in stressed and unstressed mice by lemon oil at a dose of 50 and 100 mg/kg. Lemon oil (50 and 100 mg/kg) was further able to control the corticosterone level in plasma for stressed mice. Lemon oil significantly (p < 0.001) elevated the level of catalase, superoxide dismutase and reduced glutathione levels both in stressed and unstressed animals with respect to controlled group along with TBARS both in stressed and unstressed compared with control group. Hence it can be concluded that memory enhancing activity might be related to reduction in AChE and TBARS activity and by elevated GSH, SOD and catalase through decrease in raised plasma corticosterone levels.

Protective effect of oleane-12-en-3ß-ol-28-oic acid 3ß-D-glucopyranoside in ethanol induced gastric ulcer by enhancing the prostaglandin E2 level.

ETHNOPHARMACOLOGICAL RELEVANCE: Lantana camara is a popular invasive weed utilized in the management of ulcer in different part of world. Study of specific compound present in this plant responsible for their antulcer activity is main topic of concern. Current study designed for evaluation of the antiulcer activity of oleane-12-en-3ß-ol-28-oic acid 3ß-D-glucopyranoside (OAG) from Lantana camara L. MATERIALS AND METHODS: Antiulcer activity was carried out on NSAID's (Aspirin) and ethanol induced ulcer model. The efficacy of the OAG on ulcer index, percentage protection and gastric acid secretion were evaluated. RESULTS: Ulcer protection percentage (38.37%) was significant (P < 0.001) higher in the groups treated with the higher OAG dose (50mg/kg), it also recover the mucosa with no redness, no inflammation, mild dilation of blood vessels. OAG significantly (P < 0.01 and P < 0.001) reduce acidity, free acidity and gastric acid volume. It also significantly (P < 0.01) increases the pH of stomach. CONCLUSION: On the basis of results, it can be concluded that OAG shows significant gastroprotective activity by gastric acid secretion inhibition and afford protection against gastric mucosal damage. Further increase of prostaglandin E2 level establishes the mechanism of antiulcer activity of OAG.

Preclinical renal chemo-protective potential of Prunus amygdalus Batsch seed coat via alteration of multiple molecular pathways.

Prunus amygdalus Batsch (almond) is a classical nutritive traditional Indian medicine. Along with nutritive with anti-oxidant properties, it is, clinically, used in the treatment of various diseases with underlying anti-oxidant mechanism. This study is an effort to scrutinise the renal protective effect of P. amygdalus Batsch or green almond (GA) seed coat extract and its underlying mechanism in animal model of Ferric nitrilotriacetate (Fe-NTA) induced renal cell carcinoma (RCC). RCC was induced in Swiss Albino Wistar rats by intraperitoneal injection of Fe-NTA. The rats were then treated with ethanolic extract of GA (25, 50 and 100 mg/kg per oral) for 22 weeks. Efficacy of GA administration was evaluated by change in biochemical, renal, macroscopical and histopathological parameters and alterations. Additionally, interleukin-6 (IL-6), tumour necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) and inflammatory mediator including prostaglandin E2 (PGE2), nuclear factor-kappa B (NF-κB) were also observed to explore the possible mechanisms. The oral administration of GA significantly (p < .001) altered the Fe-NTA induced RCC in rats by inhibition of renal nodules, decolourisation of tissues, tumour promoter marker including thymidine 3[H] incorporation, ornithine decarboxylase, renal parameters and anti-oxidant parameters in serum. Additionally, GA treatment significantly (p < .001) down-regulated the IL-6, IL-1ß, TNF-α, inflammatory mediators PGE2 and NF-κB in a dose-dependent manner. Histopathology observation supported the renal protective effect of GA by alteration in necrosis, size of Bowman capsules and inflammatory cells. Hence, it can be concluded that GA possesses observable chemo-protective action and effect on Fe-NTA induced RCC via dual inhibition mechanism one by inhibiting free radical generation and second by inhibiting inflammation.

Evaluation of diphenhydramine in talc induced type 2 diabetes mellitus in Wistar rats.

Evaluation of diphenhydramine in talc induced type 2 diabetes mellitus was done in Wistar rats. Oral administration of Talc (10mg/kg)carried out for 21days increased the levels of serum glutamate pyruvate transaminase (SGPT), glutamate oxaloacetate transaminase (SGOT), serum creatinine, blood glucose, urea, uric acid and triglycerides (TGs), but when the animals were treated with diphenhydramine (DPH), the levels of the aforementioned biochemical parameters decreased significantly (p<0.0001). The level of serum cholesterol and high density lipoprotein (HDL) was found to be reduced in Diabetes Mellitus (DM) control and when it was treated with DPH control animals, these makers increased significantly. The study done on DM and Diphenhydramine suggests that Talc increases the blood glucose level at a dose of 10mg/kg (0.14gm) and Diphenhydramine (1mg/kg)reduces the increased blood glucose level. These finding simply that diphenhydramine may be useful in the management of talc induced diabetes.

Triterpenoids principle of Wedelia calendulacea attenuated diethynitrosamine-induced hepatocellular carcinoma via down-regulating oxidative stress, inflammation and pathology via NF-kB pathway.

The aerial part of Wedelia calendulacea have been used in Ayurveda, Unani, Tibetan, Siddha and other folk medicine systems to protect the liver and renal tissue. Liver is considered as primary metabolizing site of body, which is prone to damage by endogenous and exogenous toxicants. A reason for liver toxicity, and major causes of the hepatocellular carcinoma (HCC). 19-α-Hydroxyurs-12(13)-ene-28 oic acid-3-O-ß-D-glucopyranoside (HEG), a triterpenoids found in the higher plants, has been known to possess protective effect against various toxicants. The aim of the current study was to scrutinize the hepatoprotective mechanism of HEG against DEN-induced oxidative stress, hyperproliferation, inflammation and apoptosis tissue injury in Wistar rats. Invitro cell lines study of HEG scrutinized against the Hep-G2 and HuH-7 cells. A single dose of DEN (200 mg/kg) and double dose of phenobarbitol were administered to induce the liver damage in rats; the dose treatment of HEG was terminated at the end of 22 weeks. Macroscopical study was performed for the confirmation of hepatic nodules. The serum and hepatic samples were collected for further biochemical and histopathological analysis. Hepatic; non-hepatic; Phase I and II antioxidant enzymes were also examined. Additionally, we also scrutinized the inflammatory cytokines viz., tumor necrosis factor-α, interlukin-6, interlukin-1ß, and Nuclear factor kappa beta (NF-kB), respectively. Histopathological study was also performed for analyzing the changes during the HCC. HEG confirmed the reduction of growth and deoxyribonucleic acid synthesis of both cell lines. DEN successfully induced the HCC in all group, which was significantly (p < 0.001) altered by the HEG in a dose-dependent manner. The decreased level of pro-inflammatory cytokines and altered membrane-bound enzyme activity were also observed. HEG inhibits the phase I, II and antioxidant enzymes at the effective dose-dependent manner, which were considered as the precursor of the HCC. The alteration of phase I, II and antioxidant enzymes confirmed the inhibition of inflammatory reaction and oxidative stress, which directly or indirectly inhibited the NF-kB expression. Collectively, we can conclude that the HEG inhibited the growth of Hepatocellular carcinoma via attenuating the NF-kB pathway.

Novel glycoside from Wedelia calendulacea inhibits diethyl nitrosamine-induced renal cancer via downregulating the COX-2 and PEG2 through nuclear factor-κB pathway.

A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-ß-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. The histopathological changes were observed in the HEG pre-treated group, which was proof for its safety concern as far as its toxicity is concerned. The isolated compound HEG can impart momentous chemo-protection against experimental RCC by suppressing the cyclooxygenase (COX-2) and prostaglandin E2 (PGE2) expression via nuclear factor-kappa B (NF-κB) pathway.

Phytoconstituents as pharmacotherapeutics in rheumatoid arthritis: challenges and scope of nano/submicromedicine in its effective delivery.

OBJECTIVES: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed. KEY FINDINGS: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kß, lipoxygenase (LOXs) and arachidonic acid (AA). Despite the presence of significant merits, the use of these bioactives has several demerits such as poor bioavailability as a function of low aqueous solubility and higher first-pass metabolism upon oral administration. The impact of nano/submicromedicine in the delivery of these bioactives against RA has gained wider attention owing to bioavailability enhancement, higher stability and better efficacy. CONCLUSION: Phytoconstituents possess immense potential in RA pharmacotherapy, but the obstacles for their effective delivery can be overcome using nano/submicrocarrier-based drug delivery technologies, which maximize the efficacy of these herbal antirheumatic drugs without any systemic adverse effects.

Melastoma malabathricum Linn attenuates complete freund's adjuvant-induced chronic inflammation in Wistar rats via inflammation response.

BACKGROUND: Natural products use for arthritis treatment is gaining importance in the medical worldt. Various studies reports medical importance of Melastoma malabathricum Linn. (MM) (Melastomataceae), also known as "putki," has a broad range of health benefits, for its free radical scavenging constituents. The current investigation scrutinizes the antioxidant and anti-inflammatory effect of MM against adjuvant-induced arthritis in experimental rats. METHODS: High-performance thin layer chromatography (HPTLC) was used for estimation of phytochemical-constituents present in the MM extract. Protective effect of MM extract in Wistar rats was estimated using CFA-induced model. The rats were divided into different groups with six rats in each group. All animals received oral administration of MM and indomethacin for 28 days. The body weight and arthritic score were scrutinized at regular intervals. At the end of experimental protocol, the rats were sacrificed, and blood samples were used for antioxidant, hematological parameters, pro-inflammatory and inflammatory mediator, respectively. Histopathological observation was used to evaluate the protective effect of MM extract. RESULT & DISCUSSION: Current study confirmed the preventive effect of MM against adjuvant-induced paw edema, paw redness and arthritic progression. MM significantly (P < 0.001) modulated the oxidative stress parameters as well as hematological parameter induced by CFA. The result also altered the distorted level of proinflammatory mediators and inflammatory mediator, which further reinforce the implication of MM in CFA induced arthritis. Histological analyses of joints of rats showed a reduction in the synovial hyperplasia and mononuclear infiltration in the MM treated group which provides evidence for the antiarthritic effect of MM. CONCLUSION: From above parameters our study states that the MM is capable of restraining the alteration produced via adjuvant-induced arthritis in aminals. The repressing effect of MM could be attributed, at least in part, to antioxidant, hematological and anti-inflammatory effect. Figure Caption: Melastoma Malabathricum Linn Attenuates Complete Freund's Adjuvant-Induced Chronic Inflammation in Wistar rats by Inflammation Response.

Inhibition on the growth of human MDA-MB-231 breast cancer cells in vitro and tumor growth in a mouse xenograft model by Se-containing polysaccharides from Pyracantha fortuneana.

Breast cancer is the second cause of cancer-related death among Women. Current therapies for breast cancer have adverse side-effects. Selenium (Se)-containing polysaccharides have multiple health benefits to humans. Pyracantha fortuneana (P. fortuneana) contains rich Se polysaccharides. We hypothesized that Se-containing polysaccharides from P. fortuneana possess anticancer activity on breast cancer via inhibiting growth and inducing apoptosis. This study aimed to assess the anticancer effect of Se-containing polysaccharides from P. fortuneana and the underlying mechanisms. Se-containing polysaccharides were purified. Their properties and monosaccharide compositions were analyzed. Their effects on cell growth, expression of cycle proteins, apoptosis and apoptosis-related protein, and tumor growth in mouse xenograft model were examined. This extract contained 93.7% (w/w) of carbohydrate, 2.1% (w/w) of uronic acid and 3.7µg/g of Se, and was considered as Se-conjugated polysaccharides (Se-PFPs). In vitro studies showed that treatment of triple negative breast cancer (TNBC) MDA-MB-231 cells with Se-PFPs (1) inhibited cell growth dose-dependently by arresting cells at G2 phase via inhibiting CDC25C-CyclinB1/CDC2 pathway; (2) caused apoptosis associated with increased p53, Bax, Puma and Noxa, decreased Bcl2, increased Bax/Bcl2 ratio and increased activities of caspases 3/9, suggesting its effect on p53-mediated cytochrome c-caspase pathway. Treatment of nude mice bearing MDA-MB-231-derived xenograft tumors with Se-PFPs significantly reduced tumor growth without altering body weight, confirming its antitumor activity without toxic side effects. Se-PFPs enhanced doxorubicin cytotoxic effects. It is concluded that Se-containing polysaccharides from P. fortuneana potently inhibit the growth and induce apoptosis of TNBC cells and can be potential anticancer agent for TNBC.

Chemomodulatory effect Melastoma Malabathricum Linn against chemically induced renal carcinogenesis rats via attenuation of inflammation, oxidative stress, and early markers of tumor expansion.

Melastoma malabathricum Linn (MM) has high valued for its commercial significance. Indian market (northeast) has great demand for the plants, which extended, its use as a traditional home remedy due to its anti-inflammatory effects. In this study, we scrutinize the therapeutic and protective effect of MM against diethylnitrosamine (DEN) and ferric nitrilotriacetate (Fe-NTA)-induced renal carcinogenesis, renal hyperproliferation, and oxidative stress in rats. Liquid chromatography mass spectroscopy (LC-MS) was used for identification of phytoconstituents. Administration of DEN confirmed the initiation the renal carcinogenesis via enhancing the expansion of tumor incidence. Intraperitoneally, administration of Fe-NTA boost the antioxidant enzymes (phase I), viz., superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR), glutathione peroxidase (GPx) and phase II, viz., quinone reductase (QR) and glutathione-S-transferase (GST). It also increased the content of renal lipid peroxidation (LPO), hydrogen peroxidase (H2O2) with decrease content in glutathione content (GSH). It also increased the renal biochemical and non-biochemical parameter. It also confirmed the augment the level of thymidine [3H] incorporation into renal DNA, ornithine decarboxylase (ODC) activity and increased the generation of proinflammatory (TNF-α, IL-6 and IL-ß) and inflammatory mediator (PGE2). We also analyzed the macroscopic and histologic of renal tissue. In addition, the effect of phytoconstituent of MM extract was evaluated in silico and free radical scavenging activity against the DPPH and ABTS free radicals. LC-MS confirmed the presence of quercetin >gallic acid in MM extract. Renal carcinogenesis rats treated with MM (100, 250, and 500 mg/kg) confirmed the significantly (P < 0.001) protective effect via reduction the antioxidant (phase I and phase II) enzymes, biochemical parameter and restore the proinflammatory and inflammatory mediator at dose dependent manner. MM altered the ODC and thymidine activity in renal DNA. The chemoprotective effect of MM was confirmed via decreased the renal tumor incidence, which was confirmed by the macroscopic and histopathological observation. Consequently, our result suggests that MM is a potent chemoprotective agent and suppresses DEN+ Fe-NTA-induced renal carcinogenesis, inflammatory reaction, and oxidative stress injury in Wister rats.

Paederia foetida Linn. inhibits adjuvant induced arthritis by suppression of PGE(2) and COX-2 expression via nuclear factor-κB.

The current investigation was undertaken to determine the anti-inflammatory and antioxidant effects of Paederia foetida Linn. (PF) along with its mechanism of action when implemented in tissue protection. HPTLC was used in the identification of the compound quercetin, while in vitro analysis confirmed the significance of the antioxidant and anti-inflammatory action of PF. We initially demonstrated the in vivo anti-inflammatory effect of PF, evaluating it against a variety of phlogistic agents as well as turpentine oil, prostaglandin and arachidonic acid. Groups of rats, fasted overnight, were treated as follows: Group I: normal control (vehicle), Group II: PF (100 mg kg(-1)), Group III: arthritic control (CFA only, 0.05 ml), Group IV, V, VI: CFA (0.05 ml) + PF (25, 50 and 100 mg kg(-1)) and Group VII: CFA (0.05 ml) + indomethacin (10 mg per kg b.w.). PF significantly protected against paw edema, arthritic index and body weight alteration induced by Complete Fruend's Adjuvant (CFA). Other observations, like histological and macroscopic changes, were observed in CFA induced inflammation in knee joints. Subcutaneous administration of CFA was accompanied by proinflammatory cytokine status, as appraised by the amplification of interleukin-2 (IL-2), interleukin-1ß (IL-1ß) and tumor necrosis factor (TNF-α); oxidative stress status was estimated by the enhancement of the level of lipid peroxidation (LPO) and the depletion of superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione (GSH). Pre-treatment with PF significantly (P < 0.001) protected against CFA induced oxidative stress and proinflammatory cytokines. More prominently, CFA administration augmented tissue and plasma superoxide (O2) and hydrogen peroxide (H2O2) levels, while the PF pre-treatment significantly (P < 0.001) reversed all CFA induced intracellular interruption. Following CFA induced arthritis, PF was tested for its free radical scavenging activity against the DPPH and ABTS radicals and its inhibitory proficiency against COX-1 and COX-2 in vitro. Considering the above, the current research confirmed momentous protection against CFA induced arthritis, which could be attributed to its anti-inflammatory and pro-oxidant nature.

Dual inhibition of arachidonic acid pathway by mulberry leaf extract.

The present work investigates the anti-inflammatory, analgesic and antipyretic activity of methanolic extract of mulberry leaves of variety S-1, S-13 and S-146. The S-146 extract was further evaluated for its efficacy against adjuvant arthritis in albino rats followed by inhibitory potential for COX 1, COX 2 and 5 LOX. The HPLC analysis enumerated the presence of morin, reversterol, scopoletin and 7-hydroxy coumarin as the major constituents. The anti-inflammatory, antipyretic and analgesic activity observed in the present experiment could be accredited to the dual inhibition in the AA pathway. The inhibition of COX and LOX enzymes could be imparted to the presence of resveraterol, morin, scopoletin and 7-hydroxy coumarin.

Antidiabetic potential of triterpenoid saponin isolated from Primula denticulate.

CONTEXT: Primula denticulate Sm. (Primulaceae), commonly known as drumstick primula, is traditionally used to treat diabetes and urinary disorders. In the present study, a new triterpenoid saponin was isolated. Triterpenoids generally show antidiabetic activity. Considering its traditional use and chemical nature of the molecule, the present study was designed to evaluate the antidiabetic activity. OBJECTIVE: Antidiabetic activity of triterpenoid saponin (TTS) isolated from P. denticulate. MATERIALS AND METHODS: A new TTS was isolated from the leaf of P. denticulate by column chromatography on CHCl3/MeOH (8.5:1.5) fraction. It was further characterized by using NMR, UV, and IR spectroscopic methods. Ethanol and aqueous extracts of the leaf were also prepared. Antidiabetic study for TTS, ethanol extract, and aqueous extract was carried out in streptozotocin (STZ)-induced diabetic rats at doses of 200, 1000, and 1000 mg/kg body weight, respectively. A toxicity study was also performed. RESULTS: Isolated new TTS molecule was characterized as 3-O[ß-d-xylopyranosyl-(1 → 2)-ß-d-glucopyranosyl-(1 → 4)-α-l-arabinopyranosyloxy]-16α-hydroxy-13ß,28-epoxy-olean-30-al by NMR, UV, and IR spectroscopic methods. This new TTS was found to be effective in lowering blood-glucose level in the experimental rat model, thus establishing its antidiabetic property (168.8 ± 4.58) when compared with disease control (258.8 ± 0.60). Its LD50 value was found at a dose of 2000 mg/kg. The level of insulin was restored by TTS and ethanol extract up to 31.49 µU/ml and 38.90 µU/ml, respectively, when compared with disease control (18.45 µU/ml). DISCUSSION AND CONCLUSION: In conclusion, 3-O[ß-d-xylopyranosyl-(1 → 2)-ß-d-glucopyranosyl-(1 → 4)-α-l-arabinopyranosyloxy]-16α-hydroxy-3ß,28-epoxy-olean-30-al possesses potential glucose lowering properties, i.e., antidiabetic potential against STZ-induced diabetic rats.

Paederia foetida Linn. leaf extract: an antihyperlipidemic, antihyperglycaemic and antioxidant activity.

BACKGROUND: The primary objective of the present investigation is to evaluate the antidiabetic, antihyperlidemic and antioxidant activity of the methanolic extract of the Paederia foetida Linn. (PF) leaf extract in the streptozotocin induced diabetic rats. METHODS: Single intraperitoneal injection (IP) of streptozotocin (60 mg/kg body weight) was used for induction of diabetes is swiss albino (wistar strain) rats. The induction of diabetes was confirmed after 3 days as noticing the increase in blood sugar level of tested rats. PF at a once a daily dose of 100 mg/kg, 250 mg/kg, 500 mg/kg, p.o. along with glibenclamide 10 mg/kg, p.o. was also given for 28 days. On the 28th day rats from all the groups fasted overnight fasted and the blood was collected from the puncturing the retro orbit of the eye under mild anesthetic condition. There collected blood sample was used to determine the antihyperlipidemic, hypoglycemic and antioxidant parameters. RESULTS: The oral acute toxicity studies did not show any toxic effect till the dose at 2000 mg/kg. While oral glucose tolerance test showed better glucose tolerance in tested rats. The statistical data indicated that the different dose of the PF significantly increased the body weight, hexokinase, plasma insulin, high density lipoprotein cholesterol, superoxide dismutase, catalase and glutathione peroxides. It also decreases the level of fasting blood glucose, total cholesterol, triglycerides, low density lipoprotein cholesterol, very low density lipoprotein cholesterol, malonaldehyde, glucose-6-phosphate, fructose-1-6-biphosphate and glycated hemoglobin in STZ induced diabetic rats. The histopathology of STZ induce diabetic rats, as expected the test dose of PF extract considerably modulates the pathological condition of various vital organ viz. heart, kidney, liver, pancreas as shown in the histopathology examinations. CONCLUSIONS: Our investigation has clearly indicated that the leaf extract of Paederia foetida Linn. showed remarkable antihyperglycemic activity due to its possible systematic effect involving in the pancreatic and extra pancreatic mechanism. Forever, the antihyperlipidemic activity was exerted possible by lowering the higher level of lipid profile and decreasing the intercalated disc space in the heart. The antioxidant activity of extract was due to inhibition of lipid peroxidation and increasing the SOD, GPx and CAT. It was corroborate that the extract shown the Paederia foetida Linn leaves potential to be act as antidiabetic, antihyperlipidemic and antioxidant properties.

Antineoplastic potential of Bryophyllum pinnatum lam. on chemically induced hepatocarcinogenesis in rats.

BACKGROUND: Bryophyllum pinnatum Lam. used in folk medicine in tropical Africa, tropical America, India, China and Australia contains a wide range of active compounds, well known for their haemostatic and wound-healing properties. OBJECTIVE: The present study was designed to evaluate the effect of Bryophyllum pinnatum Lam. on N-diethylnitrosamine (DENA)-induced hepatic injury in rats. MATERIAL AND METHODS: The aerial part of B. pinnatum aqueous and ethanolic extract was prepared in doses of 250 mg/kg and 500 mg/kg. Hepatic injury was induced by DENA. Acute toxicity was also carried out. RESULT: Treatment with different doses of ethanolic extract of B. Pinnatum (250 mg/kg, p.o.) was not significantly able to treat the liver injury induced by DENA, but 500 mg/kg dose of ethanolic extract of B. Pinnatum protects the liver slightly. Treatment with different doses of aqueous extract of B. Pinnatum (250 and 500 mg/kg, p.o.) significantly (P*<0.05; P**<0.01 and P***<0.001) treated the liver injury induced by DENA. CONCLUSION: It may be inferred from the present study that the hepatoprotective activities of the aqueous extract of B. Pinnatum leaves in DENA-induced hepatotoxicity may involve its antioxidant or oxidative free radical scavenging activities by alleviating lipid peroxidation through scavenging of free radicals, or by enhancing the activity of antioxidants.

Umbelliferone ß-D-galactopyranoside from Aegle marmelos (L.) corr. an ethnomedicinal plant with antidiabetic, antihyperlipidemic and antioxidative activity.

BACKGROUND: Aegle marmelos (L.) Corr. (Rutaceae), commonly known as bael, is used to treat fevers, abdomen pain, palpitation of the heart, urinary troubles, melancholia, anorexia, dyspepsia, diabetes and diarrhea in Indian traditional systems of medicine. The object of the present study was to evaluate the antidiabetic, antihyperlipidemic and antioxidant oxidative stress of umbelliferone ß-D-galactopyranoside (UFG) from stem bark of Aegle marmelos Correa. in STZ (streptozotocin) induced diabetic rat. METHODS: Diabetes was induced in rat by single intraperitoneal injection of STZ (60 mg/kg). The rat was divided into the following groups; I - normal control, II - diabetic control, III - UFG (10 mg/kg), IV - UFG (20 mg/kg), V - UFG (40 mg/kg), VI - Glibenclamide (10 mg/kg, p.o., once a daily dose). Diabetes was measured by change the level blood glucose, plasma insulin and the oxidative stress were assessed in the liver by estimation of the level of antioxidant markers i.e. superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT) and Malondialdehyde (MDA) and antihyperlipidemic effect was measured by estimation of total cholesterol, triglycerides, LDL (low density lipoprotein) cholesterol, HDL (high density lipoprotein) cholesterol, VLDL (very low density lipoprotein) cholesterol. However in a study, the increased body weight was observed and utilization of glucose was in the oral glucose tolerance test. RESULT: Daily oral administration of different dose of UFG for 28 days showed significantly (P < 0.001) decreased in fasting blood glucose level and improve plasma insulin level as compared to the diabetic control group. Also it significantly (P < 0.001) decreased the level of glycated hemoglobin, glucose-6-phosphatase, fructose-1-6-biphosphate and increased the level of hexokinase. UFG treatment decreased liver MDA and increased the level of SOD, GPx and CAT. UFG treatment of lipids it's increased the level of cholesterol, triglycerides, VLDL, LDL cholesterol and decreased the level of HDL cholesterol. Histologically, inflammatory cell in blood vessels, intercalated disc, fat degeneration and focal necrosis observed in diabetic rat organ but was less obvious in UFG treated groups. The mechanism of action of UFG may be due to the increased level of pancreatic insulin secretion and effect on the antioxidant marker. CONCLUSION: UFG posses an antidiabetic, antioxidant and antihyperlipidemic effect on the STZ induced diabetic rat. Hence it could be the better choice to cure the diabetes.

Anti-diabetic, anti-oxidant and anti-hyperlipidemic activities of Melastoma malabathricum Linn. leaves in streptozotocin induced diabetic rats.

BACKGROUND: Melastoma malabathricum (MM) Linn leaves traditionally use in the treatment of diabetic conditions. The aim of the present investigation was to evaluate the antioxidant, antihyperlipidemic and antidiabetic activity of methanolic extract taken from Melastoma malabathricum Linn (Melastomaceae). METHODS: The methanolic leaves extract of MM Linn leaves used for the study. Chemical test of different extract, acute toxicity study and oral glucose test was performed. Diabetes was induced in rat by single intra-peritoneal injection of streptozotocin (55 mg/kg). The rats were divided into following groups: Group I - normal control, Group II (Vehicle) - diabetic control, Group III (STZ-toxic) - MM I (100 mg/kg, p.o.), Group IV - MM II (250 mg/kg, p.o.), Group V - MM III (500 mg/kg, p.o.), Group VI - glibenclamide (10 mg/kg, p.o.). Bodyweight of each rat in the different groups was recorded daily. Biochemical and antioxidant enzyme parameters were determined on day 28. Histology of different organ (heart, liver, kidney, and pancreas) was performed after sacrificing the rats with euthanasia. RESULTS: The methanolic extract of MM did not show any acute toxicity up-to the dose of 2000 mg/kg and shown better glucose utilization in oral glucose tolerance test. Orally treatment of different doses of MM leaves extract decreased the level of serum glucose, glycated hemoglobin, glucose-6-phosphatase, fructose-1-6-biphosphate and increased the level of plasma insulin, hexokinase. MM treatment decreased liver malondialdehyde but increased the level of superoxide dismutase, catalase and glutathione peroxidase. In oral glucose tolerance test observed increased utilization of glucose. Streptozotocin induced diabetes groups rat treated with different doses of MM leaves extract and glibenclamide significantly increased the body weight. Histopathology analysis on different organ of STZ (streptozotocin) induced diabetic rat show there regenerative effect on the liver, kidney, heart and pancreas. CONCLUSION: The antioxidant, antihyperlipidemic and antidiabetic effect of methanolic extract from Melastoma malabathricum Linn suggests a potential therapeutic treatment to antidiabetic conditions.