ABSTRACT
Bitter taste perception is important in preventing animals from ingesting potentially toxic compounds. Whole-genome assembly (WGA) data have revealed that bitter taste receptor genes (TAS2Rs) comprise a multigene family with dozens of intact and disrupted genes in primates. However, publicly available WGA data are often incomplete, especially for multigene families. In this study, we employed a targeted capture (TC) approach specifically probing TAS2Rs for ten species of cercopithecid primates with diverse diets, including eight omnivorous cercopithecine species and two folivorous colobine species. We designed RNA probes for all TAS2Rs that we modeled to be intact in the common ancestor of cercopithecids ("ancestral-cercopithecid TAS2R gene set"). The TC was followed by short-read and high-depth massive-parallel sequencing. TC retrieved more intact TAS2R genes than found in WGA databases. We confirmed a large number of gene "births" at the common ancestor of cercopithecids and found that the colobine common ancestor and the cercopithecine common ancestor had contrasting trajectories: four gene "deaths" and three gene births, respectively. The number of intact TAS2R genes was markedly reduced in colobines (25-28 detected via TC and 20-26 detected via WGA analysis) as compared with cercopithecines (27-36 via TC and 19-30 via WGA). Birth or death events occurred at almost every phylogenetic-tree branch, making the composition of intact genes variable among species. These results show that evolutionary change in intact TAS2R genes is a complex process, refute a simple general prediction that herbivory favors more TAS2R genes, and have implications for understanding dietary adaptations and the evolution of detoxification abilities.
Subject(s)
Colobinae , Receptors, G-Protein-Coupled , Animals , Receptors, G-Protein-Coupled/genetics , Colobinae/genetics , Diet/veterinary , Multigene Family , Phylogeny , Cercopithecidae/genetics , Evolution, Molecular , TasteABSTRACT
This research study mainly focused on the dynamic malware detection. Malware progressively changes, leading to the use of dynamic malware detection techniques in this research study. Each day brings a new influx of malicious software programmes that pose a threat to online safety by exploiting vulnerabilities in the Internet. The proliferation of harmful software has rendered manual heuristic examination of malware analysis ineffective. Automatic behaviour-based malware detection using machine learning algorithms is thus considered a game-changing innovation. Threats are automatically evaluated based on their behaviours in a simulated environment, and reports are created. These records are converted into sparse vector models for use in further machine learning efforts. Classifiers used to synthesise the results of this study included kNN, DT, RF, AdaBoost, SGD, extra trees and the Gaussian NB classifier. After reviewing the test and experimental data for all five classifiers, we found that the RF, SGD, extra trees and Gaussian NB Classifier all achieved a 100% accuracy in the test, as well as a perfect precision (1.00), a good recall (1.00), and a good f1-score (1.00). Therefore, it is reasonable to assume that the proof-of-concept employing autonomous behaviour-based malware analysis and machine learning methodologies might identify malware effectively and rapidly.
Subject(s)
Algorithms , Computer Security , Machine Learning , SoftwareABSTRACT
The lack of safety and efficacy of existing hepatoprotective agents urge the need to explore novel hepatoprotective agents. The research work was planned to study the therapeutic potential of some newly synthesized chalcones against 4-acetaminophenol induced hepatotoxicity in rats. Male albino rats (N = 30) were divided into 6 groups of 5 animals each i.e. group I; Toxic control (4-acetaminophenol), group II; normal control (Normal saline), group III; Positive control (silymarin; 50 mg/kg bw) and groups IV-VI (test groups) treated with 3 chalcone analogues i-e 3a, 3f & 3 g (100, 150, 150 mg/kg bw, respectively). All the study group animals were administered with 4-acetaminophenol to induce hepatotoxicity except normal control. Following hepatotoxicity induction, test group animals were administered with selected doses of test compounds and toxic group animals left untreated. Liver enzymes including ALT, AST, ALP and serum bilirubin were determined photometrically. Antioxidant activities of test compounds were also determined. Histopathological examination of liver biopsies was also carried out through H & E staining. The test chalcones (3a, 3f & 3 g) significantly decreased the levels of liver enzymes and serum bilirubin toward normal and the pattern of results in the test group animals were comparable to silymarin administered animals indicating the hepatoprotective potential of test compounds. Moreover, the test chalcones (3a, 3f & 3 g) antagonized the effect of 4-acetaminophenol and thus, raised the catalase (CAT) and superoxide dismutase (SOD) while decreased the malondialdehyde (MDA) in experimental animals. The test chalcones (3a, 3f & 3 g) on histological examination of liver showed improvement of tissue morphology. The study concluded that the tested compounds have antioxidant potential and may act as hepatoprotective agent. However, in-depth studies are required to validate their safety and to elucidate the exact mechanism of action.
ABSTRACT
BACKGROUND: In recent years, 1, 2, 4-triazole and its derivatives have been reported to be pharmacologically significant scaffolds. They possess analgesic, anti-tubercular, anti-inflammatory, anti-convulsant, anti-oxidant, anti-fungal, anti-cancer, anxiolytic and anti-depressant activity. This study was designed and conducted to evaluate the potential anti-inflammatory, analgesic and antipyretic activities of Triazole derivatives. METHODS: Swiss albino (male and female) mice weighing 20-30 g (10-24 weeks female), (5-14 weeks male) and Wister Kyoto rats (male and female) weighing 200-300 g (8-10 weeks old) were used for the present study. Anti-inflammatory activity was checked using Lambda carrageenan (λ) and egg albumin-induced paw edema models. Analgesic via Writhing Reflex induced by acetic acid and formalin, furthermore anti-pyretic activity was assessed by yeast induced pyrexia. RESULTS: Both of the test compounds exhibited encouraging anti-inflammatory analgesic and antipyretic results when compared with standard drug ibuprofen. The maximum inhibition of edema for the compound (S)-1-(4-Amino-5-mercapto-4H-1,2,4-triazole-3-yl) ethanol [3] was found to be (91)% as compared to reference drug ibuprofen (82)%, while (S)-1-(6-Phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)ethanol [5e] showed equipotent results to ibuprofen (81)%. The derivatives were also screened for their anti-nociceptive activity by Acetic acid writhing and tail immersion test. Compound 3 showed a significant reduction in wriths (83)% as compared to standard drug ibuprofen 71.5% and [5] showed comparable results to ibuprofen by exhibiting 70% reduction in writh at the same dose as that of standard drug, moreover, there were no signs of toxicity being observed after administration of high doses of test compounds to mice. CONCLUSIONS: It is evident from the results that compounds 3(compound A) and 5(compound B) are a potential candidate for anti-inflammatory, analgesic and anti-pyretic and the scaffold could be used for further structural modifications. Further studies would help to evaluate their molecular mechanism of action regarding these beneficial activities.
Subject(s)
Analgesics/pharmacology , Anti-Inflammatory Agents/pharmacology , Antipyretics/pharmacology , Triazoles/chemical synthesis , Triazoles/pharmacology , Animals , Female , Male , Mice , Rats , Rats, Inbred WKYABSTRACT
We report high photocatalytic hydrogen evolution from water-glycerol mixture under visible light illumination using sol-gel method synthesized zinc oxide (ZnO), Lutetium (Lu) modified ZnO and Lu modified ZnO/CNTs composite. X-ray diffraction (XRD), transmission electron microscopy (TEM), energy dispersive X-ray (EDX), Brunauer-Emmett-Teller (BET), UV-Visible diffuse reflectance spectroscopy (UV-Vis DRS), photoluminescence (PL), X-ray photoelectron spectroscopy (XPS), photocurrent transient response and electrochemical impedance spectroscopy (EIS) Nyquist studies were used to determine the reason for improved photocatalytic hydrogen evolution. The highest hydrogen evolution rate of 380 µmolh-1 was obtained for Lu modified ZnO/CNTs composite, 3.11 times the amount generated over Lu modified ZnO and 10.5 times than using pure ZnO sample. This efficient enhancement in the photocatalytic hydrogen evolution was apparently attributed to the red shift in the optical absorption, increased charge separation, high surface area, cleavage of glycerol by Lu and synergistic effect between Lu and CNTs. Moreover, the effect of Lu and CNTs loading on the photocatalytic hydrogen evolution activity of Lu modified ZnO/CNTs was also studied under analogous experimental conditions. A mechanism of photocatalytic hydrogen evolution by Lu modified ZnO/CNTs composite was also proposed. Additionally, synthesized samples showed prolonged photostability with steady hydrogen evolution in successive cycle runs. This report might attract much attention to design highly efficient and inexpensive photocatalyst for hydrogen evolution under visible light illumination.
ABSTRACT
Ziziphus oxyphylla Edgew (Z. oxyphylla) is a small shrub to a medium sized tree. The aim of the present study was to evaluate the hepatoprotective activity of Z. oxyphylla in paracetamol-induced hepatotoxic rat model. Silymarin was used as a standard drug. Methanol extract was found to be the most potent in in-vitro antioxidant studies. The methanol extract of Z. oxyphylla was administered to experimental animals. The hepatoprotective effect of extract was evaluated by measuring liver biochemical markers, anti-oxidant enzymes and blood lipid profile. Treatment with the paracetamol increased the level of hepatic biomarkers, blood lipid profile and decreased anti-oxidant enzymes. Pre-treatment with Z. oxyphylla caused restoration of hepatic biomarkers, blood lipid profile and antioxidant enzymes levels. It is concluded that the methanol extract of Z. oxyphylla possesses hepatoprotective activity that might be due to quercetin and kaempferol glycosides present in the plant extract. Further studies are required to elucidate the exact mechanism of action of these isolated flavonoid glycosides.
Subject(s)
Antioxidants/pharmacology , Chemical and Drug Induced Liver Injury/prevention & control , Liver/drug effects , Oxidative Stress/drug effects , Plant Extracts/pharmacology , Ziziphus , Acetaminophen , Animals , Antioxidants/isolation & purification , Biomarkers/blood , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/metabolism , Chemical and Drug Induced Liver Injury/pathology , Disease Models, Animal , Enzymes/blood , Lipids/blood , Liver/metabolism , Liver/pathology , Male , Methanol/chemistry , Plant Extracts/isolation & purification , Plant Leaves , Rats, Wistar , Solvents/chemistry , Ziziphus/chemistryABSTRACT
Lactucaserriola (L. serriola), commonly known asprickly lettuce, is an annual and biennial herb. The plant is traditionally used as sedative, hypnotic, cough suppressant, expectorant, purgative, diuretic, vasorelaxant, demulcent, antiseptic and antispasmodic. Aim of present study was to evaluate protective effect of L. serriola in paracetamol-induced hepatotoxicity. Silymarin was used as a standard drug. Hepatoprotective effect of extract was determined by liver biochemical markers, anti-oxidant enzymes and blood lipid profile. Methanolic extract was found to be the most potent in in-vitro antioxidant assays and used for further studies. Treatment with paracetamol increased the level of hepatic biomarkers, blood lipid profile and decreased anti-oxidant enzyme levels. Pre-treatment with Lactuca serriola caused restoration of hepatic biomarkers, blood lipid profile and antioxidant enzymes. FTIR represented that L. serriola contains hydroxyl (-OH), carboxylic acid (C=O) and alkene (C=C) groups. HPLC analysis showed presence of polyphenolic compounds in the methanolic extract of L. serriola. It is concluded that the methanolic extract of Lactuca serriola possesses hepatoprotective potential that might be linked to the presence of polyphenolic compounds and their anti-oxidant activities.
Subject(s)
Antioxidants/pharmacology , Asteraceae/chemistry , Chromatography, High Pressure Liquid/methods , Liver/drug effects , Phytochemicals/analysis , Plant Extracts/pharmacology , Spectroscopy, Fourier Transform Infrared/methods , Acetaminophen/toxicity , Animals , Lipids/blood , Liver/metabolism , Liver/pathology , Male , Oxidative Stress/drug effects , Protective Agents/pharmacology , RatsABSTRACT
BACKGROUND: Delay in seeking health care by breast cancer patients is associated with advanced stage of disease at presentation and poor survival rates. This study aimed to identify the reasons for delayed presentation and their association with various sociodemographic variables. METHODS: A total of 200 female patients with abnormal clinical findings, ie, lump or palpable mass, were consecutively invited for this study. Diagnostic delay was defined as a consultation with a health care provider more than 3 months from the appearance of the first symptoms. Sociodemographic variables, presenting symptoms, knowledge about diseases and its symptoms, time between seeking medical attention after appearance of symptoms and causes of delayed presentation were investigated. Chi-squared and logistic regression tests for significance and associations were used. RESULTS: Among 125 women with breast cancer fulfilling the inclusion criteria, aged 24-75 years, 88.8% (n=111) presented late (≥3 months) and 59% presented with advanced stage of disease (stage III/IV). The majority (65.6%) were older than 40 years of age, 99.2% were married, 60.8% had <8 years of education, 67.2% had poor social status, and 64.8% had a negative family history of any cancer type. Almost all patients (96%) complained about the presence of a painless lump in their breast. Ignorance of disease or the presence of painless lumps in the breast and low financial resources for therapy (81.1%) were the main variables associated with delayed presentation. Educational factors (P<0.001, OR 4.682) and social status (P<0.001, OR 1.8) were also associated with delayed presentation. CONCLUSION: Our study highlighted the variables associated with delayed presentation in Pakistani breast cancer patients. A significant number of patients presented late owing to misconceptions and poor knowledge about the disease and its symptoms, while illiteracy and poor social status were the major contributing factors for delayed presentation, resulting in an advanced presentation of disease and ultimately a decreased survival rate.
ABSTRACT
BACKGROUND: Zanthoxylum armatum DC (Z. armatum), belonging to Rutaceae family, has been traditionally used for the treatment of various diseases such as hypertension, abdominal pain, headache, fever, high altitude sickness, diarrhea, dysentery, and as a tonic, condiment, and an anthelmintic treatment. HYPOTHESIS: The present study aims to evaluate the vasorelaxant effect of a methanolic extract of the fruits of Z. armatum, isolate the active components and characterize the underlying mechanism. STUDY DESIGN: A methanolic extract of fruits of Z. armatum was prepared and its vasorelaxant effect was studied using porcine coronary artery rings. Thereafter, the methanolic extract was analyzed, and a major compound was isolated and its structure elucidated (tambulin). Different pharmacological tools were used to characterize the vasorelaxant effect of tambulin. RESULTS: The methanolic extract and the isolated tambulin caused similar endothelium-independent relaxations of porcine coronary artery rings with and without endothelium indicating a direct relaxing effect at the vascular smooth muscle. Tambulin did not affect the relaxation curves to the endothelium-dependent vasodilators, bradykinin and the calcium ionophore A23187 in rings with endothelium. Tambulin (1 µM) slightly but significantly shifted leftwards the concentration-relaxation curve to the endothelium-independent vasodilators, sodium nitroprusside (SNP), forskolin (FC) and isoproterenol but not those to soluble guanylyl cyclase activators (YC-1 and BAY 41-2272) and K+ channel openers (levcromakalim and 1-EBIO). Pretreatment with tambulin inhibited, in a concentration-dependent manner, contractions to KCl, serotonin (5-HT), CaCl2 and U46619 in coronary artery rings without endothelium. Both the protein kinase A (H-89, 10 µM) and the protein kinase G (Rp-8-br-cyclic GMPS, 30 µM) inhibitors significantly reduced relaxations to tambulin in coronary artery rings without endothelium. CONCLUSION: The present findings indicate that tambulin isolated from Z. armatum (fruits) is a major active principle inducing vasorelaxation through a direct effect at the vascular smooth muscle and involving both the cyclic AMP and/or cyclic GMP relaxing pathways.
Subject(s)
Benzopyrans/pharmacology , Coronary Vessels/drug effects , Cyclic AMP/metabolism , Cyclic GMP/metabolism , Vasodilator Agents/pharmacology , Zanthoxylum/chemistry , 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid/pharmacology , Animals , Benzopyrans/chemistry , Bradykinin/pharmacology , Coronary Vessels/metabolism , Coronary Vessels/physiology , Dose-Response Relationship, Drug , Endothelium, Vascular/drug effects , Endothelium, Vascular/physiology , Fruit/chemistry , Methanol/chemistry , Muscle, Smooth, Vascular/drug effects , Muscle, Smooth, Vascular/physiology , Nitroprusside/pharmacology , Organ Culture Techniques , Plant Extracts/chemistry , Plant Extracts/pharmacology , Swine , Vasodilation/drug effects , Vasodilator Agents/administration & dosage , Vasodilator Agents/chemistry , Vasodilator Agents/isolation & purificationABSTRACT
A compound herbal formulation (POL4) is used traditionally in interior parts (Distt. Badin) of Sindh, Pakistan, for the treatment of metabolic disorders like diabetes and hyperlipidemia. This study is aimed to determine the effectiveness of POL4 and its ingredients in hyperlipidemia and associated endothelial dysfunction and hypertension. POL4 is composed of equal proportion of Nigella sativa, Cichorium intybus, Trigonella foenum graecum and Gymnema sylvestre mixed in powdered form. Chronic (6 to 7 weeks) administration of POL4 and its ingredients mixed in diet caused a notable attenuation in total cholesterol, low density lipoprotein cholesterol, triglycerides, atherogenic index, C-reactive protein and glucose, while it has increased high density lipoprotein levels. POL4 intervention markedly (p<0.01) reduced systolic blood pressure in rats to 127±1.92 vs. 145.4±1.07 mm of Hg using tail-cuff method and significantly (p<0.05) improved endothelium-dependent relaxation (75±2.88 vs. 82.75±1.22%) to acetylcholine in isolated aortae of rats in treatment groups using force transducer and PowerLab system. Similar activities were assessed on the part of ingredients of POL4. These findings indicate that POL4 and its ingredients possess antihyperlipidemic, endothelium-dependent modulatory and antihypertensive activities, thus providing an evidence to the vernacular use of POL4 in hyperlipidemia and hypertension.
Subject(s)
Diet, High-Fat/adverse effects , Endothelium/drug effects , Hypolipidemic Agents/pharmacology , Plant Extracts/pharmacology , Plant Preparations/pharmacology , Animals , Antihypertensive Agents/pharmacology , Aorta/drug effects , Aorta/metabolism , Blood Pressure/drug effects , C-Reactive Protein/metabolism , Cichorium intybus/chemistry , Cholesterol, LDL/blood , Endothelium/metabolism , Female , Hyperlipidemias/drug therapy , Hyperlipidemias/metabolism , Hypertension/drug therapy , Hypertension/metabolism , Male , Nigella sativa/chemistry , Pakistan , Rats , Rats, Sprague-Dawley , Trigonella/chemistryABSTRACT
BACKGROUND: A compound herbal formulation (POL4) has been used in the indigenous system of medicine to treat cardiometabolic disorders like diabetes and associated hypertension. POL4 and most of its constituents have not been studied widely for its therapeutic use in hypertension. This study is aimed to determine the efficacy and possible insight into mechanism(s) for the medicinal use of POL4 and its ingredients in hypertension. METHODS: The aqueous methanolic extracts of POL4 (POL4.Cr) and its components [Cichorium intybus (Ci.Cr), Gymnema sylvestre (Gs.Cr), Nigella sativa (Ns.Cr) and Trigonella foenum graecum (Tfg.Cr)] were tested for blood pressure lowering activity in anaesthetized Sprague-Dawley rats. To assess the vasomodulatory effect, isolated tissue experiments were performed on rat aortic strips using isometric force transducer coupled with PowerLab data acquisition system. RESULTS: Administration of POL4 to rats caused a dose-dependent (1-100 mg/kg) fall in mean arterial pressure (MAP) with maximum effect of 85.33 ± 1.76% at 100 mg/kg, similar to the effect of verapamil. All ingredients of POL4 also decreased blood pressure with varying efficacy in following order Ns.Cr â Ci.Cr > Tfg.Cr > Gs.Cr. In rat aortic preparations, POL4 and its ingredients inhibited K+ (80 mM)-induced contractions, Ci.Cr was the most potent followed by Ns.Cr > Tfg.Cr > Gs.Cr â POL4. Against phenylephrine (P.E) contractions, Ci.Cr and Tfg.Cr exhibited complete relaxation, while POL4.Cr, Gs.Cr and Ns.Cr showed vasomodulatory effect. The Ca++ antagonist activity was confirmed when POL4 and its ingredients shifted Ca++ concentrations-response curves to the right in a manner similar to that of verapamil. On baseline of rat aorta, the parent formulation and its ingredients (except Tfg.Cr) exhibited partially phentolamine (1 µM)-sensitive vasoconstriction. CONCLUSION: These data show that POL4 and its constituents possess blood pressure lowering activity mediated through inhibition of Ca++ influx via membranous Ca++ channels and receptor (α-adrenergic) operated pathways. Thus, this study provides a rationale to the medicinal use of POL4 and its constituents in hypertension.
Subject(s)
Cardiovascular Diseases/drug therapy , Cichorium intybus , Gymnema sylvestre , Hypertension/drug therapy , Nigella sativa , Phytotherapy/methods , Plant Preparations , Trigonella , Animals , Aorta/drug effects , Blood Pressure/drug effects , Disease Models, Animal , Flavonoids/analysis , Guinea Pigs , Heart Atria/drug effects , Phenols/analysis , Plant Preparations/chemistry , Plant Preparations/pharmacology , Plant Preparations/therapeutic use , Rats , Rats, Sprague-Dawley , Vasoconstriction/drug effectsABSTRACT
The present investigation was carried out to evaluate the effect of aerial parts of Sonchus asper L. in normotensive, glucose and egg feed diet induced hypertensive rats. Aqueous-methanolic extract of Sonchus asper in 250, 500 and 1000 mg/kg doses was studied in normotensive and glucose induced hypertensive rats using the non-invasive technique. The results obtained showed that the extract has significantly (p < 0.5 - p < 0.001) decreased the blood pressure and heart rate in dose dependent manner. The dose 1000 mg/kg of the extract produced the maximum antihypertensive effect and was selected for further experiments. The extract was found to prevent the rise in blood pressure of egg and glucose fed rats as compared to control group in 21 days study. The LD50 of the plant extract was 3500 mg/kg b.w. in mice and sub-chronic toxicity study showed that there was no significant alteration in the blood chemistry of the extract treated rats. It is conceivable, therefore, that the aqueous-methanolic extract of Sonchus asper has exerted considerable antihypertensive activity in rats and has duly supported traditional medicinal use of plant in hypertension.
Subject(s)
Antihypertensive Agents/pharmacology , Blood Pressure/drug effects , Hypertension/drug therapy , Plant Extracts/pharmacology , Sonchus , Animals , Antihypertensive Agents/isolation & purification , Antihypertensive Agents/toxicity , Diet , Disease Models, Animal , Dose-Response Relationship, Drug , Heart Rate/drug effects , Hypertension/etiology , Hypertension/physiopathology , Lethal Dose 50 , Methanol/chemistry , Mice , Phytotherapy , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Plants, Medicinal , Rats, Sprague-Dawley , Solvents/chemistry , Sonchus/chemistryABSTRACT
In present study hypoglycaemic effects of the crude powdered C. decussata and its methanolic extract (ME) in alloxan diabetic rabbits were evaluated. The hypoglycaemic effect was measured by blood glucose, insulin level, HbA1c and his to pathology of pancreas. Glucose lowering effect of the ME was studied in diabetic rabbits. The effects of extract on blood glucose, body weight, food in take, fluid intake, OGTT were also evaluated. The results showed that 0.5,1 and 2g/kg of the powder significantly decreased blood glucose levels in normal rabbits and diabetic rabbits at the intervals checked. Oral intake of pioglitazone also reduced the levels in these rabbits. Synergistic hypoglycaemic effect of 600mg/kg of ME with different doses of insulin (2 & 3unit/kg, s/c) further reduced blood glucose levels of treated alloxan-diabetic rabbits. The oral glucose tolerance test revealed lowered area under curve values in ME treated rabbits. Treatment with ME (400 and 600 mg/kg) for 30 days showed highly significant decrease in blood glucose level by augmenting insulin secretion, HbA1cand significant increase in body weight, serum insulin levels in treated diabetic rabbits. Histopathology study showed regeneration of ß-cells. These studies have, therefore, supported the traditional use of this herb in diabetic patients.
Subject(s)
Alloxan , Diabetes Mellitus, Experimental/drug therapy , Gentianaceae , Hypoglycemic Agents/pharmacology , Methanol/chemistry , Plant Extracts/pharmacology , Solvents/chemistry , Animals , Biomarkers/blood , Blood Glucose/drug effects , Blood Glucose/metabolism , Body Weight/drug effects , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/pathology , Drinking/drug effects , Eating/drug effects , Female , Gentianaceae/chemistry , Glucose Tolerance Test , Glycated Hemoglobin/metabolism , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Insulin/blood , Insulin-Secreting Cells/drug effects , Insulin-Secreting Cells/metabolism , Insulin-Secreting Cells/pathology , Male , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal , Rabbits , Time FactorsABSTRACT
INTRODUCTION: Numerous herbal medicines have been recommended for the treatment of different diseases. Achyranthes aspera, Linn. (Family: Amaranthaceae), popularly known as Charchitta or Pitpapra, is commonly used by traditional healers for the treatment of fever, malaria, dysentery, asthma, arterial hypertension, pneumonia, and diabetes. The root extract is well reputed for its insect molting hormonal activity. This investigation was conducted to evaluate the effects of saponins from Achyranthes aspera seeds on the serum lipid profile of albino rats fed a high cholesterol diet. MATERIAL AND METHODS: Hypolipidemic, antioxidant and hepatoprotective activities of these saponins were tested as described previously. To determine the mechanism underlying the observed effects, serum antioxidant status was assessed according to ABTS (2,2'-azino-bis-3-ethylbenzo-thiazoline-6-sulfonic acid), superoxide dismutase and ferric ion reducing antioxidant power (FRAP) assays in saponin-treated hyperlipidemic animals. Liver enzyme levels were determined to reveal any possible hepatotoxicity. RESULTS: Four-week oral administration of A. aspera seed saponins produced a significant (p < 0.05) decrease of total cholesterol, total triglycerides and LDL-C and a significant increase of HDL-C level in hyperlipidemic rats. Treatment with A. aspera seed saponins also showed a significant (p < 0.01) improvement of serum antioxidant status in tested animals. No significant hepatotoxicity was produced by such treatment as the serum liver enzyme activity remained unaltered. CONCLUSIONS: Saponins from A. aspera seeds possess antihyperlipidemic and antioxidant properties which might lead to improvement of serum lipid profile and blood antioxidant status. Our findings support the folkloric use of this indigenous plant in the treatment of hyperlipidemia. However, its exact mechanism of action remains to be elucidated.
ABSTRACT
Berberis orhob, otrvs Bien. ex Aitch. (B.o.) has been reported to have antihypertensive effect in different experimental models. The aim of present study was to evaluate the possible antihypertensive mechanism. Aqueous methanolic extract of B.o. roots and its various fractions namely (ethyl acetate, n-butanol or aqueous) in different concentrations (10 ng/mL, 100 ng/mL, I pg/mL, 10 pg/mL, 100 pg/mL ) were evaluated in isolated perfused rabbit heart to assess their effect on force of contraction, HR and perfusion pressure. The crude extract of B.o. and its fractions exhibited a significant decrease in heart rate, contractility and perfusion pressure of isolated rabbit heart, however, butanolic fraction produced more prominent effect and was selected for further study. The effects of butanol fraction were not blocked by atropine (10' M) in isolated perfused heart. However, butanol fraction significantly blocked the effects of adrenaline (10' M). It is therefore conceivable that cardiac depressant activity of B.o. butanol fraction might be due to the presence of certain 3-blocking agents which might be responsible for antihypertensive effect However, further experiments are required to isolate the active compound(s) and elucidate exact mechanism of action.
Subject(s)
Berberis , Heart/drug effects , Plant Extracts/pharmacology , Animals , Blood Pressure/drug effects , Depression, Chemical , Epinephrine/pharmacology , Female , Heart Rate/drug effects , In Vitro Techniques , Male , Myocardial Contraction/drug effects , RabbitsABSTRACT
Traditionally Thymus linearis Benth. have been used for treatment of various diseases including hypertension. The present study was conducted to evaluate the hypotensive and antihypertensive effect of aqueous methanolic extract of aerial parts of Thymus linearis Benth. in normotensive and hypertensive rats. Acute and subchronic studies were also conducted. The aqueous methanolic extract produced a significant decrease in SBP, DBP, MBP and heart rate of both normotensive and hypertensive rats. LDv, of the extract was found to be 3000 mg/kg. The extract also exhibited a reduction in serum ALT, AST, ALP, cholesterol, triglycerides and LDL levels, while a significant increase in HDL level was observed. It is conceivable therefore, that Thymus linearis Benth. contains certain active compound(s) that are possibly responsible for the observed antihypertensive activity. Moreover, these findings further authenticate the traditional use of this plant in folklore medicine.
Subject(s)
Antihypertensive Agents/pharmacology , Plant Extracts/pharmacology , Thymus Plant , Animals , Blood Pressure/drug effects , Female , Heart Rate/drug effects , Male , Plant Components, Aerial , Plant Extracts/toxicity , Rats , Rats, Sprague-DawleyABSTRACT
The cardiac activity of Saussurea lappa roots was evaluated in isolated perfused rabbit heart by the Langendorff's technique. Heart rate, contractility and coronary flow were determined in the presence of different concentrations of methanolic extract of Saussurea lappa, digoxin and diltiazem. The extract exhibited significant (p<0.01) positive inotropic effect at the first three doses (0.5/µg, 2.5/µg and 5.0/µg) while a significant negative chronotropic effect and coronary flow rates were observed at all the doses tested. These effects were comparable to the effects of digoxin and diltiazem. The increase in force of contraction with decrease in heart rate and coronary flow rates were also observed to be dose dependent as increase in the dose of test extract further enhanced the effects except contractility that started decreasing at higher doses. It is conceivable therefore, that Saussurea lappa roots contain certain pharmacologically active compounds that could be involved in the cardiotonic activity of the extract.
Subject(s)
Cardiotonic Agents/pharmacology , Plant Extracts/pharmacology , Saussurea , Animals , Digoxin/pharmacology , Diltiazem/pharmacology , Female , Male , Plant Roots , RabbitsABSTRACT
The present study evaluated the anti-hyperglycemic and lipid-lowering properties of Emblica officinalis Gaertn. fruit in normal and diabetic human volunteers. The results indicated a significant decrease (P < 0.05) in fasting and 2-h post-prandial blood glucose levels on the 21st day in both normal and diabetic subjects receiving 1, 2 or 3 g E. officinalis powder per day as compared with their baseline values. Significant (P < 0.05) decreases were also observed in total cholesterol and triglycerides in both normal and diabetic volunteers on day 21 that were given either 2 or 3 g E. officinalis powder per day. However, diabetic volunteers receiving only 3 g E. officinalis powder exhibited a significant (P < 0.05) decrease in total lipids on day 21. Both normal and diabetic volunteers receiving 2 or 3 g E. officinalis powder significantly (P < 0.05) improved high-density lipoprotein-cholesterol and lowered low-density lipoprotein-cholesterol levels.
Subject(s)
Blood Glucose/metabolism , Diabetes Mellitus, Type 2/drug therapy , Hypoglycemic Agents/therapeutic use , Hypolipidemic Agents/therapeutic use , Lipids/blood , Phyllanthus emblica , Plant Preparations/therapeutic use , Adult , Cholesterol/blood , Cholesterol, HDL/blood , Cholesterol, LDL/blood , Diabetes Mellitus, Type 2/blood , Fasting , Female , Fruit , Humans , Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/pharmacology , Male , Middle Aged , Plant Preparations/pharmacology , Postprandial Period , Reference Values , Triglycerides/bloodABSTRACT
This paper describes in vitro and in vivo anthelmintic activities of Swertia chirata. In vitro studies revealed that at 25 mg/ml (P>/=0.05) the crude aqueous (CAE) and methanolic extracts (CME) of S. chirata whole plant showed an anthelmintic effect on live Haemonchus contortus. Moreover, in the in vivo study, the whole plant of S. chirata administered as crude powder (CP), CAE and CME at the dose of 3 g/kg to sheep naturally infected with mixed species of gastrointestinal nematodes, showed a significant reduction in egg per gram of faeces.
Subject(s)
Antinematodal Agents/pharmacology , Nematoda/drug effects , Phytotherapy , Plant Extracts/pharmacology , Swertia , Administration, Oral , Animals , Antinematodal Agents/administration & dosage , Antinematodal Agents/therapeutic use , Feces/parasitology , Female , Intestinal Diseases, Parasitic/drug therapy , Intestinal Diseases, Parasitic/veterinary , Male , Nematode Infections/drug therapy , Nematode Infections/veterinary , Parasite Egg Count , Parasitic Sensitivity Tests , Plant Extracts/administration & dosage , Plant Extracts/therapeutic use , Sheep , Sheep Diseases/drug therapy , Sheep Diseases/parasitologyABSTRACT
This paper describes the anthelmintic activity of Zingiber officinale Roscoe (family Zingiberaceae) rhizome, commonly known as ginger, to justify its traditional use in veterinary medicine. Crude powder (CP) and crude aqueous extract (CAE) of dried ginger (1-3 g/kg) were administered to sheep naturally infected with mixed species of gastrointestinal nematodes. Both CP and CAE exhibited a dose- and a time-dependent anthelmintic effect with respective maximum reduction of 25.6% and 66.6% in eggs per gram (EPG) of faeces on day 10 of post-treatment. Levamisole (7.5 mg/kg), a standard anthelmintic agent, exhibited 99.2% reduction in EPG. This study shows that ginger possesses in vivo anthelmintic activity in sheep thus justifying the age-old traditional use of this plant in helminth infestation.