scholarly journals Antiulcerogenic Activity of 1-Hydroxy-3,7,8-trimethoxyxanthone Isolated from the Methanol Extract of Anthocleista vogelii PLANCH. in Rats

Ulcers ◽  
2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Gilbert Ateufack ◽  
Télesphore B. Nguelefack ◽  
Hippolyte K. Wabo ◽  
Pierre Tane ◽  
Albert Kamanyi

Anthocleista vogelii (Loganiaceae) PLANCH. is used in Cameroonian ethnomedicine for the treatment of stomach ache and for curing fever and is used as purgative. Further investigations have shown that the stem bark of this plant possesses potent antiulcer properties. We have investigated the cytoprotective and antisecretory actions of 1-hydroxy-3,7,8-trimethoxyxanthone (AV), the xanthone obtained from the methanol extract of the stem bark. Oral administration of AV at the doses of 1, 2, and 5 mg/kg prevented in a dose-dependent manner ulcers induced by HCl/ethanol (60.90 to 93.22%), Indometacin (46.86 to 89.68%), and pylorus ligation (0.00 to 70.69%). AV reduced pylorus-ligated gastric acid secretion from 134.17 mEq/l in the controls to 118.55, 121.50, and 96.93 mEq/l, respectively, for the 1, 2, and 5 mg/kg doses and increased mucus secretion significantly in a dose-dependent manner in all experimental models. The cytoprotective and antisecretory properties of AV could thus be due to its ability to strengthen gastric mucosal defences through enhanced gastric mucus production.

2014 ◽  
Vol 25 (3-4) ◽  
pp. 24-33
Author(s):  
O. I. Dzjuba ◽  
M. V. Yatsenko

The article deals with the history of the study and the current state of research of physiological and biochemical properties of the plant genus Sedum that are useful for human and has been used in folk medicine for many years. It was noticed that antioxidant properties of extracts from plants S. sarmentosum, S. sempervivoides, S. takesimense were caused by the presence of phenolic compounds. Methanol extract of plants S. takesimense exhibited strong scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals as well as significant inhibitory effects on lipid peroxidation and low density lipoprotein (LDL) oxidation induced by a metal ion Cu2+. Various immunomodulatory activities of various fractions of plants extracts (S. dendroideum, S. kamtschaticum, S. sarmentosum, S. telephium) are observed. It was shown that the ethanol extract of S. sarmentosum and it’s fractions suppressed specific antibody and cellular responses to ovalbumin in mice. The methanol extract of plants S. sarmentosum reduced the levels of anti-inflammatory markers, such as volume of exudates, number of polymorphonuclear leukocytes, suppressed nitric oxide synthesis in activated macrophages via suppressed induction of inducible nitric oxide synthase (iNOS). Polysaccharides fractions from plants S. telephium inducing productions of tumor necrosis factor alpha (TNF-α), increasing the intensity of phagocytosis in vitro and in vivo. Methanol extract from the whole part of S. kamtschaticum strongly inhibit PGE2 production from lipopolysaccharide-induced RAW 264.7 cells, a mouse macrophage cell line via modulating activity in gene expression of the enzyme cyclooxygenase-2 (COX-2). The methanol extract of plants S. sarmentosum and the major kaempferol glycosides from S. dendroideum have antinociceptive activity. It was noticed that anti-adipogenic activity of extracts from plants S. kamtschaticum were caused by inhibition of peroxisome-proliferator-activated receptor γ (PPARγ) expression and it’s dependent target genes, such as genes encoding adipocyte protein 2 (аР2), lipoprotein lipase (LPL), adiponectin and CD36. Polysaccharides fractions from S. telephium cause inhibition of cell adhesion of human fibroblast (MRC5) to laminin and fibronectin via interfere with integrin-mediated cell behaviour and they contributed to the role of polysaccharides in cell-matrix interaction. The methanol extract of plants S. sarmentosum exhibited a significant inhibitory activity in the chick embryo chorioallantoic membrane angiogenesis in a dose-dependent manner. The crude alkaloid fraction of S. sarmentosum caused a dose-dependent inhibition of cell proliferation on murine hepatoma cell line BNL CL.2 and human hepatoma cell line HepG2 without necrosis or apoptosis. Alkaloids from plants S. sarmentosum may improve survival of hepatoma patients via the inhibition of excessive growth of tumor cells. Plant’s juices have antiviral activity (S. sarmentosum, S. spurium, S. stahlii). Crude ethanol extract S. praealtum have spermicidal activity of the in mice and a relevant inhibitory effect of aqueous extract on human spermatozoa motility as well as an anti-fertilizing activity in rats. Hepatoprotective triterpenes, e.g., δ-amyrone, 3-epi-δ-amyrin, δ-amyrin and sarmentolin were isolated from S. sarmentosum. 2- and 2,6-substituted piperidine alkaloids (e.g., norsedamine, allosedridine, sedamine, allosedamine) are observed in plants S. acre, which in the presence of data on the use of pyridine and piperidine derivatives for treating neurodegenerative diseases (e.g., Alzheimer's disease), points on the promising research in this area. Taking into account that biologically active compounds are accumulated in the aboveground vegetative organs of plants of Sedum, the prospects of further study of the use of Sedum for the purposes of biotechnology and in the pharmaceutical industry becomes apparent. This work extends the existing views regarding the use of plants Sedum.


Author(s):  
Vanessa Mba Matah Marthe ◽  
Gilbert Ateufack ◽  
Marius Mbiantcha ◽  
William Yousseu Nana ◽  
Albert Donatien Atsamo ◽  
...  

AbstractObjectivesIn African traditional medicine, Distemonanthus benthamianus (Caesalpiniaceae) is used to treat many diseases including gastric ulcers. We evaluated in this study, the cytoprotective and antisecretory properties of the methanolic extract of the stem bark of this plant using different technics of gastric lesion induction.MethodsCytoprotective and antisecretory activity of the methanolic extract of D. benthamianus stem bark was evolved through six methods of gastric lesion induction in experimental Wistar male rats (150–200 g): (1) gastric lesions induced by HCl/ethanol, (2) gastric lesions induced by Indomethacin- HCl/ethanol, (3) gastric lesion induced by Indomethacin, (4) gastric lesions induced by Pylorus ligation, (5) gastric lesions induced by histamine-Pylorus ligation, (6) gastric lesions induced by carbachol-Pylorus ligation. Mucus and gastric mucosal ulceration were evaluated. pH, gastric volume, and acidity were quantified in all pylorus ligation induction technics. Nitric oxide (NO) level was determined in indomethacin induced gastric ulcers.ResultsAt different doses (125, 250 and 500 mg/kg), extract reduced significantly the ulcer index. In all models used, that is 100.00% with HCl/ethanol; 100.00% with HCl/ethanol/indomethacin; 95.70% with Indomethacin; 74.79% with pylorus ligation, 95.94% histamine-Pylorus ligation, 99.54% carbachol-Pylorus ligation at the highest dose of 500 mg/kg. The lesion formation reduces in all the methods used followed by a significant increase of mucus production. The pylorus ligation technic revealed that the extract has an antisecretory activity.ConclusionsThe methanolic extract of D. benthamianus stem bark has both cytoprotective and antisecretory effects. This extract exerts its antisecretory effect trough cholinergic and histaminergic pathways.


2000 ◽  
Vol 44 (6) ◽  
pp. 1757-1760 ◽  
Author(s):  
Brent E. Korba ◽  
R. F. Schinazi ◽  
Paul Cote ◽  
Bud C. Tennant ◽  
John L. Gerin

ABSTRACT Emtricitabine [(−)FTC] [(−)-β-2′,3′-dideoxy-5-fluoro-3′-thiacytidine] has been shown to be an effective inhibitor of hepatitis B virus (HBV) in cell culture, with a potency and selectivity that are essentially identical to those of lamivudine. The antiviral activity of oral administration of (−)FTC against WHV replication in chronically infected woodchucks, an established and predictive model for antiviral therapy against HBV, was examined in a placebo-controlled study. (−)FTC significantly reduced viremia and intrahepatic WHV replication in a dose-dependent manner that was comparable to the antiviral activity of lamivudine observed in previous studies conducted by our laboratories. No effect on the levels of hepatic WHV RNA or the levels of woodchuck hepatitis surface antigen or anti-woodchuck hepatitis surface and core antibodies in the serum of the treated animals was observed. No evidence of drug-related toxicity was observed in any of the animals treated.


Author(s):  
Amit Subedi ◽  
Mohan Prasad Amatya ◽  
Tirtha Maiya Shrestha ◽  
Shyam Kumar Mishra ◽  
Bharat Mani Pokhrel

The methanol extract of the bark of Machilus odoratissima was subjected to investigate its antioxidant and antibacterial properties. The phytochemical screening demonstrated the presence of different types of compound like terpenoids, tannins, deoxy sugar, saponins and phenolic compounds. The methanol extract of the plant was tested for antioxidant activity using scavenging activity of DPPH(1,1-diphenyl-2-picrylhydrazil) radical method and antibacterial activity against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli & Pseudomonas aeruginosa bacteria using cup plate method. The extract exhibited high free radical scavenging activity. IC50 was found to be 3.37μg/ml. Antibacterial activity was observed against S. aureus in dose dependent manner DOI: http://dx.doi.org/10.3126/kuset.v8i1.6045 KUSET 2012; 8(1): 73-80


1999 ◽  
Vol 77 (11) ◽  
pp. 886-895 ◽  
Author(s):  
Gordon Bolger ◽  
Jean-Claude Vigeant ◽  
Francine Liard ◽  
Bruno Simoneau ◽  
Diane Thibeault ◽  
...  

The human renin infused rat model (HRIRM) was used as an in vivo small-animal model for evaluating the efficacy of a collection of inhibitors of human renin. The intravenous infusion of recombinant human renin (2.4 µg·kg-1·min-1) in the ganglion-blocked, nephrectomized rat produced a mean blood pressor response of 47 ± 3 mmHg (1 mmHg = 133.3 Pa), which was reduced by captopril, enalkiren, and losartan in a dose-dependent manner following oral administration, with ED50 values of 0.3 ± 0.1, 2.5 ± 0.9, and 5.2 ± 1.6 mg/kg, respectively. A series of peptidomimetic P2-P3 butanediamide renin inhibitors inhibited purified recombinant human renin in vitro in a concentration-dependent manner, with IC50 values ranging from 0.4 to 20 nM at pH 6.0, with a higher range of IC50 values (0.8-80 nM) observed at pH 7.4. Following i.v. administration of renin inhibitors, the pressor response to infused human renin in the HRIRM was inhibited in a dose-dependent manner, with ED50 values ranging from 4 to 600 µg/kg. The in vivo inhibition of human renin following i.v. administration in the rat correlated significantly better with the in vitro inhibition of human renin at pH 7.4 (r = 0.8) compared with pH 6.0 (r = 0.5). Oral administration of renin inhibitors also resulted in a dose-dependent inhibition of the pressor response to infused human renin, with ED50 values ranging from 0.4 to 6.0 mg/kg and the identification of six renin inhibitors with an oral potency of <1 mg/kg. The ED50 of renin inhibitors for inhibition of angiotensin I formation in vivo was highly correlated (r = 0.9) with the ED50 for inhibition of the pressor response. These results demonstrate the high potency, dose dependence, and availability following oral administration of the butanediamide series of renin inhibitors.Key words: renin-angiotensin system, recombinant human renin, rat, renin inhibitors.


2020 ◽  
Author(s):  
Joy I. Odimegwu ◽  
Tolulope F. Okanlawon ◽  
Obumneme Noel ◽  
Ismail Ishola

ABSTRACTBackgroundThe rise in occurrence of hypertension, a non-communicable disease and a major factor for chronic renal failure, cardiovascular disease, and stroke, which most times lead to sudden death is worrisome. Resistant hypertension is more common and may have no symptoms at all for months or years, but then can cause heart attack, stroke, and vision and kidney damage. Prevention and quick management of hypertension are therefore essential in reducing the risk of these debilitating ailments. Aqueous and ethanolic extracts of the leaves of Clerodendrum chinensis (AeC and EeC) are used by local communities of West Africa as medicine for rapid antihypertensive actions. We aim to discover the scientific basis for the use of the herb as medicine.MethodsThis work investigates the antihypertensive effects of AeC and EeC in L-Arginine Methyl Ester Hydrochloride (L-NAME)-induced hypertensive rats Acetylcholine, L-Arginine and Sodium Nitroprusside were used as standards. All results were expressed as means ± standard error of mean. Differences were considered significant at p <0.05.ResultsIntravenous administration of the extracts caused a significant decrease in the Mean Arterial Blood Pressure (MABP) in a dose-dependent manner. AeC at 100mg/kg caused a significant decline in blood pressure in a dose-related manner. Likewise at 100mg/kg, EeC reduced MABP steadily from 103.9± 2.55 to 34.1± 0.95mmHg. The two extracts; possess significant antihypertensive properties.ConclusionsBoth extracts show significant antihypertensive effects and at high doses could lead to hypotension and so should be used with care. Further research is necessary to determine safe dosage forms.


Author(s):  
Carla Wulandari Sabandar ◽  
Juriyati Jalil ◽  
Norizan Ahmat ◽  
Nor-Ashila Aladdin ◽  
Harni Sartika Kamaruddin ◽  
...  

Songi (Dillenia serrata) is a tree endemic to Southeast Sulawesi and its stem bark been used in folk medicine. Nonetheless, only a handful scientific knowledge regarding chemistry and biological activities has been investigated on the plant. The present study aimed to investigate the antioxidant and xanthine oxidase (XO) inhibitory activity of the stem bark of the plant. Methanol extract and organic fractions (petroleum ether, ethyl acetate, and methanol) of the dried powdered stem bark of songi were evaluated for phytochemical screening, total phenolic (TPC), total flavonoid contents (TFC), DPPH, FRAP, and XO in vitro assays. Flavonoids, tannins, terpenoids, steroids, and saponins present in the extract. TPC and TFC in extract were 59.2 mg GAE/g and 23.4 mg QE/g. The contents in organic fractions were in solvent-dependent manner (methanol>ethyl acetate>petroleum ether). Extract and fractions scavenged DPPH radicals (48.2–59.7%) at 100 μg/mL compared to ascorbic acid, trolox, and gallic acid (90.3–93.8%). FRAP values varied from 0.8–3.4 μg/μg equivalent trolox amount (quercetin and gallic acid were 25.7 dan 32.4 μg/μg, respectively). They also inhibited xanthine oxidase (15.3–50.3%) at 100 μg/mL (allopurinol, 98.2%). The study concluded the potential of methanol extract and organic fraction of the stem bark of songi, thus highlighted the prospect of songi to be used in herbal and drugs development from nature.


Author(s):  
B. O. Oluwatayo ◽  
T. A. Kolawole ◽  
C. C. Wali ◽  
O. A. Olayanju ◽  
A. E. J. Okwori

Background: This study investigated the potential antioxidant effects of aqueous extract of the stem bark of Theobroma cacao L. in Wistar rats. Methods: Twenty Wistar rats weighing between 126 g – 224 g were grouped randomly into 4groups of 5 rats each. Group 1 served as control and received water while groups 2, 3 and 4 rats were given 1000mg/kg, 3000mg/kg and 5000mg/kg b.wt of the extract respectively for 28days. On the 29th day, the rats were anaesthetized and blood samples were collected for analysis of some haematological parameters, enzymatic and non- enzymatic antioxidant activities. Results: The results obtained showed that there was significant increase (p<0.001) in SOD, Catalase activities and MDA levels in a dose dependent manner. The results also showed significant increase (p<0.001) in RBC Group 2, 3 and 4 rats when compared to the Group1. Significant increase was also observed in Hemoglobin (Hb) and Hematocrit (Hct) level in group 2 and 3 rats (p<0.001). Mean corpuscular volume was significantly increased in group 2 rats (p<0.001). Conclusion: The findings from this study showed the antioxidant and hematinic potentials of the stem bark of Theobroma cacao L.The aqueous extract of the stem bark of Theobroma cacao L. has a potential antioxidative and hematinic effects in Wistar rats. This is largely due to its rich phytochemical and nutritive contents. Further research work will be needed to see the possible application of these properties in humans.


2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Azis Saifudin ◽  
Ken Tanaka ◽  
Shigetoshi Kadota ◽  
Yasuhiro Tezuka

A methanol extract of the leaves of Blumea balsamifera (L.) DC. (Asteraceae) afforded a new guaian-type sesquiterpene, epiblumeaene K (1), together with four known guaian-type sesquiterpenes (2–5), three known sesquiterpenes (6–8), and nine known flavonoids (9–17) by a combination of chromatography and preparative TLC techniques. Their structures were elucidated by extensive spectroscopic methods and comparison with the literature data. Among the isolated compounds, a known sesquiterpene, β-caryophyllene 8 R,9 R-oxide (6), exhibited a significant PTP1B inhibitory activity in a dose-dependent manner, with an IC50 value of 25.8μM (5.62μg/mL).


Author(s):  
Temitayo O. Iji ◽  
Ademola A. Oyagbemi ◽  
Odunayo I. Azeez

This study was designed to investigate the effects of prolonged oral administration of calcium hypochlorite in the drinking water of commercial cockerels. It was carried out in order to ascertain probable toxicity associated with prolonged exposure to calcium hypochlorite. Thirty-two healthy birds were used; they were grouped into four groups of eight. Group 1, which served as the control, received 10 mL/kg body weight of physiological saline. Groups 2, 3 and 4 received 0.0375 g, 0.375 g and 0.75 g of calcium hypochlorite per 10 litres of drinking water for six weeks respectively. Six weeks after the administration of calcium hypochlorite, blood was collected from the jugular vein to assess liver function, lipid profiles and for markers of oxidative stress. The results revealed a significant (p < 0.05) increase in alanine aminotransferase activity in a dose-dependent manner when compared with the control. Also, there was a significant (p < 0.05) increase in aspartate aminotransferase and alkaline phosphatase activity. Similarly, there was a significant (p < 0.05) increase in total cholesterol, triglycerides, high-density lipoprotein and low-density lipoprotein levels compared with the control. There was a significant increase in malondialdehyde and hydrogen peroxide generation with a concomitant significant (p < 0.05) decrease in serum glutathione level in a dose-dependent manner when compared with the control. In this study, calcium hypochloriteinduced hepatic damage via oxidative stress and decrease in antioxidant defense system was found. Therefore, prolonged exposure of chickens to calcium hypochlorite is potentially harmful.


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