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1.

Objective:

In-vitro red blood cell (RBC) partitioning of doxycycline was studied to determine whether doxycycline penetrates RBC and its concentration was assayed keeping in view its high lipophilicity.

Materials and Methods:

Standardization of doxycycline was performed in whole blood and plasma of cattle by microbiological assay using Bacillus subtillis ATCC 6633 as indicator organizm. Actual concentration of the drug was obtained by comparing zone inhibition with standard graph and the extent of partitioning was mathematically calculated.

Results:

The R2 value of standard graph for doxycycline was 0.9934 and 0.9727 for plasma and whole blood, respectively. Overall, RBC partitioning of doxycycline was found to be 18.40 ± 1.70%.

Conclusions:

Overall RBC partitioning of doxycycline indicated low penetration into RBC. Plasma is the fluid suggested for pharmacokinetic evaluation of doxycycline.  相似文献   

2.

Objective:

To evaluate the in vivo antiplasmodial activity of the ethanol leaf extract of Stachytarpheta cayennensis in the treatment of various ailment in Niger Delta region of Nigeria, in Plasmodium berghei infected mice.

Materials and Methods:

The ethanolic leaf extract of Stachytarpheta cayennensis (90-270 mg/kg/day) was screened for blood schizonticidal activity against chloroquine sensitive Plasmodium berghei berghei in mice. The schizonticidal effect during early and established infections was investigated.

Result:

Stachytarpheta cayennensis (90-270 mg/kg/day) exhibited significant (P< 0.05) blood schizonticidal activity both in 4-day early infection test and in established infection with a considerable mean survival time comparable to that of the standard drug, chloroquine, 5 mg/kg/day.

Conclusion:

The leaf extract possesses significant (P< 0.05) antiplasmodial activity which confirms it''s use in folkloric medicine in the treatment of malaria.  相似文献   

3.

Objectives:

To study the effects of Parthenium hysterophorus L. flower on serum glucose level in normal and alloxan induced diabetic rats.

Materials and Methods:

Albino rats were divided into six groups of six animals each, three groups of normal animals receiving different treatments consisting of vehicle, aqueous extract of Parthenium hysterophorus L. flower (100 mg/kg) and the standard antidiabetic drug, glibenclamide (0.5 mg/kg). The same treatment was given to the other three groups comprising alloxan induced diabetic animals. Fasting blood glucose level was estimated using the glucose oxidase method in normal and alloxan induced diabetic rats, before and 2 h after the administration of drugs.

Results:

Parthenium hysterophorus L. showed significant reduction in blood glucose level in the diabetic (P<0.01) rats. However, the reduction in blood glucose level with aqueous extract was less than with the standard drug glibenclamide. The extract showed less hypoglycemic effect in fasted normal rats, (P<0.05).

Conclusion:

The study reveals that the active fraction of Parthenium hysterophorus L. flower extract is very promising for developing standardized phytomedicine for diabetes mellitus.  相似文献   

4.

Objective:

To evaluate the in vitro cytotoxicity and antibacterial properties of Cassia occidentalis (whole plant) via alcoholic, hydro-alcoholic, and aqueous extracts against eight human cancer cell lines from six different tissues and four bacterial strains.

Material and Methods:

in vitro cytotoxicity against the human cancer cells, cultured for 48h in presence of different concentrations C. occidentalis extracts and percentage of cell viability, was evaluated using the sulforhodamine-B (SRB) assay. The antibacterial activity was performed using the standard protocol against bacterial strains.

Results:

It was observed that aqueous extract of C. occidentalis (whole plant) had more potential than hydro-alcoholic and alcoholic extracts against HCT-15, SW-620, PC-3, MCF-7, SiHa, and OVCAR-5 human cancer cell lines at 100, 30, and 10 μg/ml in a dose-dependent manner. The hydro-alcoholic extract showed potential against Bacillus subtillis.

Conclusion:

The plant can be explored for the possible development of lead molecules for drug discovery.  相似文献   

5.

Objective:

This study was designed to evaluate the anti-inflammatory and antipyretic activity of ethyl acetate extract of Vitex leucoxylon Linn. in various animal experimental models.

Materials and Methods:

Ethyl acetate extract of V. leucoxylon Linn. evaluated for anti-inflammatory activity in carrageenan, mediator-induced rat paw edema, and cotton pellet-induced granuloma model. The antipyretic activity was evaluated by yeast-induced pyrexia model.

Results:

Single administration of the ethyl acetate extract of V. leucoxylon Linn. at dose of 500 mg/kg p.o. showed significant (P < 0.001) inhibition of rat paw edema. The ethyl acetate extract showed significant antipyretic activity in brewer yeast-induced pyrexia in rats throughout the observation period of 4 h.

Conclusion:

This study shows that ethyl acetate extract of V. leucoxylon Linn. has significant anti-inflammatory and antipyretic activity.  相似文献   

6.

Background and Purpose:

A water decoction of the poisonous shrub Cleistanthus collinus is used for suicidal purposes. The mortality rate is 28%. The clinical profile includes distal renal tubular acidosis (DRTA) and respiratory failure. The mechanism of toxicity is unclear.

Objectives:

To demonstrate features of C. collinus toxicity in a rat model and to identify its mechanism(s) of action.

Materials and Methods:

Rats were anesthetized and the carotid artery was cannulated. Electrocardiogram and respiratory movements were recorded. Either aqueous extract of C. collinus or control solution was administered intraperitoneally. Serial measurements of blood gases, electrolytes and urinary pH were made. Isolated brush border and basolateral membranes from rat kidney were incubated with C. collinus extract and reduction in ATPase activity was assessed. Venous blood samples from human volunteers and rats were incubated with an acetone extract of C. collinus and plasma potassium was estimated as an assay for sodium–potassium pump activity.

Results:

The mortality was 100% in tests and 17% in controls. Terminal event in test animals was respiratory arrest. Controls had metabolic acidosis, respiratory compensation acidic urine and hyperkalemia. Test animals showed respiratory acidosis, alkaline urine and low blood potassium as compared to controls. C. collinus extract inhibited ATPase activity in rat kidney. Plasma K+ did not increase in human blood incubated with C. collinus extract.

Conclusions and Implications:

Active principles of C. collinus inhibit proton pumps in the renal brush border, resulting in type I DRTA in rats. There is no inhibition of sodium–potassium pump activity. Test animals develop respiratory acidosis, and the immediate cause of death is respiratory arrest.  相似文献   

7.

Objective:

The present study was designed to evaluate the effect of Aegle marmelos unripe fruit extract (AMFE) on inflammatory bowel disease (IBD) in Wistar albino rats.

Materials and Methods:

Effect of AMFE was studied on acetic acid induced ulcerative colitis (1 ml of 4% acetic acid solution, transrectal) and indomethacin-induced enterocolitis (10 mg/kg, single dose, p.o) in Wistar albino rats. The extract was administered orally at different dose of 150, 200 and 250 mg/kg body weight. Disease pathogenesis was assessed by measuring disease activity index (DAI), macroscopic score, microscopic score, mesenteric mast cell protection, superoxide dismutase (SOD), and malonaldehyde (MDA) levels in the above two models.

Results:

The results showed a dose dependent decrease in intestinal inflammation following treatment with AMFE. Significant protection in mast cell degranulation was observed in acetic acid and indomethacin-induced IBD models. Treatment with AMFE significantly decreased the MDA levels and increased SOD activity.

Conclusion:

In our study, AMFE produced anti-inflammatory, antioxidant, and mast cell stabilizing effects demonstrating protective effect in inflammatory bowel disease.KEY WORDS: Aegle marmelos (bael), aqueous extract, inflammatory bowel disease  相似文献   

8.

Aims:

The aim of study was to evaluate the scientific basis for the traditional use of Elephantopus scaber leaves.

Materials and Methods:

In the present study, ethanol extract of Elephantopus scaber leaves was evaluated for preliminary phytochemical screening and antiasthmatic activity using histamine and acetylcholine-induced bronchospasm, mast cell degranulation and histamine induced constriction on isolated guinea pig tracheal chain at different dose levels. Student''s t-Test and Dunett''s test were used for statistical analysis.

Results:

The result of present investigation showed that the ethanolic extract of E. scaber significantly (P<0.001) decreased the bronchospasm induced by histamine, acetylcholine and protected mast cell degranulation as compared to control groups. It also decreased the histamine induce constriction on isolated guinea pig trachea in dose-dependent manner. Phytochemical studies revealed the presence of steroids, saponin, flavonoids, and phenolic compounds in the extract.

Conclusions:

The present study concludes that the antiasthmatic activity of ethanolic extract of E. scaber leaves may be due to the presence of flavonoids or steroids. Antiasthmatic action of the E. scaber could be due to its antihistaminic, anticholinergic and mast-cell-stabilizing property.KEY WORDS: Elephantopus scaber, bronchospasm, mast cell degranulation, compound 48/80  相似文献   

9.

AIM

To assess the similarities in intracellular pharmacokinetics (PK) of methotrexate (MTX) in red blood cells (RBCs) and other cell lines.

METHODS

Three previously published PK models for intracellular MTX and MTX polyglutamate (MTXGlu2–5) concentrations were used: (i) a model for the kinetics in RBCs, (ii) a model for the kinetics in human breast cancer cells (HBCCs) and (iii) a model for the kinetics in various white blood cell (WBC) lines. All three models were used to simulate the response in a typical individual receiving 10 mg oral MTX once weekly and the predicted steady-state concentrations (Css) and time to Css (tss) were compared.

RESULTS

The HBCC model showed a lower Css for MTXGlu2 and 3 and higher Css for MTXGlu4 and 5 compared with the RBC PK model, while tss and overall intracellular MTX exposure appeared similar. The WBC PK model showed much lower Css for the parent MTXGlu1 and of tssfor all MTXGlun, as well as a much lower cumulative Css for MTXGlu2–7 for the majority of the WBC cell lines.

CONCLUSION

RBC kinetics of MTX differ from the kinetics in other cell types such as WBCs and HBCCs to a variable degree. It is possible that similarly diverse profiles may exist across other cell lines, including those on the causal path in rheumatoid arthritis. Hence, there may not necessarily be a clear link between RBC MTX concentrations and disease control in rheumatoid arthritis.  相似文献   

10.

Objective:

This study was designed to investigate the effect of aqueous extract of Pterocarpus marsupium Roxb. on elevated inflammatory cytokine, tumor necrosis factor (TNF)-α in type 2 diabetic rats.

Materials and Methods:

Type 2 diabetes was induced by administering streptozotocin (90 mg/kg, i.p.) in a neonatal rat model. Aqueous extract of P. marsupium at a dose of 100 and 200 mg/kg was given orally to desired group of animals for a period of 4 weeks. After 4 weeks of drug treatment, parameters such as fasting blood glucose, postprandial blood glucose, and TNF-α in serum were analyzed.

Results:

Aqueous extract of P. marsupium at both doses, i.e., 100 and 200 mg/kg, decreased the fasting and postprandial blood glucose in type 2 diabetic rats. The 200 mg/kg had more pronounced effect on postprandial hyperglycemia. The drug also improved the body weight of diabetic animals. Cytokine TNF-α was found to be elevated in untreated diabetic rats due to chronic systemic inflammation. The aqueous extract at both doses significantly (P < 0.001) decreased the elevated TNF-α level in type 2 diabetic rats.

Conclusion:

Modulation of cytokine TNF-α by the rasayana drug P. marsupium is related with its potential anti-diabetic activity.  相似文献   

11.

Objective:

To evaluate the in vivo antimalarial activities of ethanolic leaf and stembark extracts of Anthocleista djalonensis used traditionally as malarial remedy in Southern Nigeria in mice infected with Plasmodium berghei berghei.

Methods:

The ethanolic extracts of the A. djalonensis leaf (1000 – 3000 mg/kg/day) and stembark (220 – 660 mg/kg/day) were screened for blood schizonticidal activity against chloroquine-sensitive P. berghei in mice. The schizonticidal effect during early and established infections was investigated.

Results:

The A. djalonensis leaf extract (1000 – 3000 mg/kg/day) exhibited a significant antiplasmodial activity both in the 4-day early infection test and in the established infection with a considerable mean survival time, which was incomparable to that of the standard drug, chloroquine (5 mg/kg/day). The stembark extract (220 – 660 mg/kg/day) also demonstrated a promising blood schizontocidal activity in early and established infections.

Conclusion:

These plant extracts possess considerable antiplasmodial activities, which justify their use in ethnomedicine and can be exploited in malaria therapy.  相似文献   

12.

Objective:

To investigate the peritoneal mast cell stabilization activity of Pothos scandens extracts

Materials and Methods:

Pothos scandens L. (family- Araceae) aerial part was successively extracted with ethanol and aqueous to prepare extract of the plant. The extracts of P. scandens were evaluated for stabilization of mast cell in rat allergic models. The extract of P. scandens ethanolic, 50% aqueous ethanolic and aqueous (1, 10 and 100 μg/ml) was studied for peritoneal mast cell stabilization activity in rat mesenteric preparation induced by C 48/80.

Result:

Preliminary phytochemical analysis revealed the presence of carbohydrates, fixed oil, proteins, alkaloids, glycosides, flavonoids and phenolic compounds. The ethanolic, 50% aqueous ethanolic and aqueous extracts of P. scandens L. showed dose dependent increase in the number of intact cells when compare with C48/80 at the concentration of 10 and 100 μg/ml. It virtues further work towards the isolation of phytoconstituents from this plant.

Conclusion:

This finding provides evidence that the P. scandens L. inhibits mast cell-derived immediate-type allergic reactions and mast cell degranulation. P. scandens has a potential as allergic anti- asthmatic agent.KEY WORDS: Compound 48/80, ethanolic extract, mast cell, Pothos scanden  相似文献   

13.

Objective:

To evaluate the hypoglycemic activity of various extracts, petroleum ether, chloroform and aqueous extract of Cassia occidentalis in normal and alloxan-induced diabetic rats.

Materials and Methods:

Petroleum ether, chloroform and aqueous extract of whole plant of Cassia occidentalis were orally tested at the dose of 200 mg/kg for hypoglycemic effect in normal and alloxan-induced diabetic rats. In addition, changes in body weight, serum cholesterol, triglyceride and total protein levels, assessed in the ethanol extract-treated diabetic rats, were compared with diabetic control and normal animals. Histopathological observations during 21 days treatment were also evaluated.

Results:

Aqueous extract of C. occidentalis produced a significant reduction in fasting blood glucose levels in the normal and alloxan-induced diabetic rats. Apart from aqueous extract, petroleum ether extract showed activity from day 14 and chloroform extract showed activity from 7 days. Significant differences were observed in serum lipid profiles (cholesterol and triglyceride), serum protein, and changes in body weight by aqueous extract treated-diabetic animals, when compared with the diabetic control and normal animals. Concurrent histopathological studies of the pancreas of these animals showed comparable regeneration by extract which were earlier necrosed by alloxan.

Conclusion:

Aqueous extract of C. occidentalis exhibited significant antihyperglycemic activity in normal and alloxan-induced diabetic rats. They also showed improvement in parameters like body weight and serum lipid profiles as well as histopathological studies showed regeneration of β-cells of pancreas and so might be of value in diabetes treatment.  相似文献   

14.

Objective:

The current work was aimed to evaluate the nephroprotective potential of Butea monosperma.

Materials and Methods:

Butea monosperma was collected from local forest of Jabalpur and extracted with ethanol. Healthy adult male Wistar albino rats between 5 and 6 months of age and weighing about 150-200 g were used for the study. Acute toxicity studies were performed to determine dose of extract. Nephrotoxicity was induced by gentamicin. Animals were divided in four groups in which first group served as positive control, second group as gentamicin treated toxic control; animals of group three and four were treated with Butea monosperma extract. Extract was administered to animals via oral route. Serum creatinine, serum urea, and blood urea nitrogen were estimated. Body weight was also determined. Histopathological studies were performed to access gross anatomical changes in animals.

Results:

The extract of Butea monosperma was found to be rich in flavonoids, polyphenolics, and alkaloids. Urine creatinine, serum urea, and blood urea nitrogen were found to be significantly (P < 0.001) increased in rats treated with only gentamicin; whereas, treatment with the ethanolic extract of leaf of Butea monosperma reversed the effect of gentamicin indicating nephroprotective activity.

Conclusion:

The present study revealed that ethanolic extract of Butea monosperma is a good source of phytochemicals. The phytoconstituents flavonoids, phenolics, and alkaloids present in the extracts may be responsible for antioxidant activity. By the virtue of antioxidant activity, Butea monosperma demonstrated nephroprotective activity.KEY WORDS: Butea monosperma, gentamicin, nephroprotective  相似文献   

15.

Objective:

The present study was performed to evaluate the preventive and curative antidiarrheal effects of the methanol extract, fractions and compound from the stem bark of Trilepisium madagascariense in rats.

Materials and Methods:

The methanol extract from the stem bark of T. madagascariense, its fractions (n-hexane, ethyl acetate, n-butanol and aqueous residue) and compound (obtained from further column chromatography of the ethyl acetate fraction) were evaluated for the antidiarrheal activity in rats. These test samples (at 100, 200 and 400 mg/kg for the extract and fractions and 2.5 mg/kg for compound) were assayed on the latent periods, purging indices and fecal frequencies in castor oil-induced diarrhea. Gastrointestinal transit and castor oil-induced enteropooling assays were conducted. Shigella-induced diarrhea was assayed. Blood chemistry and fecal Shigella load were examined.

Results:

The fractionation of the ethyl acetate fraction from the methanol extract of T. madagascariense afforded a known compound [isoliquiritigenin (1)]. Compound 1 increased the latent period of diarrhea induction (179.40 min) compared to the saline control (60.80 min). The purging indices, fecal frequencies and intestinal enteropooling decreased with an increase in the dose of test samples. The blood cell counts, sera creatinine and fecal Shigella load decreased significantly (P ≤ 0.05) in the plant extract-treated rats compared to the saline control.

Conclusion:

The results of our study, being reported for the first time, provide clear evidence that the methanol extract, fractions and isoliquiritigenin from T. madagascariense stem bark possess antidiarrheal activities.  相似文献   

16.

Objectives:

The purpose of the present study was to investigate the anti-inflammatory properties of aqueous extract of the leaves of H. integrifolia, Planch.

Materials and Methods:

The hind paw edema was produced in rats by subplanter injection of carageenan. The aqueous extract of H. integrifolia, Planch. (AHI) at dose (250 and 500 mg/kg p.o) was given to observe % inhibition of paw edema which were comparable with indomethacin (10 mg/kg p.o) used as a reference drug.

Results:

The extract administered orally at doses of 250 and 500 mglkg p.o produced a significant (P < 0.05) dose dependent inhibition of edema formation

Conclusions:

A significant % inhibition of paw edema by the aqueous extract of leaves of H. integrifolia, Planch. and its almost nearby same % inhibition with indomethacin suggest its usefulness as an anti-inflammatory agent.  相似文献   

17.

Objectives:

This study was conducted to determine the effect of ethanolic extract of the dried stems of Tinospora crispa in a male rat model of hepatic fibrosis caused by the hepatotoxin, thioacetamide.

Materials and Methods:

The extract was gavaged daily to the rats, at doses of 100 and 200 mg/kg along with thioacetamide at a dose of 200 mg/kg twice weekly. To assess the effectivity of extract, against thioacetamide, the activity of aminotransferases (alanine aminotransferase, aspartate aminotransferase), alkaline phosphatase (AP); and bilirubin were measured, together with morphological and histopathological indices in the liver of healthy and thioacetamide-treated rats.

Results:

A significant increase in the activity of liver enzymes, bilirubin and G-glutamyl transferase and gross and histopathological changes were determined. Although previous in vitro study established that this extract had strong antioxidant activity, this in vivo study establishes that this extract contains hepatotoxins whose identity may be quite different from those compounds with antioxidant properties.

Conclusion:

The study confirms that complete reliance on data obtained using in vitro methodologies may lead to erroneous conclusions pertaining to the safety of phytopharmaceuticals.  相似文献   

18.

Objective:

To assess the anticataleptic and antiepileptic activity of leaves of Mucuna pruriens in albino rats.

Materials and Methods:

Haloperidol-induced catalepsy (HIC), maximum electro-shock (MES) method, pilocarpine-induced Status epilepticus (PISE) and single-dose effect of M. pruriens were employed.

Results:

M. pruriens (100 mg/kg) had significant anticataleptic and antiepileptic activity in HIC, MES, and PISE.

Conclusions:

M. pruriens extract has the potential to be an anticataleptic and antiepileptic drug. Dopamine and 5-HT may have a role in such activity.  相似文献   

19.

Objective:

The objective of the present study was to evaluate the adaptogenic property of the ethyl acetate-soluble fraction of methanol extract of Morus alba roots against a rat model of chronic stress (CS).

Materials and Methods:

Rats were exposed to stress procedure for 21 days. The stress procedure was mild, unpredictable footshock, administered for 1 h once daily for 21 days. Rats were administered with the ethyl acetate soluble fraction of methanol extract of M. alba roots (25, 50 and 100 mg/kg p.o) 1 h before footshock for 21 days and behavioral parameters were evaluated for cognitive dysfunction and depression using elevated plus maze and despair swim test, respectively. On day 21, rats were sacrificed immediately after stress and blood was collected for biochemical estimation. The adrenal gland and spleen were dissected for organ weight and the stomach was dissected for ulcer score.

Results:

CS significantly induced cognitive deficit, mental depression and hyperglycemia and increased blood corticosterone levels, gastric ulcerations and adrenal gland weight, but decreased the splenic weight. Pre-treatments with the ethyl acetate soluble fraction of methanol extract of M. alba roots (25, 50 and 100 mg/kg, p.o.) significantly attenuated the CS-induced perturbations. Diazepam (1 mg/kg, p.o.) was used as the standard antistress drug.

Conclusion:

The results indicate that M. alba possesses significant adaptogenic activity, indicating its possible clinical utility as an antistress agent.  相似文献   

20.

Objective:

algae isolates obtained from fresh and marine resources could be one of the richest sources of novel bioactive secondary metabolites expected to have pharmaceutical significance for new drug development. This study was conducted to evaluate the antiangiogenic and antiproliferative activity of Chlorella pyrenoidosa in experimental models of angiogenesis and by MTT assay.

Materials and Methods:

lyophilized extract of C. pyrenoidosa was extracted using dichloromethane/methanol (2:1), concentrated and vacuum evaporated to obtain the dried extract. The crude extract was evaluated in the vascular endothelial growth factor (VEGF)-induced angiogenesis in in ovo chick chorioallantoic membrane assay (CAM) at various concentrations (n = 8) using thalidomide and normal saline as positive and untreated control groups, respectively. The crude extract was also subjected to the antiangiogenic activity in the silver nitrate/potassium nitrate cautery model of corneal neovascularization (CN) in rats where topical bevacizumab was used as a positive control. The vasculature was photographed and blood vessel density was quantified using Aphelion imaging software. The extract was also evaluated for its anti proliferative activity by microculture tetrazolium test (MTT) assay using HeLa cancer cell line (ATCC).

Results:

VEGF increased the blood vessel density by 220% as compared to normal and thalidomide treatment decreased it to 67.2% in in ovo assay. In the in-vivo CN model, the mean neovascular density in the control group, the C. pyrenoidosa extract and bevacizumab group were found to be 100%, 59.02%, and 32.20%, respectively. The Chlorella pyrenoidosa extract negatively affected the viability of HeLa cells. An IC50 value of the extract was 570 μg/ml, respectively.

Conclusion:

a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity by MTT assay. In this study, it could be attributed that the activity may be due to the presence of secondary metabolites in the C. pyrenoidosa extract.KEY WORDS: Algae, angiogenesis, chorioallantoic membrane, corneal neovascularization, vascular endothelial growth factor  相似文献   

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