Nigella sativa modulates splenocyte proliferation, Th1/Th2 cytokine profile, macrophage function and NK anti-tumor activity

Aim of the study

Nigella sativa, also known as blackseed, has long been used in traditional medicine for treating various conditions related to the respiratory and gastrointestinal systems as well as different types of cancers. In this study, the potential immunomodulatory effects of Nigella sativa are investigated in light of splenocyte proliferation, macrophage function, and NK anti-tumor activity using BLAB/c and C57/BL6 primary cells.

Materials and methods

Splenocyte proliferation was assessed by [³H]-thymidine incorporation. Griess assay was performed to evaluate NO production by macrophages. ELISA was performed to measure the level of cytokines secreted by splenocytes and macrophages. NK cytotoxic activity against YAC-1 tumor cells was examined by JAM assay.

Results

We demonstrate that the aqueous extract of Nigella sativa significantly enhances splenocyte proliferation in a dose-responsive manner. In addition, the aqueous extract of Nigella sativa favors the secretion of Th2, versus Th1, cytokines by splenocytes. The secretion of IL-6, TNFα, and NO; key pro-inflammatory mediators, by primary macrophages is significantly suppressed by the aqueous extract of Nigella sativa, indicating that Nigella sativa exerts anti-inflammatory effects in vitro. Finally, experimental evidence indicates that the aqueous extract of Nigella sativa significantly enhances NK cytotoxic activity against YAC-1 tumor cells, suggesting that the documented anti-tumor effects of Nigella sativa may be, at least in part, attributed to its ability to serve as a stimulant of NK anti-tumor activity.

Conclusions

Our data present Nigella sativa as a traditionally used herb with potent immunomodulatory, anti-inflammatory, and anti-tumor effects. We anticipate that Nigella sativa ingredients may be employed as effective therapeutic agents in the regulation of diverse immune reactions implicated in various conditions and diseases such as cancer.     

Sida rhomboidea.Roxb leaf extract ameliorates gentamicin induced nephrotoxicity and renal dysfunction in rats

Ethnopharmacological relevance

Sida rhomboidea.Roxb (SR) known as “Mahabala” in Ayurveda and marketed as “Shahadeyi” is used in ethnomedicine to treat ailments such as dysuria and urinary disorders.

Aim of the study

To evaluate nephroprotective potential of SR against gentamicin (GM) induced nephrotoxicity and renal dysfunction.

Materials and methods

Nephrotoxicity was induced in rats with GM (100 mg/kg bodyweight (i.p.) for 8 days) and were treated with SR extract (200 and 400 mg/kg bodyweight (p.o.) for 8 days) or 0.5% carboxymethyl cellulose (vehicle). Plasma and urine urea and creatinine, renal enzymatic and non-enzymatic antioxidants along with lipid peroxidation were evaluated in various experimental groups.

Results

GM treatment induced significant elevation (p < 0.05) in plasma and urine urea, creatinine, renal lipid peroxidation along with significant decrement (p < 0.05) in renal enzymatic and non-enzymatic antioxidants. SR treatment to GM treated rats (GM + SR) recorded significant decrement (p < 0.05) in plasma and urine urea and creatinine, renal lipid peroxidation along with significant increment (p < 0.05) in renal enzymatic and non-enzymatic antioxidants.

Conclusion

SR leaf extract ameliorates GM induced nephrotoxicity and renal dysfunction and thus validates its ethnomedicinal use.     

Antiulcerogenic activity of Lantana camara leaves on gastric and duodenal ulcers in experimental rats

Ethnopharmacological relevance

Lantana camara L. (Verbenaceae), a widely growing shrub has been used in the traditional medicine for treating many ailments. The objective of the present study was to evaluate the effects of methanolic extract of Lantana camara leaves on gastric and duodenal ulcers.

Materials and methods

The antiulcerogenic effect of methanolic extract of Lantana camara was evaluated in aspirin induced gastric ulcerogenesis in pyloric ligated rats, ethanol induced gastric ulcer, and cysteamine induced duodenal ulcer models. The extract was administered orally at two different doses of 250 mg/kg and 500 mg/kg. The lipid peroxidation, reduced glutathione levels of ethanol induced gastric ulcer model and inhibition zone in diameter against Helicobacter pylori also determined.

Results

The L. camara extract significantly (P < 0.01) reduced ulcer index, total acidity and significantly (P < 0.01) increased the gastric pH of aspirin + pylorus-ligation induced ulcerogenesis and ethanol induced gastric ulcer models. The extract also significantly (P < 0.01) reduced the ulcer index of cysteamine induced duodenal ulcer. The L. camara showed significant (P < 0.01) reduction in lipid peroxidation and increase in reduced glutathione levels. The inhibition zone in diameter of extract against H. pylori was 20 mm.

Conclusion

The methanolic extract of Lantana camara leaves shown healing of gastric ulcers and also prevents development of duodenal ulcers in rats.     

Nigella sativa inhibits intestinal glucose absorption and improves glucose tolerance in rats

Aim of the study

Nigella sativa L. (Ranunculaceae) seeds have been used traditionally for centuries, notably for treating diabetes.

Materials and methods

We studied the effects of the crude aqueous extract of Nigella sativa seeds on intestinal glucose absorption in vitro using a short-circuit current technique and in vivo using an oral glucose tolerance test.

Results

The aqueous extract of Nigella sativa (0.1 pg/ml to 100 ng/ml) exerted dose-dependent inhibition of sodium-dependent glucose transport across isolated rat jejunum. Maximal inhibition exceeded 80% and IC₅₀ was close to 10 pg/ml. An oral glucose tolerance test was carried out in rats after the initial dose and after a 6-week treatment of Nigella sativa (2 g/(kg day)), and compared to metformin (300 mg/(kg day)). Chronic Nigella sativa treatment improved glucose tolerance as efficiently as metformin. Nigella sativa and metformin also reduced body weight without any toxic effect.

Conclusions

To our knowledge, this is the first demonstration that Nigella sativa directly inhibits the electrogenic intestinal absorption of glucose in vitro. Together with the observed improvement of glucose tolerance and body weight in rats after chronic oral administration in vivo, these effects further validate the traditional use of Nigella sativa seeds against diabetes.     

Ginseng total saponins enhance neurogenesis after focal cerebral ischemia

Ethnopharmacological relevance

Ginseng, the root of Panax ginseng C.A. Meyer, is one of the most commonly used healing herbs for stroke and chronic debilitating conditions in China. Ginsenosides are the main active principles for ginseng's efficacy, but the mechanisms have not been fully clarified.

Aim of the study

To test the hypothesis whether or not the administration of Ginseng total saponins (GTS) can enhance neurogenesis after focal cerebral ischemia, and thereby improve neurological deficits.

Materials and methods

Male Wistar rats received intraperitoneal injections of GTS dissolved at a dose of 25 mg kg⁻¹ d⁻¹ or normal saline (NS) of same volume 3 days before the permanent middle cerebral artery occlusion (MCAO) model establishment until the animals were killed at the time points of 1 d, 3 d, 7 d and 14 d. The neurological function was assessed blindly. BrdU immunostaining and double staining were performed by following the 3-steps method.

Results

(A) GTS-treated rats have better neurological scores compared with those in NS group at 14 d time point (p < 0.05); (B) the number of BrdU⁺ cells and BrdU⁺/NeuN⁺ cells in GTS group were significantly higher than those in NS group in the ipsilateral subventricular zone and in the ipsilateral infarct area after MCAO, respectively (p < 0.05 or p < 0.01); (C) the increase of the number of BrdU⁺/NeuN⁺ cells highly correlated with the decrease of neurological scores. Coefficient correlation r = −0.828 (p < 0.01).

Conclusion

GTS can improve neurological deficits after focal cerebral ischemia by inducing endogenous neural stem cells activation and thereby enhance adult central nervous system regeneration.     

Effects of Scutellariae radix and Aloe vera gel extracts on immunoglobulin E and cytokine levels in atopic dermatitis NC/Nga mice

Aim of the study

The present study aimed to investigate the effects of Scutellariae radix (SR) and Aloe vera gel (AV), alone or in combination, on levels of immunoglobulin E (IgE) and inflammatory cytokines in spontaneous atopic dermatitis(AD)-like skin lesions.

Materials and methods

After spontaneous AD-like skin lesion was developed by adaptation to conventional conditions, mice were randomly assigned to control, SR (50 mg/kg, p.o.), AV (0.8 mg/kg, p.o.) and SRAV (50 mg of SR and 0.8 mg of AV/kg, p.o.) groups, and were treated for 6 weeks.

Results

SR and SRAV suppressed IL-5 levels compared with control, but had no effects on IgE levels (P < 0.05). AV increased IgE levels, but decreased both IL-5 and IL-10 compared with control (P < 0.05).

Conclusion

These results suggest that SR and AV modulate immunological responses in AD, mainly through influencing IL-5 or IL-10 levels.     

Screening of Caesalpinia bonduc leaves for antipsoriatic activity

Ethnopharmacological relevance

Leaves of Caesalpinia bonduc (L.) Roxb. (Caesalpiniaceae) have been used by traditional Siddha healer of Malabar region for psoriasis treatment.

Aim of the study

To evaluate the Caesalpinia bonduc decoction (CBD), Caesalpinia bonduc hydroalcoholic extract (CBHA) for antipsoriatic activity.

Materials and methods

Mouse tail test for psoriasis was used for the evaluation of antipsoriatic activity. Extracts were tested at a dose of 500 mg/kg b.w. and fractions at 250 mg/kg b.w. in Swiss albino mice. Parameters studied in the mouse tail test were changes in epidermal thickness and percentage orthokeratotic values. In vitro antiproliferant assay on HaCaT cell lines and in vitro lipoxygenase inhibition were also carried out.

Results

Butanol fraction of Caesalpinia bonduc hydroalcoholic extract (CBHAB) and water fraction of Caesalpinia bonduc hydroalcoholic extract (CBHAW) produced significant orthokeratosis (p < 0.001). In relative epidermal thickness, a significant (p < 0.05) reduction with respect to control was observed in groups treated with retinoic acid, CBD, butanol fraction of Caesalpinia bonduc decoction (CBDB), water fraction of Caesalpinia bonduc hydroalcoholic extract (CBHAW). Maximum antiproliferant activity was shown by CBHA (IC₅₀, 77.5 ± 12.7 μg/ml). In lipoxygenase inhibition assay, water fraction of Caesalpinia bonduc decoction (CBDW) showed maximum activity with an IC₅₀ value of 164.71 ± 4.57 μg/ml.

Conclusions

Among all the tested samples only CBHAW showed good activity in the mouse tail test, antiproliferant activity in HaCaT cells and lipoxygenase inhibition assay. Other extracts and fractions showed varying degrees of activity. The present study supports the traditional use of Caesalpinia bonduc leaves for psoriasis treatment.     

Cytochrome P450 inhibitory potential of Triphala--a Rasayana from Ayurveda

Ethnopharmacological relevance

‘Triphala’ is one of the age-old, most commonly used polyherbal preparation from Ayurveda as Rasayana drug.

Aim of the study

This study was aimed at evaluating the effect of ‘Triphala’ on drug modulating enzymes to assess its safety through its potential to interact with co-administered drugs.

Materials and methods

The cytochrome P450 inhibitory effect of ‘triphala’ formulation was investigated on rat liver microsomes using CYP450-CO complex assay and on individual isoform such as CYP3A4 and 2D6 using fluorescence screening. RP-HPLC method was developed to standardize ‘triphala’ and its individual components using gallic acid as analytical marker compound.

Results

RP-HPLC analysis demonstrated the presence of gallic acid (4.30 ± 2.09 mg/g) in the formulation. The formulation showed 23% inhibition of the rat liver microsomes through CYP450-CO complex assay which is comparatively less when compared with the individual components. Further, the effect of standardized formulation dissolved in ethanol showed CYP3A4 and CYP2D6 inhibitory activity at the IC₅₀ values of 119.65 ± 1.91 μg/ml and 105.03 ± 0.98 μg/ml respectively. Gallic acid was also found to inhibit both the isoforms at the IC₅₀ values of 87.24 ± 1.11 μg/ml and 92.03 ± 0.38 μg/ml respectively.

Conclusions

Various concentrations of the formulation and its individual components showed significantly less inhibitory activity (p < 0.001) on individual isoforms when compared with the positive control. Assessment on the in vitro effect of ‘triphala’ on drug modulating enzymes has important implications for predicting the likelihood of herb-drug interactions if these are administered concomitantly.     

Hypoglycemic effect of a leaf extract of Pseuderanthemum palatiferum (Nees) Radlk. in normal and streptozotocin-induced diabetic rats

Ethnopharmacological relevance

Pseuderanthemum palatiferum (Nees) Radlk (Acanthaceae) was first found in Northern Vietnam and expanded throughout the country including the Mekong Delta region. The leaves of this plant are recommended in folk medicine of Vietnam and Thailand for promoting and treating various diseases including hypertension, diarrhea, arthritis, hemorrhoids, stomachache, tumors, colitis, bleeding, wounds, constipation, flu, colon cancer, nephritis, and diabetes.

Aim of the study

The hypoglycemic effect of an 80% ethanolic leaf extract from the leaves of Pseuderanthemum palatiferum (PPE) was investigated in normal and streptozotocin (STZ)-induced diabetic rats.

Materials and methods

The PPE was administered daily and orally to the rats at the doses of 250, 500, and 1000 mg/kg body weight (b.w.) for 14 days. The levels of fasting plasma glucose (FPG), serum insulin, and biochemical data such as blood urea nitrogen (BUN), triglycerides (TG), total cholesterol (TC), high-density lipoprotein (HDL), low-density lipoprotein (LDL), and alkaline phosphatase (ALP) were evaluated. The hypoglycemic effect of PPE was compared to that of the known anti-diabetic drug glibenclamide (0.25 mg/kg b.w.).

Results

FPG and serum insulin in normal rats were not significantly different from the control and test groups in all dosages. The treated diabetic rats which had received PPE and glibenclamide showed significantly (p < 0.05) decreased FPG and increased serum insulin levels at the end of the experiment. The hypoglycemic effect of PPE at the dose of 250 mg/kg b.w. was significantly (p < 0.05) more effective than that of glibenclamide. The serum insulin in PPE fed diabetic rats at the dose of 250 mg/kg b.w. was not different from those which had received glibenclamide, and this dose was significantly (p < 0.05) more effective than PPE at the doses of 500 and 1000 mg/kg b.w. while PPE increased HDL and decreased TC, TG, LDL, BUN and ALP in the diabetic rats.

Conclusions

PPE has a beneficial effect in hyperglycemic rats and may prevent the complication of diabetes.     

Evaluation of anticancer activity of ethanol extract of Sesbania grandiflora (Agati Sesban) against Ehrlich ascites carcinoma in Swiss albino mice

Ethno pharmacological relevance

The plant Sesbania grandiflora (Fabaceae) is commonly known as “Sesbania” and “agathi” in ayurvedic system of medicine and reputed in the indigenous medicine in India. It is also known as “Agati Sesban” or “humming bird tree” in English. All parts of this unique plant are useful and have a wide spectrum of medicinal properties. The plant has various uses in folk and traditional medicines for headache, swellings, anemia, bronchitis, pains, liver disorders and tumors.

Aim of the study

The objective of the present study was to explore the anticancer activity of the ethanol extract of Sesbania grandiflora against Ehrlich ascites carcinoma (EAC)-bearing Swiss albino mice.

Materials and methods

Anticancer activity of ethanol extract of Sesbania grandiflora (EESG) of both leaves and flowers were evaluated in Swiss albino mice against Ehrlich Ascites Carcinoma (EAC) cell line at the doses of 100 and 200 mg/kg body weight intraperitoneally. The extracts were administered for 14 consecutive days. Twenty-four hours of last dose and 18 h of fasting, the mice were sacrificed and the anticancer effect of EESG was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters and biochemical parameters of EAC bearing host.

Results

Sesbania grandiflora extracts showed significant decrease in (p < 0.01) tumor volume, viable cell count, tumor weight and elevated the life span of EAC bearing mice. Hematological profile such as RBC, hemoglobin and lymphocyte count reverted to normal level in EESG treated mice. The extracts significantly (p < 0.05) decreased the levels of lipid peroxidation and significantly (p < 0.05) increased the levels of GSH, SOD and CAT.

Conclusion

The results showed that the ethanol extract of Sesbania grandiflora was effective in inhibiting the tumor growth in ascitic models and that is comparable to 5-Fluorouracil.     

Protective effects of Polygonatum sibiricum polysaccharide on ovariectomy-induced bone loss in rats

Ethnopharmacological relevance

To assess the ability of traditional Chinese medicine Polygonatum sibiricum polysaccharide to prevent bone loss in the ovariectomized rat.

Materials and methods

PSP was administered intragastrically to the rats. After 35 days, the total body bone mineral density (BMD) was assessed in all of the rats. All sections were processed for immunohistochemistry and hematoxylin-eosin staining (H.E.).

Results

BMD was lower in the ovariectomized group (OVX, 0.163 g/cm²), the group that received a moderate dose of PSP on OVX animals (OVX + MP, 0.163 g/cm²) and the group that received a low dose of PSP on OVX animals (OVX + LP, 0.162 g/cm²) than in the sham-operated group (SHAM, 0.180 g/cm²), the OVX + E₂ group (OVX + E₂, 0.176 g/cm²) and the group that received a high dose of PSP on OVX animals (OVX + HP, 0.174 g/cm²) (P < 0.05). Clear arrangements of bone trabeculae were observed in the OVX + E₂ and OVX + HP. The expression of bone morphogenetic proteins (BMP) and basic fibroblast growth factor (bFGF) in the OVX, OVX + MP and OVX + LP was down regulated compared to the SHAM, OVX + E₂ and OVX + HP (P < 0.05). The rats in the OVX + E₂ and OVX + HP had lower levels of bone Gla protein (BGP), bone alkaline phosphatase (BALP), tartrate-resistant acid phosphatase (TRAP) and tumor necrosis factor α(TNF-α) expression than the rats in the OVX, OVX + MP and OVX + LP (P < 0.05).

Conclusion

This experiment demonstrates that the administration of PSP to ovariectomized rats reverses bone loss and prevents osteoporosis.     

Anti-inflammatory activity of Terminalia paniculata bark extract against acute and chronic inflammation in rats

Ethnopharmacological relevance

Terminalia paniculata Roxb. (Family-Combretaceae) is a wild tree commonly used in traditional ayurvedic medicine for the treatment of inflammation of parotid glands and in menstrual disorders.

Aim of the study

To explore the folk use of Terminalia paniculata on pharmacological grounds to evaluate the scientific basis of anti-inflammatory activity.

Materials and methods

The anti-inflammatory activity of Terminalia paniculata was studied against carrageenan-induced hind paw edema, air pouch inflammation and complete Freund's adjuvant (CFA)-induced arthritis in rats. The aqueous extract of Terminalia paniculata bark (TPW) was administered at the concentrations of 100, 200 and 400 mg/kg body weight.

Results

TPW showed significant (p < 0.05) anti-inflammatory activity by reducing the edema volume in carrageenan-induced paw edema in rats. Further, TPW (400 mg/kg) also reduced the carrageenan-induced leukocyte migration (50.92 ± 5.71%) and myeloperoxidase activity (49.31 ± 5.24%) in air pouch exudates. TPW (200 mg/kg) exhibits anti-rheumatic and analgesic activities by improving the altered haematological milieu (ESR, CRP, RF, WBC, RBC and Hb) and also by inhibiting the flexion scores and radiographic changes in CFA-induced arthritis. This extract also had significant (p < 0.05) effects on the occurrence of secondary lesions compared to CFA control.

Conclusions

Terminalia paniculata bark may be a potential preventive or therapeutic candidate for the treatment of chronic inflammation and arthritis.     

Gastroprotective effect of standardized leaf extract from Argyreia speciosa on experimental gastric ulcers in rats

Ethnopharmacological relevance

Argyreia speciosa (L.f), Sweet (Family Convolvulaceae) is used traditionally in Indian System of Medicine as aphrodisiac, rejuvenating agent, intellect promoting agent, brain tonic and in the therapy of hepatomegaly, diabetes and chronic ulcer.

Aim of the study

To study the gastroprotective effect of standardized butanol fraction of Argyreia speciosa leaf (ASE).

Materials and methods

The butanol fraction of Argyreia speciosa leaf (ASE; 50, 100 and 200 mg/kg body weight) was administered orally, twice daily for 5 days for prevention from Aspirin (ASP)-, ethanol (EtOH)-, cold-restraint stress (CRS) - and pylorus ligation (PL)-induced ulcers. Estimation of antioxidant enzymes activity was carried out in CRS-induced ulcer model, and various gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PL-induced ulcer model.

Result

ASE showed dose-dependent ulcer protective effect in ASP 23.64-58.76% (p < 0.01 to p < 0.001), EtOH 15.45-58.45% (p < 0.001), CRS 19.39-78.36% (p < 0.001) and PL 19.67-69.04% (p < 0.05 to p < 0.01), respectively. The percentage of protection by standard drug ranitidine was 77.77-84.32% (p < 0.01 to p < 0.001) in various gastric ulcer models. The gastric wall mucus was significantly (p < 0.001) enhanced by ASE and is regarded as the first line of defence against EtOH-induced gastric ulcers showing cytoprotective property. ASE showed a marginal decrease in volume, acid pepsin concentration and acid pepsin output. However, ASE reduced the ulcer index with significant decrease in LPO level (p < 0.001), and SOD level (p < 0.01 to p < 0.001) as compared with CRS-induced group. A gradual and significant increase in CAT values were observed at 100 and 200 mg/kg dose levels (p < 0.01 to p < 0.001).

Conclusions

The results of our study revealed that Argyreia speciosa possess significant dose dependent gastroprotective activity, probably due to its free radical scavenging activity.     

Anti-inflammatory effect of a methanolic extract of leaves of Dregea volubilis

Aim of study

The aim of this study was to establish the anti-inflammatory activity of the methanolic extract of Dregea volubilis leaves (MEDV) with its fractions and to delineate the possible mechanism of action for MEDV.

Materials and methods

The anti-inflammatory activities of MEDV along with its petroleum ether and chloroform fractions were evaluated in a carrageenan induced model of acute inflammation. The effect of MEDV on lipopolysaccharide induced production of nitric oxide (NO) in macrophages was also studied.

Results

MEDV (100, 200 and 400 mg/kg body weight) significantly reduced carrageenan induced paw edema; chloroform fraction was most potent (66%, p < 0.001). MEDV was non-toxic up to 125 μg/ml in mouse peritoneal macrophages wherein it (0-100 μg/ml) reduced lipopolysaccharide induced NO production.

Conclusion

MEDV possesses significant anti-inflammatory activity. Chloroform fraction of MEDV showed best anti-inflammatory activity.     

Optimized project of traditional Chinese medicine in treating chronic kidney disease stage 3: a multicenter double-blinded randomized controlled trial

Ethnopharmacological relevance

Stage 3 is the key phase of chronic kidney disease. Traditional Chinese medicine (TCM) has been used for the treatment of chronic kidney disease. But a large sample trial is desirable.

Materials and methods

A total of 578 Chinese patients with primary glomerulonephritis in CKD stage 3 were randomly assigned to three groups: patients received TCM (TCM group), benazepril (Ben group), TCM combined with benazepril (TCM + Ben group). Patients were followed up for 24 weeks. The primary endpoint was the time to the composite of 50% increased of serum creatinine, end stage renal disease or death.

Results

eGFR in the TCM and the TCM + Ben group were improved (week 24 vs. baseline, P < 0.05) while eGFR in the Ben group was decreased (week 24 vs. baseline, P > 0.05). 24 h urinary protein excretion (UP) and urinary albumin/creatinine (UAlb/Cr) were decreased in the TCM + Ben (week 24 vs. baseline, P < 0.05) and the Ben group (week 24 vs. baseline, P > 0.05). UP and UAlb/Cr were increased in the TCM group to week 12, then were stable (week 24 vs. baseline, P < 0.05). The hemoglobin in the TCM group was also improved (week 24 vs. baseline, P < 0.05). The accumulative survival rate in the TCM + Ben group was higher than that in the TCM group and the Ben group (P = 0.044). Side effects in the TCM group were the lowest in these groups (P < 0.05). The patients with dry cough in the TCM + Ben group and the Ben group were increased as compared with the TCM group (P < 0.05). Hyperkalemia happened less frequently in the TCM group as compared with the other two groups (P = 0.052).

Conclusions

For the patients with CKD stage 3, TCM can improve eGFR and hemoglobin with lower side effects. Benazepril significantly decreased the proteinuria. Chinese medicine integrated with benazepril can ameliorate renal function and decrease proteinuria synergistically.     

Exploring Tagetes erecta Linn flower for the elastase, hyaluronidase and MMP-1 inhibitory activity

Ethnopharmacological relevance

Traditionally Tagetes erecta Linn flower is claimed to treat skin diseases like sores, burns, wounds, ulcers, eczema and several other skin ailments. The aim of the present experiment was to evaluate the anti-wrinkle potential of standardized flower extract of Tagetes erecta.

Materials and methods

The Tagetes erecta extract and fractions were screened for hyaluronidase, elastase and matrix metalloproteinase (MMP-1) inhibitory activity compared with the activity of standard oleanolic acid. Syringic acid and β-amyrin were obtained from the extract and quantified through RP-HPLC. Also the compounds were evaluated for anti-wrinkle activity.

Results

The methanol extract showed significant (^aP < 0.05) hyaluronidase and elastase inhibition with IC50 of 11.70 ± 1.79 μg mL⁻¹ and 4.13 ± 0.93 μg mL⁻¹ respectively and better MMP-1 inhibition compared to standard oleanolic acid. The isolated compounds syringic acid and β-amyrin found to inhibit enzymes comparable to oleanolic acid. The RP-HPLC analysis revealed that good amounts of syringic acid and β-amyrin (2.30%, w/w and 0.06%) are present in Tagetes erecta.

Conclusion

Tagetes erecta flower showed effective inhibition of hyaluronidase, elastase and MMP-1. Therefore, this experiment further rationalizes the traditional uses of this plant, which may be useful as an anti-wrinkle agent.     

Modulation of inflammatory markers by the ethanolic extract of Leucas aspera in adjuvant arthritis

Aim of the study

To investigate the anti-inflammatory and antioxidant potential of ethanolic extract of Leucas aspera (EELA) in adjuvant arthritis.

Materials and methods

Complete Freund's adjuvant served to induce arthritis. EELA was administered in two doses along with vehicle control (0.1% carboxymethyl cellulose) and positive control (Diclofenac). Levels of tumour necrosis factor (TNF-)-α, C-reactive protein (CRP), Interleukin-2 (IL-2), Cathepsin D, activities of antioxidant enzymes superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) were estimated in plasma/hemolysate and tissue. HPLC analysis of EELA was also performed.

Results

EELA exhibited significant anti-inflammatory (p < 0.001) and antioxidant activity (p < 0.001). It did not show mortality up to 2000 mg/kg body weight. Histopathological studies confirmed complete cartilage regeneration and near normal joint in EELA2 treated arthritic rats.

Conclusion

This study highlighted the antioxidant and anti-inflammatory potential of Leucas aspera. Three major families of compounds present in EELA may explain these activities: catechins (epicatechin, beta epicatechin), flavonoids (procyanidin), phytosterols (beta-sitosterol) apart from glycosides, phenolic compounds and tannins.     

Treatment of high fat diet induced type 2 diabetes in C57BL/6J mice by two medicinal plants used in traditional treatment of diabetes in the east of Algeria

Aim of the study

Hydro-alcoholic extracts of Centaurium erythraea Rafn (CE), Gentianaceae and Artemisia herba-alba Asso (AHA), Asteraceae, medicinal plants used in traditional treatment of diabetes in north-eastern Algeria, were tested in established type 2 diabetes induced with a standardized high fat diet (HFD) in mice.

Materials and methods

After confirmation of diabetes (17th week), plant extracts were administered orally by gavage at a dose of 2 g/kg daily for 18 weeks to male C57BL/6J mice fed HFD. Animals were weighed, food intake and plasma glucose measured weekly, insulin and lipid profile at study end.

Results

At 35 weeks, groups treated with AHA or CE vs. HFD control had a significant reduction in mean (±SD) fasting blood glucose concentrations (143.8 ± 23.9 and 139.5 ± 14.2 vs. 229.0 ± 20.8 mg/dL, p < 0.05, respectively), triglyceride (18.9 ± 11.1 and 16.0 ± 6.5 vs. 62.8 ± 18.3 mg/dL, p < 0.05), total cholesterol (1.2 ± 0.1 and 1.2 ± 0.3 vs. 1.8 ± 1.1 g/L, p < 0.05) and serum insulin concentrations (1.7 ± 0.7 and 0.9 ± 0.7 vs. 3.3 ± 14.3 ng/mL, p < 0.05). Plant extracts also markedly reduced insulin resistance as compared to HFD controls (AHA: 15.6 ± 9.1, CE: 9.0 ± 7.7 vs. HFD control 38.5 ± 30.3, p < 0.05). The plant extracts decreased calorie intake and had little effect on body weight or HDL-cholesterol.

Conclusion

AHA has already been shown to have a antihyperglycaemic and antihyperlipidemic effect but this is the first demonstration of an effect of AHA and CE on established HFD-induced diabetes.     

Subchronic administration of Catha edulis F. (khat) extract is marked by elevation of cardiac biomarkers and subendocardial necrosis besides blood pressure alteration in rats

Ethnpharmacological relevance

Khat is a widely chewed herb for its stimulant effect, however, its effects on the cardiovascular system are a source of growing concern, as prevalence of chewing is increasing and susceptible individuals may experience cardiovascular episodes. This study attempted to evaluate cardiovascular substrates that predispose individuals to these episodes by using both biochemical and morphologic-pathologic studies.

Materials and methods

Rats were treated with either Tween 80 (2% in distilled water) (CON), or khat extract (100 mg/kg, K100; 200 mg/kg, K200; or 400 mg/kg, K400 doses) orally for 6 weeks. Blood pressure (BP) in each group was measured before dosing and 1, 2 and 3 h after-dose as well as weekly for 6 weeks using Tail cuff method. On day 45, blood was drawn for assessment of cardiac biomarkers and animals were sacrificed, and histological examination was undertaken for any overt damage on the myocardium.

Results

K400 was the only dose that significantly increased BP at 2 (p < 0.05) and 3 h (p < 0.001) postdose compared to predose level. Likewise, the 3 h postdose BP of each week was significantly greater (p < 0.001) than baseline BP only at 400 mg/kg. However, when the weekly values were compared among themselves, the difference was not statistically significant and a progressive change in postdose BP had not been observed. On the other hand, predose systolic BP of K400 rats tended to decline at week 3 and significantly decreased (p < 0.05) beyond week 4 compared to baseline values, but the decline was not significant for the rest of the doses. Biomarker assessments revealed that whereas levels of total creatine kinase were found to be elevated significantly for K100 (p < 0.05), K200 and K400 (p < 0.001 in both cases); aspartate aminotransferease was increased in K200 (p < 0.01) and K400 (p < 0.001) compared to CON rats. By contrast, levels of cardiac troponin T was significantly increased (p < 0.001) only in K400 rats. Heart tissues of CON and K100 rats were normal, while those from K200 showed signs of focal lesions but normal architecture of the myocardium was maintained. K400 rats, however, displayed fragmentation and segmentation of fibers, edema and mottled staining.

Conclusions

These findings collectively indicate that the high dose of crude khat extract modulated most of the hemodynamic, biochemical and histopathological parameters in rats and hence chronic use of khat at higher dose and for longer sessions bear a significant risk for cardiovascular morbidities.