Anti-inflammatory evaluation of Coronopus didymus in the pleurisy and paw oedema models in mice

Ethnopharmacological relevance

Mastrunço (Coronopus didymus – CD) is currently considered as a medicinal specie often used in Brazil, especially in southeast region, for the treatment of several diseases in which pain and inflammation are common. Treatment with the plant can be done by infusion, decoction, or through food. The aim of this study was: to investigate the anti-inflammatory effect of hydroalcoholic extract obtained from the leaves of CD following the traditional procedure.

Materials and methods

The anti-inflammatory activity was determined using mouse of pleurisy and paw oedema models, both process being induced by different flogistic agents such as: carrageenan (Cg), bradykinin (BK), histamine (HIS), substance P (SP), dextran (DEX) or prostaglandin E₂ (PGE₂). We evaluated the effect of CD (200–600 mg/kg) administered by oral route (p.o.) upon leukocytes migration, myeloperoxidase (MPO), and adenosine-deaminase (ADA) activities and nitric oxide (NO) levels.

Results

CD (200–600 mg/kg) inhibited the leukocytes by 60.0 ± 1.42%, neutrophils by 82.75 ± 1.29%, MPO by 42.30 ± 4.23%, and ADA activities by 57.89 ± 1.94%, as well as NO levels by 64.28 ± 2.15% in Cg induced pleurisy. CD also inhibited total and differential leukocytes in the pleurisy induced by BK (1.30 ± 0.11/0.29 ± 0.02), HIS (1.20 ± 0.09/0.42 ± 0.05) and SP (0.74 ± 0.06/0.14 ± 0.01). In addition, CD was effective in reducing paw oedema induced by Cg by 72.79 ± 1.13%, SP by 68.26. ± 0.78%, BK by 66.66. ± 0.77%, PGE₂ by 53.346. ± 1.18 and DEX by 65.14 ± 2.35%.

Conclusion

Several mechanisms, including the inhibition of enzymes (MPO and ADA) and mediators (BK, HIS, SP, NO and PGE₂) release and/or action, appear to account for the anti-inflammatory effect of Coronopus didymus.     

Antispasmodic effects and composition of the essential oils from two South American chemotypes of Lippia alba

Ethopharmacology relevance

Lippia alba (Mill.) N. E. Brown (Verbenaceae) is an aromatic species used in Central and South America as eupeptic for indigestion. In Argentina, it is used by the “criollos” from the Chaco province. There are several chemotypes which differ in the chemical composition of the essential oils. Nowadays, it is experimentally cultivated in some countries of the region, including Argentina.

Aim of the study

To compare the chemical composition and pharmacology of the essential oils from two chemotypes: “citral” (CEO) and “linalool” (LEO), in isolated rat duodenum and ileum. Methods: Contractile concentration–response curves (CRC) of acetylcholine (ACh) and calcium in 40 mM K⁺-medium (Ca²⁺-CRC) were done in isolated intestine portions, in the absence and presence of CEO or LEO at different concentrations.

Results

Likewise verapamil, CEO and LEO induced a non-competitive inhibition of the ACh-CRC, with IC₅₀ of 7.0±0.3 mg CEO/mL and 37.2±4.2 mg LEO/mL. l-NAME, a NO-synthase blocker, increased the IC₅₀ of CEO to 26.1±8.7 mg CEO/mL. Likewise verapamil, CEO and LEO non-competitively inhibited the Ca²⁺-CRC, with IC₅₀ of 6.3±1.7 mg CEO/mL, 7.0±2.5 mg LEO/mL and 0.24±0.04 mg verapamil/mL (pIC₅₀: 6.28). CEO was proved to possess limonene, neral, geranial and (−)-carvone as the major components, while LEO was rich in linalool.

Conclusions

Results suggest that CEO has five times more potency than LEO to inhibit muscarinic contractions. The essential oils of both chemotypes interfered with the Ca²⁺-influx, but with an IC₅₀ about 28 times higher than that of verapamil. Moreover, CEO partially stimulated the NO production. These results show the medicinal usefulness of both Lippia alba chemotypes, thus validating its traditional use, potency and mechanism of action.     

Pharmacokinetic properties of hydroxysafflor yellow A in healthy Chinese female volunteers

Ethnopharmacological relevance

Hydroxysafflor yellow A (HSYA) was isolated from the dried flower of Carthamus tinctorius L. which was extensively used in traditional Chinese medicine to treat diseases due to blood stasis. However, there have been few detailed pharmacokinetic studies about HSYA on human beings.

Aim of the study

The aim was to investigate the pharmacokinetic characteristics of HSYA in healthy Chinese female volunteers.

Materials and methods

The volunteers were given intravenous infusion of single doses of safflor yellow injection (containing HSYA 35, 70 and 140 mg) in separate trial periods with 1 week washout period. The concentration levels of HSYA in plasma were determined with HPLC. Various pharmacokinetic parameters were estimated from the plasma concentration versus time data using non-compartmental methods.

Results

The C_max values were 2.02 ± 0.18, 7.47 ± 0.67 and 14.48 ± 4.71 μg/mL after the administration of single doses of 35, 70, and 140 mg of HSYA, respectively. The corresponding values of AUC_0–15h were 6.57 ± 1.20, 25.90 ± 4.62 and 48.47 ± 12.11 μg/(mL h⁻¹), and the values of t_1/2 were 3.21 ± 1.26, 3.33 ± 0.68 and 2.98 ± 0.09 h. The Student–Newman–Keuls test results showed that C_max and AUC_0–15h were both linearly related to dose.

Conclusions

In this study, the pharmacokinetic properties of HSYA are based on first-order kinetics over the dose range tested.     

Evaluation of the analgesic and anti-inflammatory effects of the essential oil of Lippia gracilis leaves

Aim of the study

The aim of the present study is to investigate the antinociceptive, anti-inflammatory, and antioxidant activities of essential oil (EO) of Lippia gracilis Schauer (Verbenaceae) leaves to support the medicinal uses claimed by folklore practitioners in the caatinga region (semi-arid) of Northeastern Brazil.

Materials and methods

The chemical composition and antinociceptive and anti-inflammatory activities of the EO of Lippia gracilis leaves (50–200 mg/kg) were investigated. Antinociceptive activity of the EO was evaluated by writhing test. Anti-inflammatory activity of the EO was evaluated using paw oedema and peritonitis methods.

Results

Oral treatment with the EO of Lippia gracilis leaves elicited inhibitory activity on acetic acid effect at 50, 100, and 200 mg/kg (30.33 ± 2.36, 25.20 ± 1.48, and 21.00 ± 1.54 abdominal writhes, respectively, P < 0.05), as compared with the control group (36.73 ± 1.92 writhes). The compound acetylsalicylic acid (ASA, 300 mg/kg) inhibited the acetic acid-induced writhing (12.67 ± 0.50 abdominal writhes, P < 0.001). Carrageenan-induced oedema formation was reduced with the EO of Lippia gracilis leaves at 200 mg/kg (0.72 ± 0.06 mL h, P < 0.001) and by the reference compound ASA (300 mg/kg, 0.85 ± 0.04 mL h, P < 0.001), as compared with the control group (1.76 ± 0.06 mL h). Leukocyte migration into the peritoneal cavity induced by carrageenan was reduced with the EO of Lippia gracilis leaves at 50, 100, and 200 mg/kg (13.81 ± 0.61, 11.77 ± 0.91, and 10.30 ± 0.60 leukocytes × 10⁶/mL, respectively, P < 0.01), and by the compound dexamethasone (2 mg/kg, 5.34 ± 0.33 leukocytes × 10⁶/mL, P < 0.001), as compared with the control group (16.71 ± 0.54 leukocytes × 10⁶/mL). The analyses of the essential oil allowed the identification of Lippia gracilis as a thymol-p-cymene chemotype (32.68% and 17.82%, respectively).

Conclusions

The EO of Lippia gracilis leaves shows antinociceptive and anti-inflammatory activities.     

Anti-inflammatory effects of YeongyoSeungma-tang

Ethnopharmacological relevance

YeongyoSeungma-tang which includes Fructus Forsythia, has been used in oriental traditional medicine for treatment of early smallpox and atopic dermatitis.

Aim of the study

YeongyoSeungma-tang was carried out to investigate for anti-inflammatory effects.

Materials and methods

YeongyoSeungma-tang was tested for anti-inflammatory effects against lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E₂ (PGE₂), and tumor necrosis factor alpha (TNF-α) releases as well as nuclear factor kappa B (NF-κB) expression using RAW264.7 macrophage cells.

Results

YeongyoSeungma-tang significantly inhibited generation of NO (42% and 59% inhibition at doses of 5 μg/mL and 10 μg/mL, respectively), PGE₂ (46% and 80% inhibition at doses of 5 μg/mL and 10 μg/mL, respectively) and TNF-α (6% and 23% inhibition at doses of 5 μg/mL and 10 μg/mL, respectively) on LPS-stimulated RAW 264.7 cells in a concentration-dependent manner. Consistently in these observations, the expression of inducible NO synthase (iNOS) enzyme was also inhibited by YeongyoSeungma-tang. However, YeongyoSeungma-tang did not show any influence on the expression of cyclooxygenase-2. The cream containing 0.075% YeongyoSeungma-tang showed good skin moisturizing effect without any irritation.

Conclusion

The present study may support the fact that YeongyoSeungma-tang can have the good possibility as an anti-inflammatory agent for troubled skins.     

Enhancement of oral moisture using tablets containing extract of Capparis masaikai Levl.

Aim of the study

This study was performed to examine the effects of tablets containing an extract of Capparis masaikai Levl. (M-tablets) on enhancing oral moisture.

Subjects and methods

The moistening effect of M-tablets was examined in 21 healthy subjects aged 25.1 ± 2.4 (mean ± S.D.) years in comparison with control tablets. After sucking tablets, the oral moisture was measured using a saliva wetness tester and a moisture checker. To evaluate the effects of the M-tablets on oral conditions, additional 50 subjects aged 30.6 ± 7.5 years were examined. The subjects recorded changes in refreshment, oral moisture, ease in speaking, and taste of water using a visual analog scale (VAS).

Results

The L-SALIVO^® value of the M-tablet increased significantly from 1.83 ± 0.17 (mean ± S.E.M.) at baseline to 3.02 ± 0.21 at 15 min (P < 0.01). The Mucus^® value of the M-tablet also increased from 37.50 ± 0.22 at baseline to 38.30 ± 0.26 at 15 min (P < 0.01). The VAS value for oral moisture increased significantly from 47.4 ± 2.0 to 69.6 ± 2.2 after taking the M-tablet (P < 0.01). The VAS value for taste of water also increased from 50.0 ± 1.1 to 66.7 ± 3.2 (P < 0.01).

Conclusion

These results suggest that M-tablets are useful for enhancing oral moisture, which leads to improvement of oral conditions.     

Passive opium smoking does not have beneficial effect on plasma lipids and cardiovascular indices in hypercholesterolemic rabbits with ischemic and non-ischemic hearts

Background

To scientifically test a traditionally belief of some Asian countries residents that opium may prevent or have ameliorating effects on cardiovascular diseases (CVD) we investigated the effect of passive opium smoking (POS) on plasma lipids and some cardiovascular parameters in hypercholesterolemic rabbits with ischemic and non-ischemic hearts.

Methods

40 rabbits were fed for 2 weeks with cholesterol-enriched diet and divided to control (CTL), short-term opium (SO) and long-term opium (LO) groups. SO and LO groups were exposed to POS for 3 days and 4 weeks respectively. ECG, blood pressure (BP) and left ventricular pressure recorded and serum lipid and cardiac troponin I levels were measured. Isoproterenol (ISO) injected for induction of cardiac ischemia and after 4 h the above variables were measured along with cardiac histopathology assessment.

Results

HDL cholesterol decreased significantly in LO compared to CTL group (35 ± 5 vs 53 ± 5 mg/dl). Groups treated with ISO showed significantly higher increments in troponin I level (P < 0.05) except for LO group and reduction of BP was higher in ISO and SO + ISO groups compared to CTL and SO groups respectively (−38 ± 6 vs −23 ± 4 and −37 ± 11 vs −11 ± 3 percent respectively, P < 0.05). Reduction in BP was significantly lower in LO + ISO compared to ISO group. Opium exposure caused a trend of increase in blood pressure, LDL cholesterol and ECG disturbances, attenuated ISO induced myonecrosis but augmented tissue congestion and hemorrhage.

Conclusion

POS can be considered as a CVD risk factor. Opium does not reduce BP or cholesterol level, as is anticipated by its users.     

Hypotensive and endothelium-independent vasorelaxant effects of methanolic extract from Curcuma longa L. in rats

Ethnopharmacological relevance

Curcuma longa L. (CL) is a yellow rhizome that is used in African traditional medicine to treat palpitation, hypertension or other related blood circulation disorders.

Aim of the study

To justify the use of CL in ethnomedicine, we investigated the vasorelaxant effect of methanolic extract of CL (CLME) and its underlying mechanisms in isolated rat mesenteric artery.

Materials and methods

The effect of CLME on the mean arterial pressure (MAP) and heart rate (HR) (pulse interval) were determined in vivo in non-anaesthetized rats. Superior mesenteric rings were isolated, suspended in organ baths containing Tyrode solution at 37 °C and gassed with 95% O₂ + 5% CO₂, under a resting tension of 0.75 g. The vasorelaxant effects of CLME were studied by means of isometric tension recording experiments.

Results

In normotensive rats, CLME (10, 20 and 30 mg/kg, i.v.) induced dose-dependent hypotension (2.0 ± 0.5%; 27.1 ± 5.0% and 26.7 ± 4.6%, respectively), and pronounced bradycardia (5.8 ± 1.2%, 19.3 ± 3.2% and 22.9 ± 4.6%, respectively). CLME (1–1000 μg/mL) induced concentration-dependent relaxation of tonic contractions evoked by phenylephrine (Phe) (10 μM) and KCl (80 mM) in rings with intact-endothelium (E_max = 82.3 ± 3.2% and 97.7 ± 0.7%) or denuded-endothelium (E_max = 91.4 ± 1.0% and 97.8 ± 1.1%). Also, in a depolarized, Ca²⁺ free medium, CLME inhibited CaCl₂ (1 μM–30 mM)-induced contractions and caused a concentration-dependent rightward shift of the response curves, indicating that CLME inhibited the contractile mechanisms involving extracellular Ca²⁺ influx. In addition, in Ca²⁺ free media containing EGTA (1 mM), CLME inhibited the transient contraction of denuded rings constricted with Phe, but not those evoked by caffeine (20 mM). In contrast, neither glibenclamide, BaCl₂, tetraethylammonium nor 4-aminopyridine affected CLME-induced relaxation.

Conclusions

These results demonstrate the hypotensive and bradycardic effects of CLME, as well as its potent vasodilation of rat mesenteric arteries. These effects, may in part, be due to the inhibition of extracellular Ca²⁺ influx and/or inhibition of intracellular Ca²⁺ mobilization from Phe-sensitive stores.     

MAO-A inhibitory activity of quercetin from Calluna vulgaris (L.) Hull.

Aim of the study

This study investigated MAO-A inhibitory activity of methanol extract of Calluna vulgaris (L.) Hull., which traditionally has been used as a nerve calming remedy.

Materials and methods

A methanolic extract of Calluna vulgaris was partitioned against heptane, ethyl acetate and water. The three fractions were tested in a photometric peroxidase linked MAO-A bioassay. The ethyl acetate phase showed the highest MAO-A inhibitory activity. Quercetin was isolated by VLC through bioassay-guided fractionation and purified by re-crystallisation. The structure was elucidated by LC–MS and ¹H NMR.

Results

The IC₅₀-value for MAO-A inhibition by quercetin was 18 ± 0.2 μM in an assay where the IC₅₀-value for MAO-A inhibition by clorgylin was 0.2 ± 0.02 μM.

Conclusion

The content of quercetin in Calluna vulgaris might explain the reported nerve calming effect of the plant.     

Viscum album (mistletoe) extract prevents changes in levels of red blood cells,PCV, Hb,serum proteins and ESR in high salt-fed rats

Aim of the study

The present study was aimed to determine the effects of Viscum album (mistletoe) on red blood cells, packed cell volume, Hb content, absolute haematological values {mean corpuscular volume (MCV), mean corpuscular haemoglobin (MCH), mean corpuscular haemoglobin concentration (MCHC), colour index (CI)}, plasma proteins and ESR in high salt-fed rats.

Materials and methods

24 male albino Wistar rats were divided into 4 groups of 6 rats each. Group 1 received normal rat pellets + drinking water. Group 2 took same as group 1 + mistletoe extract (150 mg/kg body weight, orally once daily). Group 3 took high salt (8% NaCl) diet + 1% NaCl drinking water. Group 4 took same as group 3 + mistletoe extract (150 mg/kg body weight, orally once daily). The feeding regimens lasted for 6 weeks.

Results

We observed that the mean RBC, PCV and Hb in the control group were 5.21 ± 0.09 × 10⁶ cells/mm³, 43.50 ± 1.61%, and 10.88 ± 0.21 g/dl respectively. The extract significantly (P < 0.05) reduced the RBC (5.72 ± 0.08 × 10⁶ cells/mm³), PCV (54.50 ± 2.64%) and Hb (14.33 ± 5.78 g/dl) in high salt-fed rats to near control levels. The extract also brought the elevated total plasma protein levels and reduced ESR in the high salt-fed rats (86.77 ± 1.08 g/L and 1.83 ± 0.31 mm/h respectively) to near control levels (82.23 ± 0.91 g/L and 2.83 ± 0.31 mm/h respectively), indicating the ability of the extract to prevent marked changes in the blood viscosity. The MCV, MCH, MCHC, and CI were not significantly altered by either extract or salt loading.

Conclusion

Crude mistletoe extract prevents changes in RBC, PCV, plasma protein levels, and ESR, and indication that the extract prevents changes in blood viscosity a major determinant of arterial blood pressure.     

Mouririelliptica: Validation of gastroprotective,healing and anti-Helicobacter pylori effects

Ethnopharmacological relevance

Mouriri elliptica Martius (Melastomataceae) is species reputed in folk medicine to heal gastric ulcer and gastritis.

Aim of the study

Methanolic extract (ME) and ethyl acetate fraction (EAF) from leaves of Mouriri elliptica were evaluated for their gastroprotective, healing, immunological, toxicological and anti-Helicobacter pylori activities.

Material and methods

The gastroprotective action of ME and EAF was evaluated in rodent experimental models and to elucidate mechanisms of action, the antisecretory action, involvements of NO, SH, PGE₂, anti-Helicobacter pylori action of ME was evaluated. We also used immunohistochemical (PCNA and COX-2) and immunomodulatory (murine peritoneal macrophages) assays to evaluate Mouriri elliptica effects.

Results

ME present gastroprotective action without antisecretory effect. Otherwise, ME showed anti-Helicobacter pylori action (MIC = 0.025 μg/mL) and was able to inhibit NO production by macrophages. This species also accelerate the healing of ulcerated gastric mucosa by stimulating proliferation factors (PCNA), COX-2 and maintained basal PGE₂ level independent action of NSAID in gastric mucosa. The phytochemical investigation showed that this species possesses phenolic acid derivatives, acylglycoflavonoids and condensed tannins which probably influenced their pharmacological action.

Conclusion

All these results suggest the efficacy and safety of Mouriri elliptica in combating and healing gastric ulcer.     

Antihyperlipidemic effect of the methanolic extract from Lagenaria siceraria Stand. fruit in hyperlipidemic rats

Ethnopharmacological relevance

Lagenaria siceraria Stand. (Cucurbitaceae) fruits have been used, traditionally, in the treatment of hyperlipidemia and atherosclerotic impasse and considered as cardioprotective and cardiotonic drug.

Aim of the study

The present work was undertaken to investigate the effects of methanolic extract from Lagenaria siceraria in experimentally induced hyperlipidemia in rats.

Materials and methods

Methanolic extract of Lagenaria siceraria fruits (LSFE) (100, 200 and 300 mg/kg; p.o.) was administered to the high fat-diet-induced hyperlipidemic rats for 30 days to evaluate its antihyperlipidemic activity. Atorvastatin (10 mg/kg; p.o.) was used as a standard drug.

Results

At the 30th day, most significant reduction in lipid levels in the LSFE treated rats as compared to the rats fed with high-fat diet at the 0th day were: total cholesterol 290.14 ± 18.42 mg/dl vs. 228.58 ± 16.38 mg/dl, low-density lipoprotein cholesterol 195.14 ± 8.86 mg/dl vs. 120.57 ± 8.11 mg/dl, triglyceride 232.41 ± 15.22 mg/dl vs. 181.79 ± 15.68 mg/dl, very low-density lipoprotein cholesterol 46.48 ± 3.04 mg/dl vs. 36.35 ± 3.13 mg/dl (P < 0.0001). Conversely, high-density lipoprotein cholesterol levels were significantly (P < 0.0001) increased from 48.52 ± 6.52 to 71.66 ± 5.14 mg/dl. The increase in weight in rats administered with LSFE was less when compared to rats fed with high-fat diet. Moreover, LSFE also exhibited significant increase in excretion of bile acids.

Conclusion

The results demonstrate that the LSFE has a definite antihyperlipidemic potential. There is also a valid scientific basis for consuming it in the treatment of coronary artery diseases in India.     

In vitro xanthine oxidase inhibitory activity of the fractions of Erythrina stricta Roxb.

Aim of the study

To assay the in vitro xanthine oxidase inhibitory activity of the various fractions of the hydromethanolic extract of the leaves of Erythrina stricta and to determine its enzyme inhibition mechanism.

Materials and methods

Xanthine oxidase inhibitory activity was assayed spectrophotometrically under aerobic conditions and the degree of enzyme inhibition was determined by measuring the increase in absorbance at 295 nm associated with uric acid formation. Enzyme kinetics was carried out using Lineweaver-Burk plots using xanthine as the substrate.

Results

Among the fractions tested, the chloroform fraction exhibited highest potency (IC₅₀ 21.2 ± 1.6 μg/ml) followed by the pet–ether (IC₅₀ 30.2 ± 2.2 μg/ml), ethyl acetate (IC₅₀ 44.9 ± 1.4 μg/ml) and residual (IC₅₀ 100 ± 3.3 μg/ml) fractions. The IC₅₀ value of allopurinol used, as the standard was 6.1 ± 0.3 μg/ml. Enzyme inhibition mechanism indicated that the mode of inhibition was of a mixed type.

Conclusion

These results suggest that the use of Erythrina stricta for the treatment of gout could be attributed to its xanthine oxidase inhibitory activity.     

Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum

Ethnopharmacological importance

Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.

Aim of the study

To investigate the mode of the relaxing action of a methanolic extract prepared from the seeds of Celastrus paniculatus (CPE, 0.0001–10 μg/mL) in the rat ileum and to try to confirm on human tissues the intestinal pharmacological activity of the extract.

Materials and methods

The relaxant effect of CPE was studied in vitro by evaluating its effect on the spontaneous contractions of the isolated ileum.

Results

CPE exerted a tetrodotoxin- and ω-conotoxin-resistant inhibitory effect on rat ileum motility (IC₅₀: 0.24 ± 0.02 μg/mL; E_max: 99.0 ± 0.60%). The inhibitory effect was reduced by nifedipine but not by cyclopiazonic acid. Experiments with specific antagonists enabled us to exclude the involvement of the main endogenous spasmogenic (i.e. acetylcholine and tachykinins) and relaxing (noradrenaline, nitric oxide, ATP) compounds. CPE also relaxed the isolated human ileum (IC₅₀: 0.26 ± 0.02 μg/mL; E_max: 99.1 ± 0.46%).

Conclusion

It is concluded that (i) CPE exerted a powerful myogenic and L-type Ca²⁺-dependent relaxing effect in the isolated rat ileum and that (ii) the human ileum is sensitive to the inhibitory effect of CPE. If confirmed in vivo, our data could explain the traditional use of this herb in the treatment of intestinal spasms.     

In vitro antimicrobial activity of Caesalpinia ferrea Martius fruits against oral pathogens

Aim

In the Amazon region of Brazil, the fruits of Caesalpinia ferrea Martius (Brazilian ironwood) are widely used as an antimicrobial and healing medicine in many situations including oral infections. This study aimed to evaluate the antimicrobial activity of Caesalpinia ferrea Martius fruit extract against oral pathogens.

Materials and methods

Polyphenols estimation and spectral analysis (¹H NMR) of the methanol extract were carried out. The microorganisms Candida albicans, Streptococcus mutans, Streptococcus salivarius, Streptococcus oralis and Lactobacillus casei were tested using the microdilution method for planktonic cells (MIC) and a multispecies biofilm model. Chlorhexidine was used as positive control.

Results

Polyphenols in the extract were estimated at 7.3% and ¹H NMR analysis revealed hydroxy phenols and methoxilated compounds. MIC values for Candida albicans, Streptococcus mutans, Streptococcus salivarius, Streptococcus oralis and Lactobacillus casei were 25.0, 40.0, 66.0, 100.0, 66.0 μg/mL, respectively. For the biofilm assay, chlorhexidine and plant extract showed no growth at 10⁻⁴ and 10⁻⁵ microbial dilution, respectively. At 10⁻⁴ and 10⁻⁵ the growth values (mean ± SD) of the negative controls (DMSO and saline solution) for Streptococcus mutans, Streptococcus sp. and Candida albicans were 8.1 ± 0.7, 7.0 ± 0.6 and 5.9 ± 0.9 × 10⁶ CFU, respectively.

Conclusion

Caesalpinia ferrea fruit extract can inhibit in vitro growth of oral pathogens in planktonic and biofilm models supporting its use for oral infections.     

Hypoglycemic effect of quassinoids from Brucea javanica (L.) Merr (Simaroubaceae) seeds

Ethnopharmacological relevance

The seeds of Brucea javanica (L.) Merr (Simaroubaceae) are recommended by traditional practitioners for the treatment of diabetes mellitus.

Aim of the study

To identify the compounds responsible for blood glucose lowering effect and evaluate the acute toxicity of the compounds.

Materials and methods

Extracts, fractions and subfractions were administered to normoglycemic mice and the blood glucose concentration was monitored for 8 h. Bioactive compounds isolated through column chromatography were administered to normoglycemic mice and streptozotocin (STZ) rats with monitoring of blood glucose concentration at 0–8 h. The acute toxicity was evaluated in mice.

Results

Bioactivity-guided fractionation led to the isolation of bruceines E (1) and D (2). Normoglycemic mice administered with 1 mg/kg of 1 and 2 exhibited significant blood glucose concentration reduction of 40.07 ± 11.45% and 48.82 ± 13.34%, respectively. STZ induced diabetic rats administered with 1 and 2 exhibited significant blood glucose concentration reduction of 73.57 ± 13.64% and 87.99 ± 2.91%, respectively.

Conclusion

The reduction of blood glucose concentration by both bruceines was comparable to glibenclamide and they might act as an insulin secretagogue. The presence of a hydroxyl moiety at C₂ in 1 reduced the toxic effect by 9-fold compared to 2.     

Sedative and anticonvulsant activities of methanol extract of Dorstenia arifolia in mice

Ethnopharmacological relevance

Dorstenia arifolia is a plant that has been used in the folk medicine to produce hypnotic, sedative and ansiolitic effects but the pharmacological properties have not yet been studied. In addition, the smoke of its rhizome is reputed to induce lethargic sensation.

Aims of the study

The present study investigated possible activities of the methanol extract (ME) of Dorstenia arifolia rhizome on the central nervous system (CNS).

Materials and methods

ME was tested for sedative, hypnotic and anticonsulsant effects using locomotor activity evaluation, pentobarbital-induced sleeping time and pentylenetetrazol (PTZ)-induced convulsion, respectively.

Results

Intraperitoneal administration of ME (10 and 50 mg/kg) significantly decreased locomotor activity from 205.2 ± 25.6 movements/min (DMSO) to 112.1 ± 18.4 (P < 0.05) and 114.9 ± 16.9 (P < 0.05), respectively. Flumazenil (10 mg/kg), an antagonist of GABA_A receptor, prevented the ME-induced sedation. Treatment with ME (50 mg/kg) significantly increased the duration of pentobarbital-induced sleeping time from 41.0 ± 2.3 to 57.9 ± 2.9 min (P < 0.05). The latencies to seizures after intraperitoneal injection of PTZ was recorded and compared between groups. ME promoted a significant protection of PTZ-induced seizures and mortality in a dose-dependent manner.

Conclusions

Our findings indicate that ME of Dorstenia arifolia rizhome has pronounced central effects, and that the sedative and anticonvulsant activities may be related to a facilitation of the GABAergic transmission.     

Ethnomedicinal and ethnopharmaco-statistical studies of Eastern Rajasthan,India

Aim of study

The study was conducted in Eastern parts of Rajasthan from March 2008 to February 2009 to identify the important species used; determine the relative importance of the species surveyed and calculate the informant consensus factor (ICF) in relation to medicinal plant use.

Methodology or Material and methods

A total of 844 villagers (486 men and 358 women) were interviewed using specimen display method and a forest walk with interviewee and a semi-structured questionnaire was used to elicit the knowledge of use of medicinal plants. A total of 213 species of medicinal plants belonging to 68 families were documented.

Result

The family Fabaceae had the highest number of species (28) followed by Euphorbiaceae (14). The majority of informants (46.12%) mentioned Azadirachta indica as most popular remedy for the treatment of various ailments, followed by Ocimum sanctum (25.31%) and Tridax procumbens (21.63%). The average number of medicinal plants known and used by female and male practitioners was similar (χ = 9.192, d.f. = 17, p = 0.941). The number of medicinal plant species reported and used by each informant was not significantly (χ = 40.625, d.f. = 34, p = 0.202) different among the four districts: Alwar (7.80 ± 0.917), Bharatpur (6.88 ± 1.076), Dholpur (7.13 ± 0.965) and Karauli (7.97 ± 1.068).

Conclusion

From the study it is clear that ethnomedicinal information from traditional practitioners provides a corporeal guide towards development of new drugs than the approaches of random screening.     

Metabolic intervention of aflatoxin B1 toxicity by curcumin

Ethno pharmacological relevance

Curcumin, bioactive principle of turmeric (Curcuma longa Linn) is an important constituent of Indian traditional medicine. Turmeric has been known to possess several therapeutic properties.

Aim of the study

The modulatory effect of dietary curcumin (0.05%, w/w) on drug metabolizing and general marker enzymes of liver and formation of AFB₁-adducts (DNA and protein) due to dietary AFB₁ exposure for a period of 6 weeks in a rodent model, have been evaluated.

Materials and methods

Drug metabolizing enzymes CYP1A1, GSHT, UGT1A and general marker enzymes (LDH, ALT, AST, ALP and γ-GT) of liver were estimated by standardized methods. Aflatoxin adducts (DNA and protein) were quantitated by indirect competitive ELISA.

Results

Dietary curcumin enhanced GSHT (p < 0.001) and UGT1A1 (p < 0.05) activity and significantly reduced the activity of CYP1A1 (p < 0.001), in rats exposed to aflatoxin B₁. Supplementation of curcumin in the diet normalized the altered activities of LDH and ALT. At molecular level, curcumin significantly reduced AFB₁–N⁷-guanine adduct (p < 0.001) excretion in the urine, DNA adduct (p < 0.05) in the liver and albumin adduct (p < 0.001) in the serum.

Conclusion

The experimental results substantiates that curcumin intervention ameliorates the AFB₁ induced toxicity.