Abstract  Context: There are 33 Geranium species growing in Turkey characterized by the presence of polyphenolic compounds. Some Geranium (Geraniaceae) species are used as antidiabetics, hemostatics, antihemorrhoidals, antidiarrheics and for the treatment of pain, fevers, and gastrointestinal ailments, or are consumed as food. Objective: The in vitro antioxidant activity and antihemolytic effect of ethyl acetate (EtOAc), n-butanol (BuOH), methanol (MeOH) and water extracts of Geranium tuberosum L. subsp. tuberosum (Geraniaceae), a medicinal food plant, have been evaluated. Materials and methods: The two antioxidant enzyme activities of human erythrocyte, namely superoxide dismutase (SOD) and catalase (CAT), after in vitro incubation with the extracts, were examined in order to see whether the observed effects are related to altered enzymatic efficiency. Reduced glutathione (GSH) levels were also measured as oxidative stress marker. Antihemolytic activity of extracts was shown by hemolysis assay in erythrocytes. Furthermore, total phenolic content of extracts was measured by Folin-Ciocalteu method. Results: All extracts enhanced GSH levels, and the activity of SOD and CAT. The EtOAc extracts seems to be the most potent antioxidant at 100 µg/mL (SOD activity 173.736 ± 8.33, CAT activity 133.218 ± 3.31, GSH level 2.264 ± 2.21). However, apart from the MeOH extracts at 100 µg/mL (68.699 ± 3.93), they didn't increase the resistance of erythrocytes to H(2)O(2) induced cytotoxicity. Therefore, while a significant antioxidant effect was observed in these samples, antihemolytic effect was not determined. Discussion and conclusion: The title plant has shown high antioxidant activity without cytotoxicity up to 100 µg/mL, thus could be a potent source as natural antioxidant.

Abstract  ETHNOPHARMACOLOGICAL RELEVANCE: The present investigation was aimed to justify the pharmacological basis in traditional use of Clerodendrum colebrookianum as antihypertensive agent in north-east India.

MATERIALS AND METHODS: The aqueous extract (AECc), its aqueous, n-butanol (nBFCc), Ethyl-acetate (EtFCc) and Chloroform fractions of C. colebrookianum leaves were evaluated for antihypertensive potential by using fructose-induced hypertension model in rats and in isolated frog heart. The ex-vivo muscarinic action in isolated rat ileum, in-vitro assay for Rho-kinase (ROCK -II), phosphodiesterase-5 (PDE-5) and angiotension converting enzyme (ACE) were also carried out to establish the mechanism of action of samples. The total phenolic and flavonoied contents in test samples were estimated to establish phyto-pharmacological relationship.

RESULTS: The 100μg/mL test samples were showed calcium antagonism in rat ileum and at 50μg/mL and 75μg/mL doses exhibited ROCK-II and PDE-5 inhibition respectively where, EtFCc was caused maximum 68.62% (ROCK-II) and 52.28% (PDE-5) inhibition, but none of the sample was exhibit effect in ACE at 100μg/mL. The test samples also showed negative inotropic and chronotropic effect on isolated frog heart and significant (P<0.001) reduction in systolic blood pressure and heart rate in hypertensive rats compared to control. The total phenolic content maximum 80μg gallic acid equivalents in nBFCc and flavonoids content maximum 69.57μg Quercetin equivalent in AECc were estimated.

CONCLUSIONS: These observations established the traditional claim and thus C. colebrookianum could be a potent antihypertensive agent for use in future. The antihypertensive effect mediated by cholinergic action and following ROCK - II, PDE-5 inhibition of C. colebrookianum.

Abstract  Biological screening of Scrophularia nodosa crude extract and its fractions (hexane, chloroform, ethyl-acetate, n-butanol and aqueous) was carried out on phytotoxicity, cytotoxicity, antibacterial, antifungal and analgesic activities. Crude extract and its fractions produced 50-100% phytotoxicity at 1000μ/mL concentration whereas 25-77% phytotoxicity was observed at 10μ/mL concentration. The fractions exhibited significant antibacterial and antifungal effects. The non-toxic results of this plant were recorded in Brine Shrimps Bioassay method at all concentrations. Similarly no significant insecticidal activity was observed in crude extracts and fractions. Analgesic activity results of S. nodosa in mice were found highly significant in crude extract as compared to fractions. In writhing test crude extract at 500 mg/kg showed 65.6% highest inhibitory response in mice.

Abstract  AIM OF THE STUDY: Actinostemma lobatum Maxim, a wildlife plant of Cucurbitaceae family, has been utilized for the prevention or treatment of cardiovascular diseases as a folk remedy in Korea. However, its scientific evidence remains unclear. Thus, in the present study, we examined the effects of butanol fraction of Actinostemma lobatum Maxim (BFALM) on the in vitro and in vivo antithrombotic activity and possible mechanisms were elucidated for the first time.

MATERIAL AND METHODS: To elucidate the antithrombotic mechanism of BFALM, platelet aggregation assay, coagulation assay, glycoprotein IIb/IIIa assay, thromboxane A(2) assay and in vivo pulmonary thromboembolism experiment were performed.

RESULTS: BFALM significantly inhibited collagen, adenosine diphosphate (ADP) and thrombin-induced platelet aggregation in a concentration dependent manner. Consistently, oral administration of BFALM resulted in a dose-dependent increase of survival rates of mice with pulmonary thromboembolism induced by intravenous injection of collagen and epinephrine. In mechanism assays for the antithrombotic activity of BFALM, BFALM significantly inhibited the fibrinogen binding to the platelet surface Glycoprotein IIb/IIIa (GP IIb/IIIa) receptor in a concentration dependent fashion, as well as reduced the level of thromboxane A(2) at 400microg/ml. Furthermore, BFALM significantly prolonged the prothrombin time (PT) and activated partial thromboplastin time (APTT) compared with untreated control.

CONCLUSIONS: These results suggest that BFALM may exert antithrombotic activity through inhibition of platelet aggregation via GP IIb/IIIa and thromboxane A(2) pathways, along with anticoagulatory activity through intrinsic and extrinsic pathways.

Abstract  To compensate for possible decreases in animal production due to restrictions on the use of antibiotics as growth promoters, several non-antibiotic alternatives have been investigated. Organic acid supplementation (OAS) of feed or water has shown some promising results for affecting intestinal microbiota and reducing pathogenic bacteria in the gastrointestinal (GI) tract. However, few studies have explored the effects of OAS on microbial communities using objective molecular-based techniques. The aim of the present study was to characterize via 16S rRNA gene-based approaches responses of the intestinal microbiota after OAS in chicks. Newborn chicks were randomly divided in four treatments: (a) control (no antibiotic, no OAS); (b) antibiotic administration (bacitracin MD); (c) organic acid blend dl-2-hydroxy-4(methylthio) butanoic acid [HMTBA]; lactic, and phosphoric acid (HLP); and (d) organic acid blend HMTBA, formic, and propionic acid (HFP). Ileal contents and mucosal scrapings from 7 chicks/treatment/day were taken at 15, 22, and 29 days of age, and genomic DNA was isolated for the molecular analysis of the intestinal microbiota. The data demonstrate that HFP blend treatment for 29 consecutive days affected ileal microbial populations as indicated by community fingerprinting analysis (16S rRNA PCR-DGGE). In parallel, total bacterial and lactobacilli populations were increased by the HFP blend treatment as demonstrated by targeted qPCR analysis of 16S rRNA. In summary, the present data demonstrate that OAS, HFP blend treatment in particular, shifts intestinal microbiota, generates more homogenous and distinct populations, and increases Lactobacillus spp. colonization of the chick ileum.

Abstract  CONTEXT: The leaf of sage Salvia officinalis L. (Lamiaceae) is reputed in the folk medicine of Arabia, and Jordan in particular, to relieve pain associated with gastrointestinal disturbance.

OBJECTIVES: Evaluation of the antinociceptive and anti-inflammatory activities of aqueous and butanol extracts of S. officinalis leaf.

MATERIALS AND METHODS: The analgesic effects of the aqueous extract (10, 31.6, 100, 316, 1000 mg/kg) and butanol extract (10, 31.6, 100, 316 mg/kg) were studied using the hot-plate test for mice and the formalin-induced paw licking in rats. The effects were compared to those of morphine and the influence of naloxone on these effects was also evaluated. The same concentrations of both extracts were used to evaluate their anti-inflammatory effects using the cotton pellet granuloma and carrageenan-induced paw edema in rats.

RESULTS: The aqueous extract (10, 31.6, 100, 316, 1000 mg/kg) and butanol extract (10, 31.6, 100, 316 mg/kg) caused analgesic effect in the hot-plate latency assay as well as in early and late phases of formalin-induced paw licking in rats. These effects were reduced by the opioid receptor antagonist, naloxone (5 mg/kg). The same range of doses of both extracts caused dose-dependent inhibition of carrageenan-induced paw edema in rats as well as inhibition of cotton pellet granuloma.

DISCUSSION AND CONCLUSION: These observations suggest that the sage leaf aqueous and butanol extracts have analgesic and anti-inflammatory effects, confirming the traditional use of this plant for pain alleviation.

Abstract  Using 24 diarrheic dairy calves under 8 weeks old, multiple fecal samples (4-12) were collected individually during the clinical advancing (max. 10 days) to evaluate the importance of fecal ammonia, lactate and volatile fatty acid (VFA) levels. Removing 3 calves not recovered during the sampling, 21 calves were grouped into under 3 weeks (< 3 wk; n=11) and 3-8 weeks old (3-8 wk; n=10). Data were divided into diarrheic and recovered feces with averaging in individuals. Diarrheic feces showed lower VFA and n-butyrate, and higher acetate proportions than recovered feces at <3 wk, but not at 3-8 wk. Diarrhea showed higher lactate, and lower ammonia and minor VFA (i-butyrate, valerate), which might reflect insufficiency in gut flora and fermentation.

Abstract  The aim of the study was to investigate the effect of feeding different diets on fermentation, enzyme activities and microbial population in the rumen fluid of mithun (Bos frontalis). In a randomized block design, 20 male mithun (6-8 months of age, 152 ± 12.6 kg body weight) were randomly divided into four experimental groups (n = 5/group) and fed experimental diets ad libitum for 180 days. The diet R(1) contained tree foliages (TF), R(2) comprised of 50% concentrate mixture (CM) and 50% TF, R(3) contained 50% CM and 50% rice straw, and R(4) contained 50% CM, 25% TF and 25% rice straw. Rumen liquor was collected at 0 and 180 days of the experiment for estimation of different ruminal parameters and a digestion trial was conducted at the end of the experiment. Rumen fluid was analysed for pH, ammonia nitrogen (NH(3) -N), total-N, ruminal enzymes, short chain fatty acid (SCFA) and microbial profile. The relative quantification of ruminal microbes was carried out with real-time PCR using bacteria as the house keeping gene. The dry matter intake, nutrients digestibility, body weight gain, NH(3) -N, total-N, carboxymethyl cellulase, avicelase, xylanase, amylase, protease and molar proportion of butyrate were (p < 0.05) higher in mithun fed R(2) , R(3) and R(4) compared to those fed R(1) diet. In contrast, increased (p < 0.05) ruminal pH, molar proportion of acetate and, acetate to propionate ratio was recorded in mithun fed only TF than those fed concentrate supplemented diets. Similarly, an increase (p < 0.05) in the population of Fibrobacter succinogenes, Ruminococcus flavefaciens and total bacteria were evident in mithun fed R(2) , R(3) and R(4) compared to those fed R(1) . Therefore, it is concluded that TF 25% and/or rice straw 25% along with CM 50% may be fed to the growing mithun for improved rumen ecology, nutrient utilization and thus better performance under stall fed system.

Abstract  The total phenolic content (Folin-Ciocalteu) of the leaves of Ficus benjamina and Ficus luschnathiana was evaluated and screened by HPLC-DAD. Ficus luschnathiana crude extract (CE) presented phenolic content higher than that of F. benjamina (149.92 ± 3.65 versus 122.63 ± 2.79 mg of GAE). Kaempferol (1.63 ± 0.16 mg g(-1) dry weight of CE) and chlorogenic acid (17.77 ± 0.57 mg g(-1) of butanolic fraction) were identified and quantified in F. benjamina, whereas rutin (1.39 ± 0.20 mg g(-1)), caffeic (1.14 ± 0.13 mg g(-1)) and chlorogenic (3.73 ± 0.29 mg g(-1)) acids were quantified in the CE of F. luschnathiana. Additionaly, rutin (15.55 ± 1.92 mg g(-1)) and quercetin (3.53 ± 0.12 mg g(-1)) were quantified in ethyl acetate and butanolic fractions, respectively. Antimycobacterial activity of CEs and fractions was evaluated against Mycobacterium smegmatis by broth microdilution method. Ethyl acetate fraction from F. benjamina and n-butanol fraction from F. luschnathiana displayed the highest inhibitory activity (MIC = 312.50 µg mL(-1) and 156.25 µg mL(-1), respectively). Further studies are required to identify the compounds directly related to antimycobacterial activity.

Abstract  Enriched environments (EEs) during development have been shown to influence adult behaviour. Environmental conditions during childhood may contribute to the onset and/or pathology of schizophrenia; however, it remains unclear whether EE might prevent the development of schizophrenia. Herein, we investigated the effects of EE during adolescence on phencyclidine (PCP)-induced abnormal behaviour, a proposed schizophrenic endophenotype. Male ICR mice (3 wk old) were exposed to an EE for 4 wk and then treated with PCP for 2 wk. The EE potentiated the acute PCP treatment-induced hyperlocomotion in the locomotor test and prevented chronic PCP treatment-induced impairments of social behaviour and recognition memory in the social interaction and novel object recognition tests. It also prevented the PCP-induced decrease of acetylated Lys9 in histone H3-positive cells and increase of the histone deacetylase (HDAC)5 level in the prefrontal cortex. To investigate whether the histone modification during adolescence might be critical for the effect of EE, 3-wk-old mice were first treated with sodium butyrate (SB; an HDAC inhibitor) for 4 wk and then treated with PCP for 2 wk. Chronic SB treatment during adolescence mimicked the effects of EE, including potentiation of hyperlocomotion induced by acute PCP treatment and prevention of social and cognitive impairments, decrease of acetylated Lys9 in histone H3-positive cells and increase of the HDAC5 level in the prefrontal cortex associated with chronic PCP treatment. Our results suggest that EEs prevent PCP-induced abnormal behaviour associated with histone deacetylation. EEs during childhood might prove to be a novel strategy for prophylaxis against schizophrenia.

Abstract  This study examined the potential antilithic effects of a traditional Chinese medicine Urtica dentata Hand (UDH) in experimental rats and screened the optimal extract of UDH as a possible therapeutic agent for kidney stones. The rat model of urinary calcium oxalate stones was induced by intragastric (i.g.) administration of 2 mL of 1.25% ethylene glycol (EG) and 1% ammonium chloride (AC) for 28 days and was confirmed by Color Doppler ultrasound imaging. The rats in different experimental groups were then intragastrically given petroleum ether extract (PEE), N-butanol extract (NBE), aqueous extract (AqE) of UDH, Jieshitong (positive control drug), and saline, respectively. Treatment with NBE significantly reduced the elevated levels of urinary calcium, uric acid, phosphate, as well as increased urinary output. Accordingly, the increased calcium, oxalate levels and the number of calcium oxalate crystals deposits were remarkably reverted in the renal tissue of NBE-treated rats. In addition, NBE also prevented the impairment of renal function to decrease the contents of blood urea nitrogen (BUN) and creatinine. Taken together, these data suggest that NBE of UDH has a beneficial effect on calcium oxalate urinary stones in rats by flushing the stones out and protecting renal function.

Abstract  The present study was planned to investigate sleep-prolonging effect of C. sativum. The hydro-alcoholic extract (HAE) and its three fractions namely water (WF), ethyl acetate (EAF) and N-butanol (NBF) were prepared from C. sativum aerial parts and administrated to mice. Also, the possible cytotoxicity of the extracts was tested using cultured PC12 cells. The HAE, EAF and NBF significantly prolonged sleep duration. Only the NBF could significantly decrease sleep latency. No decrease in the neuronal surviving was observed either by HAE or by its fractions. The present data indicate that C. sativum exert sleep-prolonging action without major neurotoxic effect.

Abstract  AIM: This study evaluated the effect of 2-hydroxymethyl methacrylate (HEMA) and the type of solvent on the tensile bond strength of the following three self-etch adhesives: Adper easy one (HEMA-rich adhesive) which contained ethanol, G-Bond (HEMA-free adhesive) which contained acetone, and Xeno V (HEMA-free adhesive) which contained butanol as a solvent.

MATERIAL AND METHODS: Intact mandibular molars were mounted in self-cured resin and the occlusal surfaces were ground with # 600 SiC paper. Adhesives were applied on the prepared dentinal surfaces and the resin composite was condensed in the split brass mold (5 × 3 mm) placed over the adhesive surface. The specimens were stored in normal saline and placed in incubator at 37°C. After 24 hours, the specimens were tested in tensile mode at a crosshead speed of 1 mm/min. Statistical analysis was done using One way ANOVA and Tukey's HSD test.

RESULTS: The mean bond strengths of Adper easy one, G-Bond, and Xeno V were 12.41 MPa, 10.09 MPa, and 8.67 MPa, respectively.

CONCLUSIONS: Comparison of contemporary adhesives in this ex vivo study revealed that the ethanol-based HEMA-rich self-etch adhesive is better than HEMA-free self-etch adhesive that contained acetone and butanol as the solvents, when compared in terms of bond strength.

Abstract  In the present study, the root nodules of Premna herbacea Roxb. (PH) was investigated for its in vitro cytotoxicity and in vivo antitumor activity. Two extracts, aqueous and alcoholic; two fractions of alcoholic extract, ethyl acetate and butanol fractions were screened for their in vitro cytotoxicity by brine shrimp lethality (BSL) assay, trypan blue exclusion assay and MTT assay. Alcoholic extract and its ethyl acetate fraction were found to be the most effective in BSL assay, trypan blue exclusion assay. In vivo antitumor activity was screened in the Ehrlich ascites carcinoma (EAC) model and the Dalton lymphoma ascites (DLA) model. The extracts and the fractions were tested at two dosages (250 and 500mg/kg) by intraperitoneally (i.p.) route on every alternate day upto 13th day. Cisplatin was used as positive control in both studies in single dose (day 1) 3.5mg/kg by i.p. route. In EAC model, ascites tumor was induced by inoculating 2.5 million of EAC cells i.p. alcoholic extract at 500mg/kg was the most effective in elevating MST, reduction in body weight in EAC induced tumor. Only the effective extract i.e., alcoholic extract were studied for hematological and antioxidant parameter. It showed a restoring effect on altered hematological parameters and a significant improvement in biochemical parameters at 250mg/kg dose of alcoholic extract. These results explain the toxicity of 500mg/kg might be high. In the Dalton lymphoma ascites (DLA) model, solid tumor was developed by i.m. injection of 1 million DLA cells. Both the extracts and the fractions possessed potent antitumor activity against solid tumor models by significantly reducing the solid tumor weight and volume.

Abstract  AIM AND BACKGROUND: Antibiotic resistance currently spans most of the known classes of natural and synthetic antibiotics; limiting our options for treatment of infections and demanding discovery of new classes of antibiotics. Much effort is being directed towards developing new antibiotics to overcome this problem. Success in getting novel chemical entities from microbial sources depends essentially on novelty of its habitat. The diversity of geographical location decides the type of micro-flora. In the past various terrestrial and aqueous microorganisms have provided several novel bioactive secondary metabolites of pharmaceutical importance. Hot-springs have not been as extensively exploited as other terrestrial resources. However, perseverance with such microbes augment the probability of getting novel bioactive compounds.

MATERIALS AND METHODS: Hot-springs soil samples were collected from Hot-springs in Maharashtra. Actinomycetes and other eubacteria were isolated from these soil samples by selective methods and purified. They were classified based on gram's nature and morphology. Six representative morphological strains were screened for their anti-infective potential by agar well diffusion method as reported by Nathan P. et al (1974). The bioactivity of the active microbes was confirmed.

RESULTS: Seventy three strains of bacteria encompassing eight actinomycetes, and 65 eubacteria were isolated and purified. Among the actives eubacteria PPVWK106001 showed broad spectrum antibacterial activity encompassing both gram positive and gram negative bacterial test models. The extract was active against resistant bacteria such as MRSA and VREs. Activity was very specific as there was no activity against fungi even at 100 fold concentration. The active principle was extractable in butanol.

CONCLUSIONS: The study showed that Hot-springs exhibit diverse bacteria and it serves as potential reservoirs for bacteria of antimicrobial importance with diverse facet of activities. Thus Hot-springs microbes have ability to address issue of resistant bugs.

Abstract  Herein we report the generation of counterion radicals and their reactions in quaternary water-in-oil microemulsion. Hydrated electrons in the microemulsion CTAB/H(2)O/n-butanol/cyclohexane have a remarkably short half-life (∼1 μs) and lower yield as compared to that in the pure water system. Electrons are solvated in two regions: one is the water core and other the interface; however, the electrons in the water core have a shorter half-life than those in the interface. The decay of the solvated electrons in the interface is found to be water content dependent and it has been interpreted in terms of increased interfacial fluidity with the increase in water content of the microemulsion. Interestingly another species, dibromide radical anion (Br(2)(•-)) in CTAB and CPB microemulsions have been observed after the electron beam irradiation. Assuming that the extinction coefficient of the radicals is the same as that in the aqueous solution, the yields of the radicals per 100 eV are 0.29 and 0.48 for the Br(2)(•-) radical in CTAB and CPB containing microemulsions (W(0) = 40), respectively, under N(2)O saturated conditions. Further, we intended to study electron transfer reactions, which occur at and through the interface. The reaction of the Br(2)(•-) radical anion with ABTS [2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] has been studied to generate the ABTS radical in the water core, and further, its reaction has been investigated with the water-insoluble molecule vitamin E (tocopherol) and water-soluble vitamin C (ascorbic acid). In the present study, we were able to show that, even for molecules which are completely insoluble in water, ABTS scavenging assay is possible by pulse radiolysis technique. Furthermore, these results show that it is possible to follow the reaction of the hydrated inorganic radical with solutes dissolved in the organic phase in a microemulsion without use of a phase transfer catalyst.

Abstract  Inflammatory skin disorders, such as psoriasis and atopic dermatitis, are very common in the population; however, the treatments currently available are not well tolerated and are often ineffective. Averrhoa carambola L. (Oxalidaceae) is an Asian tree that has been used in traditional folk medicine in the treatment of several skin disorders. The present study evaluates the topical anti-inflammatory effects of the crude ethanolic extract of A. carambola leaves, its hexane, ethyl acetate, and butanol fractions and two isolated flavonoids on skin inflammation. Anti-inflammatory activity was measured using a croton oil-induced ear edema model of inflammation in mice. Topically applied ethanolic extract reduced edema in a dose-dependent manner, resulting in a maximum inhibition of 73 ± 3% and an ID(50) value of 0.05 (range: 0.02-0.13) mg/ear. Myeloperoxidase (MPO) activity was also inhibited by the extract, resulting in a maximum inhibition of 60 ± 6% (0.6 mg/ear). All of the fractions tested caused inhibition of edema formation and of MPO activity. Treatment with the ethyl acetate fraction was the most effective, resulting in inhibition levels of 75 ± 5 and 54 ± 8% for edema formation and MPO activity, respectively. However, treatment of mice with isolated compounds [apigenin-6-C-β-l-fucopyranoside and apigenin-6-C-(2″-O-α-l-rhamnopyranosyl)-β-l-fucopyranoside] did not yield successful results. Apigenin-6-C-(2″-O-α-l-rhamnopyranosyl)-β-l-fucopyranoside caused only a mild reduction in edema formation (28 ± 11%). Taken together, these preliminary results support the popular use of A. carambola as an anti-inflammatory agent and open up new possibilities for its use in skin disorders.

Abstract  The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity of the fruits of Rubus chingii was studied in vitro. Ethanolic extract, ethyl acetate and n-butanol fractions from dried R. chingii fruits revealed strong DPPH free radical scavenging activity with IC(50) values of 17.9, 3.4 and 4.0 μg/mL, respectively. The ethyl acetate and n-butanol fractions were further purified by a combination of silica gel chromatography, Lobar RP-8 chromatography, and high-pressure liquid chromatography (HPLC). Nine compounds were isolated, where methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), vanillic acid (5), kaempferol (7), and tiliroside (9) showed stronger DPPH free radical scavenging activity than that of ascorbic acid (131.8 μM) with IC(50) values of 45.2, 34.9, 78.5, and 13.7 μM, respectively. In addition, rubusine (1) is a new compound discovered in the present study and methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), methyl dioxindole-3-acetate (3), and 2-oxo-1,2-dihydroquinoline-4-carboxylic acid (4) were isolated from the fruits for the first time.

Abstract  Abutilon indicum (L.) Sweet is an Asian phytomedicine traditionally used to treat several disorders, including diabetes mellitus. However, molecular mechanisms supporting the antidiabetic effect of A. indicum L. remain unknown. The aim of this study was to evaluate whether extract of A. indicum L. improves insulin sensitivity. First, we observed the antidiabetic activity of aqueous extract of the entire plant (leaves, twigs and roots) of A. indicum L. on postprandial plasma glucose in diabetic rats. The subsequent experiments revealed that butanol fractions of the extract bind to PPARγ and activate 3T3-L1 differentiation. To measure glucose uptake enhanced by insulin-like activity, we used rat diaphragm incubated with various concentrations of the crude extract and found that the extract enhances glucose consumption in the incubated solution. Our data also indicate that the crude extract and the fractions (water and butanol) did not affect the activity of kinases involved in Akt and GSK-3β pathways; however, the reporter assay showed that the crude extract could activate glucose transporter 1 (GLUT1) promoter activity. These results suggest that the extract from A. indicum L. may be beneficial for reducing insulin resistance through its potency in regulating adipocyte differentiation through PPARγ agonist activity, and increasing glucose utilization via GLUT1.

Abstract  The efficacy of decoction in extracting mycobactericidal compounds from Flourensia cernua (Hojasé) leaves and fractionation with solvents having ascending polarity was compared with that of (i) ethanol extraction by still maceration, extraction with a Soxhlet device, shake-assisted maceration, or ultrasound-assisted maceration, followed by fractionation with n-hexane, ethyl acetate, and n-butanol; (ii) sequential extraction with n-hexane, ethyl acetate, and n-butanol, by still maceration, using a Soxhlet device, shake-assisted maceration, or ultrasound-assisted maceration. The in vitro mycobactericidal activity of each preparation was measured against drug-sensitive (SMtb) and drug-resistant (RMtb) Mycobacterium tuberculosis strains. The results of which were expressed as absolute mycobactericidal activity (AMA). These data were normalized to the ΣAMA of the decoction fraction set. Although decoction was inactive, the anti-RMtb normalized ΣAMA (NAMA) of its fractions was comparable with the anti-RMtb NAMA of the still maceration extracts and significantly higher than the anti-SMtb and anti-RMtb NAMAs of every other ethanol extract and serial extract and fraction. Hexane extracted, from decoction, material having 55.17% and 92.62% of antituberculosis activity against SMtb and RMtb, respectively. Although the mycobactericidal activity of decoction is undetectable; its efficacy in extracting F. cernua active metabolites against M. tuberculosis is substantially greater than almost all pharmacognostic methods.

Abstract  The resistant dextrin NUTRIOSE®, developed from starch, is expected to act as a prebiotic. The aim of this study was to determine the effects of NUTRIOSE® on cecal parameters, short-chain fatty acid (SCFA) concentrations, and fecal excretion in rats. In an initial experiment, twenty-four male Fischer F344 rats were randomly assigned to one of the following four treatments for 14 days: G0 (control diet), G2.5 (control diet + 2.5% of dextrin), G5 (control diet + 5% of dextrin), and G10 (control diet + 10% of dextrin). After 14 days, total cecal weight, cecal content, and cecal wall weight were significantly increased in G5 and G10 compared to G0. At the same time, cecal pH was significantly lower in G10 compared to G0. Total SCFA concentration was significantly higher in G10 than in G5, G2.5, and G0, and significantly higher in G5 than in G0. Acetate, butyrate, and propionate concentrations were significantly increased in G5 and G10 compared to the controls. In a second trial based on a similar design, eighteen male Fischer F344 rats were treated with a control diet supplemented with 5% of dextrin or 5% of fructo-oligosaccharide. The results obtained with NUTRIOSE® were similar to those obtained with the fructo-oligosaccharide. In a third experiment, two groups of 5 Fischer F344 rats were orally treated with 100 and 1,000 mg/kg NUTRIOSE®, respectively, and from 18% to 25% of the dextrin was excreted in the feces. The results of these three studies show that the consumption of NUTRIOSE®, by its effects on total cecal weight, cecal content, cecal wall weight, pH, and SCFA production, could induce healthy benefits since these effects are reported to be prebiotic effects.

Abstract  In this study, Sesbania grandiflora, a plant in the Leguminosae family, was investigated for its antibacterial activities. The agar well diffusion assay as well as the agar and broth dilution assays were used for determination of antibacterial activities. The crude ethanolic extracts obtained from different parts of this plant exhibited different potent activities. The stem bark has the most potential to yield an extract with the highest antibacterial action. The fractionation of the stem bark with different solvents indicated that the fractionated extracts obtained from ethyl acetate or butanol possessed the most pronounced antibacterial activity. The kinetic study of bactericidal activities revealed that the butanol fractionated extract of the stem bark was effective against Gram negative bacteria. This study suggests that the stem bark of S. grandiflora contains promising antibacterial substances for clinical purposes.

Abstract  Antiapoptotic and antioxidant activities of aqueous-methanolic extract (CAME) of Orthosiphonstamineus Benth(OS), and its hexane (HF), chloroform (CF), n-butanol (NBF), ethyl acetate (EAF) and water (WF) fractions were investigated. Antioxidant properties were evaluated using the assays of Folin-Ciocalteu, aluminiumtrichloride, β-carotene bleaching and DPPH. The role of OS against hydrogen peroxide induced apoptosis on MDA-M231 epithelial cells was examined using MTT assay, phase contrast microscope, colorimetric assay of caspase-3, western blot and quantitative real-time PCR. Results showed that EAF showed the highest total phenolic content followed by CAME, NBF, WF, CF and HF, respectively. Flavonoid content was in the order of the CF > EAF > HF > CAME > NBF > WF. The IC(50) values on DPPH assay for different extract/fractions were 126.2 ± 23, 31.25 ± 1.2, 15.25 ± 2.3, 13.56 ± 1.9, 23.0 ± 3.2, and 16.66 ± 1.5 μg/ml for HF, CF, EAF, NBF, WF and CAME, respectively. OSreduced the oxidation of β-carotene by hydroperoxides. Cell death was dose-dependently inhibited by pretreatment with OS. Caspase-3 and distinct morphological features suggest the anti-apoptotic activities of OS. This plant not only increased the expression of Bcl-2, but also decreased Bax expression, and ultimately reduced H(2)O(2)-induced apoptosis. The current results showed that phenolics may provide health and nutritional benefits.

Abstract  The reaction methyl naphthalene-2-sulfonate + Br(-) was investigated in several alkanediyl-α-ω-bis(dodecyldimethylammonium) bromide, 12-s-12,2Br(-) (with s = 2, 3, 4, 5, 6, 8, 10, 12), micellar solutions in the absence and in the presence of various additives. The additives were 1,2-propylene glycol, which remains in the bulk phase, N-decyl N-methylglucamide, MEGA10, which forms mixed micelles with the dimeric surfactants, and 1-butanol, which distributes between the aqueous and micellar phases. Information about the micellar reaction media was obtained by using conductivity and fluorescence measurements. In all cases, with the exception of water-1,2-prop 12-5-12,2Br(-) micellar solutions, with 30% weight percentage of the organic solvent, a sphere-to-rod transition takes place upon increasing surfactant concentration. In order to quantitatively explain the experimental data within the whole surfactant concentration range, a kinetic equation based on the pseudophase kinetic model was considered, together with the decrease in the micellar ionization degree accompanying micellar growth. However, theoretical predictions did not agree with the experimental kinetic data for surfactant concentrations above the morphological transition. An empirical kinetic equation was proposed in order to explain the data. It contains a parameter b which is assumed to account for the medium micellar kinetic effects caused by the morphological transition. The use of this empirical equation permits the quantitative rationalization of the kinetic micellar effects in the whole surfactant concentration range.

Abstract  OBJECTIVE: To investigate the immunosuppressive potential of Pluchea lanceolata 50% ethanolic extract (PL) and its bioactive chloroform fraction (PLC).

MATERIALS AND METHODS: Preliminary screening of the Pluchea lanceolata 50% ethanolic extract (PL) was carried out with basic models of immunomodulation, such as, the humoral antibody response (hemagglutination antibody titers), cell-mediated immune response (delayed-type hypersensitivity), skin allograft rejection test, in vitro (C. albicans method), and in vivo phagocytosis (carbon clearance test). The extract was then fractionated with chloroform, n-butanol, and water to receive the respective fractions by partitioning. These fractions were employed for flow cytometry to study the T-cell specific immunosuppressive potential of these fractions.

RESULTS: Oral administration of PL at doses of 50 to 800 mg/kg in mice, with sheep red blood cells (SRBC) as an antigen, inhibited both humoral and cell-mediated immune responses, as evidenced by the production of the circulating antibody titer and delayed-type hypersensitiviy reaction results, respectively, and the immune suppression was statistically significant (P < 0.01) in Balb/C mice. PL also decreased the process of phagocytosis both in vitro (31.23%) and ex vivo (32.81%) and delayed the graft rejection time (30.76%). To study the T-cell-specific activities, chloroform, n-butanol, and water fractions from P. lanceolata were tested for T-cell specific immunosuppressive evaluation, wherein only the chloroform fraction (PLC) showed significant (P < 0.01) suppression of CD8+ / CD4+ T-cell surface markers and intracellular Th1 (IL-2 and IFN-(Y)) cytokines at 25 - 200 mg/kg p.o. doses. PLC, however, did not show significant suppression of the Th2 (IL-4) cytokine.

CONCLUSION: The findings from the present investigation reveal that P. lanceolata causes immunosuppression by inhibiting Th1 cytokines.