The Potential Antidepressant Action of Duloxetine Co-Administered with the TAAR1 Receptor Agonist SEP-363856 in Mice

Here, we explored the possible interaction between duloxetine and SEP-363856 (SEP-856) in depression-related reactions. The results showed that oral administration of duloxetine showed powerful antidepressant-like effects in both the forced swimming test (FST) and the suspension tail test (TST). SEP-856 orally administered alone also exerted an antidepressant-like effect in FST and TST, especially at doses of 0.3, 1, and 10 mg/kg. In addition, duloxetine (15 mg/kg) and SEP-856 (15 mg/kg) both showed antidepressant-like effects in the sucrose preference test (SPT). Most importantly, in the above experiments, compared with duloxetine alone, the simultaneous use of duloxetine and SEP-856 caused a more significant antidepressant-like effect. It is worth noting that doses of drug combination in FST and TST did not change the motor activities of mice in the open-field test (OFT). Thus, duloxetine and SEP-856 seem to play a synergistic role in regulating depression-related behaviors and might be beneficial for refractory depression.     

Chemical composition and antioxidant,antibacterial activity of Cirsium rivulare (Jacq) All. roots

The mixture of three phytosterols (campesterol, stigmasterol and β-sitosterol), β-sitosterol 3-O-glucoside and syringin were isolated from hexane and methanol extract of Cirsium rivulare roots after chromatographic separation. The main component of the source was syringin which was obtained with the yield 0.08% of the dry source. In hexane extract, the qualitative and quantitative composition of fatty acids was determined. The predominant component was linoleic acid (23.31 mg/g of extract). The extracts showed antioxidant activity. The ability to scavenge DPPH? free radical was in correlation with appointed total phenol content. The not-defatted methanolic extract was the most active. Hexane and defatted methanol extracts showed moderate antibacterial activity against G(+) and G(?) strains with MIC and MBC ranged from 25 to 200 μg/mL.     

Effects of aqueous extracts of Acacia albida stem bark on Wistar albino rats infected with Trypanosoma evansi

The effect of aqueous extract of Acacia albida stem bark was investigated in Wistar albino rats infected with Trypanosoma evansi. The extract showed highest reduction in parasitemia at the dose of 600 mg/kg body weight (bw). A dose of 300 mg/kg bw improved packed cell volume the most by 14.35%. The group treated with 150 and 600 mg/kg bw of the extract showed significant decrease (P < 0.05) in alanine transaminase and aspartate transaminase levels which were lower than those of the group treated with diminazene aceturate. The group treated with 150 mg/kg bw of the extract showed the least urea, albumin and protein level and lowest relative organ weight. There was a significant difference (P < 0.05) in the levels of catalase and Thiobarbituric acid reactive substances in liver and kidney of the animals in the infected-untreated group and the extracts-treated groups. The results of this study show that the extracts of A. albida have antitrypanosomal activity against T. evansi infection.     

Complementary and Comparative Study on Hypoglycemic and Antihyperglycemic Activity of Various Extracts of Eugenia jambolana Seed, Momordica charantia Fruits, Gymnema sylvestre, and Trigonella foenum graecum Seeds in Rats

In present study, we investigated hypoglycemic and antihyperglycemic potential of five extracts (water, ethanol, methanol, hexane, and chloroform) of four plants (i.e., seeds of Eugenia jambolana, fruits of Momordica charantia, leaves of Gymnema sylvestre, and seeds of Trigonella foenum graecum) alone and/or in combination with glimepiride in rats. Ethanol extract of E. jambolana, water extract of M. charantia, ethanol extract of G. sylvestre, and water extract of T. graecum exhibited highest hypoglycemic and antihyperglycemic activity (most active) in rats among all the extracts, while hexane extracts exhibited least activities. Most active extracts were further studied to dose-dependent (200, 100, and 50 mg/kg body weight (bw)) hypoglycemic and antihyperglycemic effects alone and in combination with glimepiride (20, 10, and 5 mg/kg bw). The combination of most active extracts (200 mg/kg bw) and lower dose of glimepiride (5 mg/kg bw) showed safer and potent hypoglycemic as well as antihyperglycemic activities without creating severe hypoglycemia in normal rats, while higher doses (200 mg/kg bw of most active extracts, and 10 and 20 mg/kg bw of glimepiride) were generated lethal hypoglycemia in normal rats. From this study, it may be concluded that the ethanol extract of E. jambolana seeds, water extract of M. charantia fruits, ethanol extract of G. sylvestre leaves, and water extract of T. graecum seeds have higher hypoglycemic and antihyperglycemic potential and may use as complementary medicine to treat the diabetic population by significantly reducing dose of standard drugs.     

Evaluation of hepatoprotective activity of aqueous extracts of leaves of Basella alba in albino rats

This study was done to evaluate possible hepatoprotective effects of aqueous leaf extracts of Basella alba in comparison with silymarin in paracetamol-induced hepatotoxicity in albino rats. Six groups of six albino rats each received orally for 6 weeks, vehicle, paracetamol (2 g/kg/day), paracetamol (2 g/kg/day) plus silymarin (50 mg/kg/day), paracetamol (2 g/kg/day) plus B. alba extract (60 mg/kg/day), paracetamol (2 g/kg/day) plus B. alba extract (80 mg/kg/day) and paracetamol (2 g/kg/day) plus B. alba extract (100 mg/kg/day). Hepatoprotective effect was evaluated by comparing serum bilirubin, serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, proteins, alkaline phosphatase and liver histopathology. Results were represented as mean ± SEM. One-way ANOVA was done followed by post hoc Tukey's test with a highly significance level of P < 0.001. Aqueous leaf extracts of B. alba 100 mg/kg/day orally had significant hepatoprotective effect in paracetamol-induced hepatotoxicity in albino rats. The results were well comparable and even in some respects superior to standard drug silymarin.     

Spermicidal activity of the hexane extract of Piper longum: an in vitro study

This study was carried out to assess the spermicidal action of hexane extract from the fruits of Piper longum Linn. The sperm immobilisation studies showed that 20 mg/mL of hexane extract was able to immobilise sperms completely within 20 s. The sperm revival test revealed that the effects were spermicidal as sperm immobilisation effect was irreversible. There was also a significant reduction in sperm viability in the treated group in comparison to the control. The hypo-osmotic swelling of these sperms was significantly reduced, indicating that the hexane extract may probably cause injury to the sperm plasma membrane. Hence, this study showed that the hexane extract of P. longum possesses potential contraceptive spermicidal activity in vitro.     

α-Glucosidase inhibitory activity of marine sponges collected in Mauritius waters

This report describes the use of α-glucosidase to evaluate the anti-diabetic potential of extracts from marine sponges collected in the Mauritius waters. Initial screening at 1.0 mg/mL of 141 extracts obtained from 47 sponge species revealed 10 extracts with inhibitory activity greater than 85%. Seven of the 10 extracts were further tested at 0.1 and 0.01 mg/mL and only the methanol extract of two sponges namely Acanthostylotella sp. (ASSM) and Echinodictyum pykei (EPM) showed inhibition activity greater than 60% at 0.1 mg/mL with an IC₅₀ value of 0.16 ± 0.02 and 0.04 ± 0.01 mg/mL, respectively, while being inactive at 0.01 mg/mL.     

A new ultra-high pressure liquid chromatography method for the determination of antioxidant flavonol aglycones in six Lysimachia species

UPLC-DAD method was developed and validated for the quantitative determination of free flavonol aglycones (kaempferol, quercetin and myricetin) after acidic hydrolysis in six Lysimachia species. Quantitative analyses showed that the amounts of various flavonol aglycones were significantly different in Lysimachia vulgaris, Lysimachia nummularia, Lysimachia punctata, Lysimachia christinae, Lysimachia ciliata and Lysimachia clethroides. The L. clethroides sample was found to be the richest in kaempferol (25.77 ± 1.29 μg/mg extract) and quercetin (97.67 ± 4.61 μg/mg extract), while the L. nummularia sample contained the highest amount of myricetin (20.79 ± 1.00 μg/mg extract). The antioxidant capacity of hydrolysed extracts was evaluated using in vitro DPPH^? (2,2-diphenyl-1-picrylhydrazyl) and ABTS^?+ [2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid)] decolourisation tests. The observed radical scavenging capacities of the extracts showed a relationship with the measured flavonol aglycone content and composition. The acidic treatment resulted in an increased free radical scavenging activity compared to the untreated methanol extract.     

Polyphenolic profiling of Ipomoea carnea Jacq. by HPLC-DAD and its implications in oxidative stress and cancer

Ipomoea carnea Jacq. is an important folklore medicinal plant, assessed for its underexplored biological potential. Antioxidant, cytotoxic, antiproliferative and polyphenolic profile of whole plant was evaluated using various techniques. Maximum extract recovery (29% w/w), phenolic [13.54 ± 0.27 μg GAE/mg dry weight (DW)] and flavonoid (2.11 ± 0.10 μg QE /mg DW) content were recorded in methanol-distilled water (1:1) flower extract. HPLC-DAD analysis quantified substantial amount of six different polyphenols ranging from 0.081 to 37.95 μg/mg extract. Maximum total antioxidant and reducing potential were documented in methanol-distilled water and acetone-distilled water flower extracts (42.62 ± 0.47 and 24.38 ± 0.39 μg AAE/mg DW) respectively. Ethanol-chloroform root extract manifested highest free radical scavenging (IC₅₀ of 61.22 μg/mL) while 94.64% of the extracts showed cytotoxicity against brine shrimps. Ethanol leaf extract exhibited remarkable activity against THP-1 cell line (IC₅₀ = 8 ± 0.05 μg/mL) and protein kinases (31 mm phenotype bald zone).     

Cinnamomum cassia: an implication of serotonin reuptake inhibition in animal models of depression

The aim of the study was to explore the traditional use of Cinnamomum cassia against depression. The standardised methanolic extract of the bark of C. cassia was evaluated for antidepressant activity using various behavioural tests, i.e. tail suspension test (TST), forced swim test (FST) and locomotor activity test. The serotonergic and noradrenergic modulation was assessed using 5-hydroxytryptophan (5-HTP)-induced head twitches and yohimbine potentiation tests, respectively. The fluoxetine and phenelzine were used as positive controls in the study. The C. cassia extract significantly decreased the immobility time in TST (maximum effective dose tested was 50 mg/kg) while no effect was observed in FST and locomotor activity test. The extract significantly increased the 5-HTP-induced head twitches while yohimbine-induced lethality remained unaltered. The aforementioned results are similar to that caused by fluoxetine. The standardised methanolic extract of C. cassia demonstrated antidepressant activity that can be attributed to rise in serotonin levels.     

Antihyperglycemic,antihyperlipidemic and antioxidative evaluation of compounds from Senna sophera (L.) Roxb in streptozotocin-induced diabetic rats

Senna sophera (L.) Roxb (Common name: Kasunda, Baner) (Leguminosae) is used as traditional medicine in Africa and Asia. The compounds were isolated from methanolic extract of leaves of Senna sophera (MFCS). Compound A was identified as Hexahydroxy diphenic acid and Compound B as Kaempferol. MFCS administration to diabetic rats exhibited significant reduction in the blood sugar level and showed gain in body weight. After the treatment of 100 mg/kg of MFCS, the blood sugar level was reduced to 52.33 ± 2.83 mg/dl in comparison to the blood sugar level of vehicle control 76.66 ± 3.17 mg/dl, whereas treatment with 50 mg/kg of MFCS reduced the blood sugar level slightly (72.33 ± 2.42 mg/dl). The daily continuous administration of MFCS for a period of 21 days normalised the serum lipid levels confirming the effect of MFCS on diabetic hyperlipidemia. Treatment with MFCS also reversed the activities of antioxidants, which could be a result of decreased lipid peroxidation.     

Antioxidant,antimicrobial and urease inhibiting activities of methanolic extracts from Cyphostemma digitatum stem and roots

Cyphostemma digitatum stem and roots extracts were investigated for antioxidant, antimicrobial, urease inhibition potential and phytochemical analysis. Phytochemical screening of the roots and stem extract revealed the presence of secondary metabolites including flavonoids, alkaloids, coumarins, saponins, terpenoids, tannins, carbohydrates/reducing sugars and phenolic compounds. The methanolic extracts of the roots displayed highest antioxidant activity (93.518%) against DPPH while the crude methanolic extract of the stem showed highest antioxidant activity (66.163%) at 100 μg/mL concentration. The methanolic extracts of both stem and roots were moderately active or even found to be less active against the selected bacterial and fungal strains (Tables S2 and S3). The roots extract (methanol) showed significant urease enzyme inhibition activity (IC₅₀ = 41.2 ± 0.66; 0.2 mg/mL) while the stem extract was found moderately active (IC₅₀ = 401.1 ± 0.58; 0.2 mg/mL) against thiourea (IC₅₀ = 21.011; 0.2 mg/mL).     

Phytochemical characterisation and bioprospection for antibacterial and antioxidant activities of Lippia alba Brown ex Britton & Wilson (Verbenaceae)

Ethanol extract and fractions obtained from fresh and dry aerial parts of Lippia alba were examined in order to determine their phytochemical composition, antioxidant capacity and antibacterial activities. The ethanol extracts and fractions exhibited an antioxidant effect by the DPPH assay, especially samples of fresh plant. HPLC analysis of the ethyl acetate fractions identified the presence of phenolic acids and flavonoids. The ethanol extract and fractions showed activity against reference and multidrug-resistant strains of Staphylococcus aureus and Enterococcus faecalis (MIC range 2000–250 μg/mL). The hexane and dichloromethane fractions of fresh plant showed better activity against reference strains of Escherichia coli (MIC of 250 and 125 μg/mL, respectively), but all extracts and fractions were less active against multidrug-resistant strains of all the Gram-negative species evaluated. The results showed that the extract and fractions of L alba aerial parts showed antibacterial activity, even against multidrug-resistant Gram-positive bacteria, and antioxidant effect (DPPH assay).     

Acute and sub-acute toxicological evaluation of the alcoholic leaf and root extracts of Clerodendrum infortunatum L.

Leaf and root extracts of Clerodendrum infortunatum L. have been reported to show anthelmintic efficacy on a cestode parasite Raillietina tetragona. Its leaf showed no toxicity at 1000 mg/kg body weight but root toxicity study was not known. Therefore, our study is to test both leaf and root extracts at 2000 and 3000 mg/kg body weight concentration given orally for 15 days in four groups of Swiss albino mice, keeping another set as control (without plant extract). Weight and behaviour of mice were recorded daily. Feeding, movement pattern were normal in all treatments as that of control. Though body weight increase, there was no change in the relative organ weight. Biochemical and haematological studies revealed no significant change from control and no alteration in histopathological study of liver and kidney from that of control. The plant extracts thus shown to be safe for consumption.     

An insight into antimicrobial activity of the freshwater bryozoan Pectinatella magnifica

The antimicrobial activity of five crude extracts of the freshwater bryozoan Pectinatella magnifica (Leidy, 1851) was evaluated in vitro for the first time. P. magnifica acetone extract exhibited the highest antibacterial activity (minimum inhibitory concentrations (MIC) 0.004–0.350 mg/mL and MBC 0.007–0.500 mg/mL), while its methanol extract showed the most promising antifungal activity (MIC 0.03–0.12 mg/mL and MFC 0.06–0.25 mg/mL). Furthermore, at a concentration of 0.25 MIC, the methanol extract reduced biofilm formation of the bacterial strain Pseudomonas aeruginosa PAO1 in a considerable extent (59.14%). FTIR spectra of the most active extracts indicate the presence of carbonyl compounds, long-chain alcohols and/or sterols. According to the experimental data obtained, P. magnifica methanol extract may be considered as a good resource of novel natural products with potent antibiofilm activity against the bacterium well known for its resistance.     

Chemical characterisation and hepatoprotective potential of Cosmos sulphureus Cav. and Cosmos bipinnatus Cav.

This study was conducted to validate the hepatoprotective activity of Cosmos sulphureus and Cosmos bipinnatus. Aqua-methanolic extracts of both plants were evaluated for the presence of various phyto-constituents through HPLC. Different doses of both plant extracts were administered to rats for nine days. Standard control was silymarin 100 mg/kg. Paracetamol 1 gm/kg was administered 3 h post treatment on 9th day for induction of hepatotoxicity. Blood was collected for the evaluation of liver biochemical markers and livers were removed for histopathological evaluation 24 h post-paracetamol treatment. HPLC analysis revealed the presence of quercetin, gallic acid, caffeic acid and chlorogenic acid in both plant extracts. The extracts of both plants decreased the level of alanine aminotransaminase and total bilirubin significantly (p < 0.05), dose dependently and protected hepatocytes from paracetamol-induced hepatotoxicity. It can be concluded that both plants may possess hepatoprotective activity possibly due to the presence of quercetin and phenolic compounds.     

HPLC profiling of phenolics and flavonoids of Adonidia merrillii fruits and their antioxidant and cytotoxic properties

In this study the antioxidant and cytotoxicity activity of the Adonidia merrillii fruits were investigated using different solvent polarities (methanol, ethyl acetate and water). The results showed that the total phenolic and flavonoid contents of the methanolic extract was higher compare with other extract with respective values of 17.80 ± 0.45 mg gallic acid equivalents/g dry weight (DW) and 5.43 ± 0.33 mg rutin equivalents/g DW. Beside that The RP-HPLC analyses indicated the presence of gallic acid, pyrogallol, caffeic acid, vanillic acid, syringic acid, naringin and rutin. In the DPPH, NO2 and ABTS scavenging assays, the methanolic extract exhibited higher antioxidant activity as compared to the ethyl acetate and water extracts. The extracts exhibited moderate to weak cytotoxic activity in the assays using human hepatocytes (Chang liver cells) and NIH/3T3 (fibroblasts cell) cell lines. The findings showed the Adonidia merrillii fruit extracts to possess considerable antioxidant and cytotoxicity properties. The fruit, therefore, is a potential candidate for further work to discover antioxidant and cytotoxic drugs from natural sources.     

Effect of fruit extract on renal stone formation and kidney injury in rats

This study investigated the effect of oral administration of Cactus fruit extracts on calcium oxalate deposition, malondialdehyde (MDA) and superoxide dismutase (SOD) activity in rat model. About 42 rats were used for the study. The animals were divided into seven groups. Control group maintained on regular rat food and drinking water throughout the study period, whereas in other groups nephrolithiasis was induced by ethylene glycol. Rats in kidney stone group were sacrificed after 28 days and all remaining groups after 58 days. Treatment groups were treated with 1 and 100 mg/kg of aqueous and ethanolic extracts of Cactus fruit for 30 days. After treatment, SOD activity was increased and MDA was decreased significantly. CaOx depositions were decreased significantly, especially in ethanolic extract of Cactus fruit in high dose (100 mg/kg).     

LC Method for Determination and Pharmacokinetic Study of 5,6,7,8,3′,4′-Hexamethoxy-3-sulfonyl Flavone in Rat Plasma

A sensitive, specific and rapid high-performance liquid chromatography method was developed for determination of 5,6,7,8,3′,4′-hexamethoxy-3-sulfonyl flavone in rat plasma. A simple methanol-induced protein precipitation was applied to extract 5,6,7,8,3′,4′-hexamethoxy-3-sulfonyl flavone and Picroside II (the internal standard) from rat plasma. Chromatographic separation was achieved on a Hypersil ODS₂ analytical column (200 mm × 4.6 mm, 5 μm) with acetonitrile–0.04% triethylamine solution (adjusted to pH 5.8 using phosphoric acid) (24:76, v/v) as mobile phase. The calibration curves were linear over the range of 0.2–40 μg mL⁻¹. Absolute recoveries of 5,6,7,8,3′,4′-hexamethoxy-3-sulfonyl flavone were 82.7–95.9% from rat plasma. The intra- and inter-day relative standard deviation precisions were less than 5 and 9%, respectively. The method was successfully applied to the pharmacokinetic study of 5,6,7,8,3′,4′-hexamethoxy-3-sulfonyl flavone in rats after intravenous administration.

     

A new flavan from the Drynaria bonii H. Christ rhizomes

In Vietnam, the medicinal plant Drynaria bonii H. Christ is used for the treatment of osteoporosis, bone fractures, and stimulate the growth of hair, treat tinnitus (Ho 2002; Loi 2004). In this article, experiments were designed to investigate the proliferation activity of ethanol, n-hexane, chloroform, ethyl acetate and methanol extracts from D. bonii rhizomes on MG-63 human osteoblast-like cells. The results showed that methanol and hexane extracts had the ability to proliferate MG-63 cells at the concentration varying from 0.1 to 0.01 μg/mL. In particular, at the concentration of 0.01 μg/mL, hexane and methanol extracts illustrated the highest proliferation ratio with 9.31% and 6.16%, respectively. By column chromatography, a new compound named drynaether A (1) and five known compounds uracil (2), 4′-hydroxy-7-methoxyflavan (3), kaempferol (4), indole-3-carboxylic acid (5) and protocatechuic acid (6) were isolated and identified from the methanol extract.