Maculosin,a non-toxic antioxidant compound isolated from Streptomyces sp. KTM18

ContextStreptomyces species are prolific sources of bioactive secondary metabolites known especially for their antimicrobial and anticancer activities.ObjectiveThis study sought to isolate and characterize antioxidant molecules biosynthesized by Streptomyces sp. KTM18. The antioxidant potential of an isolated compound and its toxicity were accessed.Materials and methodsThe compound was purified using bioassay-guided chromatography techniques. Nuclear magnetic resonance (NMR) experiments were carried out for structure elucidation. The antioxidant potential of the isolated compound was determined using DPPH free radical scavenging assay. The toxicity of the isolated compound was measured using a brine shrimp lethality (BSL) assay.ResultsEthyl acetate extract of Streptomyces sp. KTM18 showed more than 90% inhibition of DPPH free radical at 50 µg/mL of the test concentration. These data were the strongest among 13 Streptomyces isolates (KTM12–KTM24). The active molecule was isolated and characterized as maculosin (molecular formula, C₁₄H₁₆N₂O₃ as determined by the [M + H]⁺ peak at 261.1259). The DPPH free radical scavenging activity of pure maculosin was higher (IC₅₀, 2.16 ± 0.05 µg/mL) than that of commercial butylated hydroxyanisole (BHA) (IC₅₀, 4.8 ± 0.05 µg/mL). No toxicity was observed for maculosin (LD₅₀, <128 µg/mL) in brine shrimp lethality assay (BSLA) up to the compound’s antioxidant activity (IC₅₀) concentration range. The commercial standard, berberine chloride, showed toxicity in BSLA with an LD₅₀ value of 8.63 ± 0.15 µg/mL.ConclusionsMaculosin may be a leading drug candidate in various cosmetic and therapeutic applications owing to its strong antioxidant and non-toxic properties.     

α-Amylase and dipeptidyl peptidase-4 (DPP-4) inhibitory effects of Melicope latifolia bark extracts and identification of bioactive constituents using in vitro and in silico approaches

ContextMelicope latifolia (DC.) T. G. Hartley (Rutaceae) was reported to contain various phytochemicals including coumarins, flavonoids, and acetophenones.ObjectiveThis study investigates the antidiabetic and antioxidant effects of M. latifolia bark extracts, fractions, and isolated constituents.Materials and methodsMelicope latifolia extracts (hexane, chloroform, and methanol), fractions, and isolated constituents with varying concentrations (0.078–10 mg/mL) were subjected to in vitro α-amylase and dipeptidyl peptidase-4 (DPP-4) inhibitory assay. Molecular docking was performed to study the binding mechanism of active compounds towards α-amylase and DPP-4 enzymes. The antioxidant activity of M. latifolia fractions and compounds were determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and β-carotene bleaching assays.ResultsMelicope latifolia chloroform extract showed the highest antidiabetic activity (α-amylase IC₅₀: 1464.32 μg/mL; DPP-4 IC₅₀: 221.58 μg/mL). Fractionation of chloroform extract yielded four major fractions (CF₁–CF₄) whereby CF₃ showed the highest antidiabetic activity (α-amylase IC₅₀: 397.68 μg/mL; DPP-4 IC₅₀: 37.16 μg/mL) and resulted in β-sitosterol (1), halfordin (2), methyl p-coumarate (3), and protocatechuic acid (4). Isolation of compounds 2–4 from the species and their DPP-4 inhibitory were reported for the first time. Compound 2 showed the highest α-amylase (IC₅₀: 197.53 μM) and β-carotene (88.48%) inhibition, and formed the highest number of molecular interactions with critical amino acid residues of α-amylase. The highest DPP-4 inhibition was exhibited by compound 3 (IC₅₀: 911.44 μM).Discussion and conclusionsThe in vitro and in silico analyses indicated the potential of M. latifolia as an alternative source of α-amylase and DPP-4 inhibitors. Further pharmacological studies on the compounds are recommended.     

Comparison of chemical profiles,antioxidation, inhibition of skin extracellular matrix degradation,and anti-tyrosinase activity between mycelium and fruiting body of Cordyceps militaris and Isaria tenuipes

ContextCordyceps militaris and Isaria tenuipes (Cordycipitaceae) are high-value fungi that are used for health-promoting food supplements. Since laboratory cultivation has begun for these fungi, increased output has been achieved.ObjectiveThis study compared the chemical profiles, antioxidant, anti-tyrosinase, and skin extracellular matrix degradation inhibition between mycelium and fruiting body of C. militaris and I. tenuipes.Materials and methodsThe antioxidative potential of 10% v/v aqueous infused extract from each fungus was separately investigated using 2,2-azinobis(3-ethylbenzo-thiazoline-6-sulphonic acid) (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant ability, and ferric thiocyanate methods. The inhibition against MMP-1, elastase, and hyaluronidase were determined to reveal their anti-wrinkle potential. Anti-tyrosinase activities were determined.ResultsC. militaris and I. tenuipes extracts were found to contain a wide range of bioactive compounds, including phenolics, flavonoids, and adenosine. A correlation was discovered between the chemical compositions and their biological activities. The extract from I. tenuipes fruiting body (IF) was highlighted as an extraordinary elastase inhibitor (IC₅₀ = 0.006 ± 0.004 mg/mL), hyaluronidase inhibitor (IC₅₀: 30.3 ± 3.2 mg/mL), and antioxidant via radical scavenging (ABTS IC₅₀: 0.22 ± 0.02 mg/mL; DPPH IC₅₀: 0.05 ± 0.02 mg/mL), thereby reducing ability (EC₁: 95.3 ± 4.8 mM FeSO₄/g extract) and lipid peroxidation prevention (IC₅₀: 0.40 ± 0.11 mg/mL). IF had a three-times higher EC₁ value than ascorbic acid and significantly higher elastase inhibition than epigallocatechin gallate.Discussion and conclusionsIF is proposed as a powerful natural extract with antioxidant and anti-wrinkle properties; therefore, it is suggested for further use in pharmaceutical, cosmeceutical, and nutraceutical industries.     

UPLC-PDA-ESI-QTOF-MS/MS fingerprint of purified flavonoid enriched fraction of Bryophyllum pinnatum; antioxidant properties,anticholinesterase activity and in silico studies

ContextBryophyllum pinnatum (Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments.ObjectivesThis study characterizes the constituents of B. pinnatum flavonoid-rich fraction (BPFRF) and investigates their antioxidant and anticholinesterase activity using in vitro and in silico approaches.Materials and methodsMethanol extract of B. pinnatum leaves was partitioned to yield the ethyl acetate fraction. BPFRF was isolated from the ethyl acetate fraction and purified. The constituent flavonoids were structurally characterized using UPLC-PDA-MS². Antioxidant activity (DPPH), Fe²⁺-induced lipid peroxidation (LP) and anticholinesterase activity (Ellman’s method) of the BPFRF and standards (ascorbic acid and rivastigmine) across a concentration range of 3.125–100 μg/mL were evaluated in vitro for 4 months. Molecular docking was performed to give insight into the binding potentials of BPFRF constituents against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE).ResultsUPLC-PDA-MS² analysis of BPFRF identified carlinoside, quercetin (most dominant), luteolin, isorhamnetin, luteolin-7-glucoside. Carlinoside was first reported in this plant. BPFRF significantly inhibited DPPH radical (IC₅₀ = 7.382 ± 0.79 µg/mL) and LP (IC₅₀ = 7.182 ± 0.60 µg/mL) better than quercetin and ascorbic acid. Also, BPFRF exhibited potent inhibition against AChE and BuChE with IC₅₀ values of 22.283 ± 0.27 µg/mL and 33.437 ± 1.46 µg/mL, respectively compared to quercetin and rivastigmine. Docking studies revealed that luteolin-7-glucoside, carlinoside and quercetin interact effectively with crucial amino acid residues of AChE and BuChE through hydrogen bonds.Discussion and conclusionsBPFRF possesses an excellent natural source of cholinesterase inhibitor and antioxidant. The material could be further explored for the potential treatment of oxidative damage and cholinergic dysfunction in Alzheimer’s disease.     

Ethanol extract of the mushroom Coprinus comatus exhibits antidiabetic and antioxidant activities in streptozotocin-induced diabetic rats

ContextEdible mushrooms have a long history of use in traditional Chinese or Japanese medicine. Coprinus comatus (O.F. Müll.) Pers. (Agaricaceae) contains antioxidant and antidiabetic agents.ObjectiveTo identify the benefits of ethanol extracts of the C. comatus fruit body in streptozotocin-induced hyperglycaemic rats by evaluating their blood glucose, glycosylated haemoglobin (HbA1c), insulin, glucagon-like peptide-1 (GLP-1), dipeptidyl peptidase-4 (DPP-4), and glutathione (GSH) levels, with and without extract administration.Materials and methodsWistar rats were either left untreated or were administered 45 mg/kg body weight (BW) streptozotocin; 45 mg/kg BW metformin; or 250, 500, or 750 mg/kg BW extract for 14 days. The blood glucose, GLP-1, DPP-4, GSH, insulin, and HbA1c levels were determined. Data were analysed using analysis of variance and Duncan’s multiple range tests.ResultsPreliminary data showed that administration of C. comatus ethanol extract dose of 250, 500, and 750 mg orally has no toxicity effects after 24 h administration. The ethanolic extract of fruiting body of C. comatus considerably reduced the rat’s fasting blood glucose levels 26.69%, and DPP-4 6.97% at dose of 750 mg. The extract reduced HbA1c 4–4.30%, increased GLP-1 71.09%, GSH 11.19% at dose of 500 mg, and increased insulin levels 13.83%. Extracts contain bioactive compounds such as flavonoid, alkaloid, terpenoids, vitamins C and E, rutin, and saponin.ConclusionsThe C. comatus extract can be used as herbal medicine that reduces diabetic symptoms. Further investigation on C. comatus extracts should be conducted with gas chromatography-mass spectrometry to characterise the bioactive compounds.     

Ethanol extract of Gynura bicolour reduces atherosclerosis risk by enhancing antioxidant capacity and reducing adhesion molecule levels

ContextGynura bicolour (Roxb. and Willd.) DC (Asteraceae) leaf is a common vegetable. Ethanol extracts of fresh G. bicolour leaves (GBEE) have several physiological effects, but studies on atherosclerosis are limited.ObjectiveWe investigated the oxidant scavenging ability and vascular adhesion molecule expression of these extracts.Materials and methodsThe antioxidant effects of 0.05–0.4 mg/mL GBEE were analyzed in vitro. Intracellular antioxidant capacity and adhesion molecule levels were detected in EA.hy926 cells pre-treated with 10–100 μg/mL GBEE for 8 h, then TNF-α for 3 h. The antioxidant capacity of red blood cells and the adhesion molecule levels in the thoracic aorta were detected in high-fat diet (HFD)-fed Sprague–Dawley rats treated with GBEE for 12 weeks.ResultsThe in vitro EC₅₀ values of GBEE based on its DPPH radical-scavenging ability, reducing power, and ferrous ion-chelating ability were 0.20, 3.21 and 0.49 mg/mL, respectively. In TNF-α-treated EA.hy926 cells, the thiobarbituric acid-reactive substance levels were decreased after 10, 50, or 100 μg/mL GBEE treatments (IC₅₀: 19.1 mg/mL). When HFD-fed rats were co-treated with GBEE, the GBEE-H group exhibited 25% higher glutathione levels than the HFD group (p < 0.05). E-selectin, intercellular adhesion molecule-1, and vascular cell adhesion protein-1 levels were decreased in TNF-α-treated EA.hy926 cells after GBEE treatment (by approximately 11–73%; p < 0.05), and the above three adhesion molecules levels were decreased in HFD-fed rats with combined GBEE treatment (by approximately 30–77%; p < 0.05).ConclusionsGBEE can protect the vascular endothelium by reducing adhesion molecule expression and regulating antioxidants. It may have the potential to prevent atherosclerosis.     

16α-Hydroxy-(–)-kauranoic Acid: A Selectively Cytotoxic Diterpene from Annona bullata

Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16-hydroxy-(–)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED₅₀ 8.25 × 10^–2 µg/ml) and selective cytotoxicity against A-549 (lung) cells in our panel of human tumor cells.     

Pharmacological effects of Artocarpus lakoocha methanol extract on inhibition of squalene synthase and other downstream enzymes of the cholesterol synthesis pathway

ContextArtocarpus lakoocha Roxb. (Moraceae) is reported to possess antioxidant, anti-inflammatory, and anti-skin ageing agents.ObjectiveThis study evaluates the pharmacological effects of A. lakoocha leaves methanol extract on enzymes involved in the cholesterol synthesis pathway in high-fat diet-induced hyperlipidemic rats.Materials and methodsTwenty-four male Wistar rats, weighing approximately 180–220 g, were divided into four groups: control, diseased (hyperlipidemic), A. lakoocha leaves extract treated, and simvastatin treated. The rats were fed with high-fat diet for 2 months to induce hyperlipidaemia, afterward, experimental groups received A. lakoocha leaves methanol extract (250 mg/kg) and simvastatin (10 mg/kg) orally until the 89^th day of the experiment, while the diseased group continued to receive high-fat diet along with normal saline.ResultsIt was found that A. lakoocha extract significantly lowered the serum total cholesterol, triglycerides, and low-density lipoprotein (LDL) levels, while effectively increasing serum high-density lipoprotein (HDL) levels as compared to the diseased group (p ≤ 0.05). The mRNA expression levels of squalene synthase and HMG-CoA reductase were found to be effectively down-regulated after the treatment with A. lakoocha leaves extract (17.45 ± 2.48 vs. 31.91 ± 5.292 and 5.85 ± 3.164 vs. 37.37 ± 6.492) and simvastatin (7.148 ± 0.76 vs. 31.91 ± 5.292, and 3.098 ± 2.09 vs. 37.37 ± 6.492) as compared to the diseased group.Discussion and ConclusionsThe results suggested that A. lakoocha leaves extract have observable beneficial effects on inhibition of enzymes involved in cholesterol synthesis pathway and improve lipid profile analogous to simvastatin.     

Evaluation of native and exotic Brazilian plants for anticancer activity

Native and exotic Brazilian plants collected in the State of Minas Gerais were evaluated for their anticancer potential. Methanol extracts from leaves of 51 plant species were tested for cytotoxicity against four tumor cell lines: B16 (murine skin), HL-60 (human leukemia), MCF-7 (human breast), and HCT-8 (human colon). Plant extracts that exhibited IC₅₀ values less than 30 μg/ml against any tumor cell line were tested on sea urchin egg development and mouse erythrocytes. In addition, all extracts were evaluated for their general toxicity using the brine shrimp lethality assay. The most active extracts against the tumor cells were those obtained from Lantana fucata, Copaifera langsdorffii, and Momordica charantia. These three extracts inhibited sea urchin development from the first cleavage, but those from C. langsdorffii and M. charantia were very active against mouse erythrocytes. Only the L. fucata extract presented no hemolytic activity. Consequently, although the extracts of L. fucata, M. charantia, and C. langsdorffii could be useful in the development of new anticancer products, the first of these extracts is the most promising since it did not present unspecific toxicity, as suggested by negative results obtained with brine shrimp lethality and mouse erythrocytes assays.     

Antimicrobial and cytotoxic constituents from leaves of Sapium baccatum

Six compounds, namely, Lupeol (1), Betulin (2), β-Taraxerol (3), Taraxerone (4), Stigmasterol (5) and β-Sitosterol (6) were isolated from the petroleum ether extract of the leaves of Sapium baccatum based on spectroscopic evidence. Lupeol (1), Betulin (2) and Stigmasterol (5) were isolated for the first time from this plant. The cytotoxic potential of the different solvent extracts (methanol, petroleum ether, carbon-tetrachloride and dichloromethane); six column fractions (F-4, F-7, F-10, F-12, F-18 and F-22) of petroleum ether extract and three pure compounds 1, 4 and 6 were determined by using brine shrimp lethality bioassay. The LC₅₀ of all the tested samples were showed to be lethal to brine shrimp nauplii. However, petroleum ether, carbon-tetrachloride extract, column fractions F-4 and F-18 of petroleum ether extract and pure compound 6 showed quite potent activity in brine shrimp lethality bioassay with LC₅₀ 1.33, 1.35, 1.40, 1.58 and 1.58 μg/ml, respectively. These result suggested that they might be contain antitumor or pesticidal activity. Further, the methanol extract and four column fractions (F-7, F-12, F-18 and F-22) of petroleum ether showed significant activity against the tested microorganisms.     

Two New Triterpene Glycosides from Dendrocalamus strictus

Abstract

The methanol extract of Gracilaria changii. B.M. Xia &; I.A. Abbott (Gracilariaciae), which exhibited antimicrobial activity, was tested for in vivo. brine shrimp lethality and in vitro.anticancer cell line activity. Both toxicity tests [brine shrimp test with LC₅₀ value 4.28 mg/mL (12 h), 3.13 mg/mL (24 h) and anticancer cell line activity with IC₅₀ value 44.10 μ g/mL] exhibited no significant toxicity result. These alga extracts, with high LC₅₀ and IC₅₀ values, are potential sources for novel antimicrobial compounds.     

Chemical composition,antioxidant, antitumor,anticancer and cytotoxic effects of Psidium guajava leaf extracts

Context Psidium guajava L. (Myrtaceae) leaves are used in traditional medicines for the treatment of cancer, inflammation and other ailments.

Objective The current study explores scientific validation for this traditional medication.

Materials and methods We used ferric-reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picryl hydrazil (DPPH) assays to estimate antioxidant activity of P. guajava leaf extracts (methanol, hexane and chloroform). Antitumour and in vivo cytotoxic activities were determined using potato disc assay (PDA) and brine shrimp lethality assay, respectively. Three human carcinoma cell lines (KBM5, SCC4 and U266) were incubated with different doses (10–100?μg/mL) of extracts and the anticancer activity was estimated by MTT assay. NF-κB suppressing activity was determined using electrophoretic mobility shift assay (EMSA). Chemical composition of the three extracts was identified by GC-MS. Total phenolic and flavonoid contents were measured by colorimetric assays.

Results and discussions The order of antioxidant activity of three extracts was methanol?>?chloroform?>?hexane. The IC₅₀ values ranged from 22.73 to 51.65?μg/mL for KBM5; 22.82 to 70.25?μg/mL for SCC4 and 20.97 to 89.55?μg/mL for U266 cells. The hexane extract exhibited potent antitumour (IC_50? value?=_?65.02?μg/mL) and cytotoxic (LC_50? value?=_?32.18?μg/mL) activities. This extract also completely inhibited the TNF-α induced NF-κB activation in KBM5 cells. GC-MS results showed that pyrogallol, palmitic acid and vitamin E were the major components of methanol, chloroform and hexane extracts. We observed significant (p?<?0.05) difference in total phenolic and flavonoid contents of different solvent extracts.

Conclusion The present study demonstrates that P. guajava leaf extracts play a substantial role against cancer and down-modulate inflammatory nuclear factor kB.     

Angelica gigas root ameliorates ischaemic stroke-induced brain injury in mice by activating the PI3K/AKT/mTOR and MAPK pathways

ContextTraditionally, the root of Angelica gigas Nakai (Umbelliferae), has long been used to treat ischaemic diseases and is considered safe in humans.ObjectiveTo investigate the neuroprotective effects of a methanol extract of A. gigas root (AGmex) on the middle cerebral artery occlusion (MCAO)-induced brain injury in mice, and the underlying mechanisms.Materials and methodsTwo hours of transient MCAO (tMCAO) was induced in C57BL/6 mice (MCAO control group and AGmex groups), AGmex was administered to the AGmex group at 300-3,000 mg/kg bw at 1, 1, and 24 h before tMCAO or at 1000 mg/kg bw at 1 h before and after tMCAO. Infarction volumes, tissue staining, and western blotting were used to investigate the mechanism underlying the neuroprotective effects of AGmex.ResultsThe median effective dose (ED₅₀) could not be measured because the AGmex treatment did not reduce the infarction volume caused by 2 h of tMCAO to within 50%; however, pre-treatment with AGmex twice at 1,000 mg/kg bw before tMCAO significantly reduced the infarction volumes. The proteins related to cell growth, differentiation, and death were upregulated by this treatment, and the major recovery mechanisms appeared to involve the attenuation of the mitochondrial function of Bcl-2/Bax and activation of the PI3K/AKT/mTOR and MAPK signalling pathways in ischaemic neurons.ConclusionsThis study provides evidence supporting the use of A. gigas root against ischaemic stroke and suggests a novel developmental starting point for the treatment of ischaemic stroke.     

Ocimum sanctum,Zingiber officinale,and Piper nigrum extracts and their effects on gut microbiota modulations (prebiotic potential), basal inflammatory markers and lipid levels: oral supplementation study in healthy rats

ContextOcimum sanctum Linn (Labiatae) (OS), Zingiber officinale Rose (Zingiberaceae) (ZO), and Piper nigrum Linn (Piperaceae) (PN) are used in traditional medicine as immunomodulator, anti-inflammatory, and bioavailability enhancer agents.ObjectiveActive phytoconstituents of OS, ZO, PN hydro-alcoholic extracts and their effects on gut microbiota, basal inflammation and lipid profile were investigated in rats.Materials and methodsActive phytoconstituents of extracts were analysed using HPLC and GC-MS. SD rats were supplemented with individual/combined extracts (OS-850; ZO-500; PN-100 mg/kg Bw) and Fructooligosaccharide (standard prebiotic-5g/kg-Bw), orally for 30 days. Haematology, lipid profile, LPS, CRP, IL-6, insulin and histology of vital organs were analysed. Caecal bacterial levels were assessed by RT-PCR.ResultsHigh content of phenolic compounds luteolin-7-O-glucoside (430 ± 2.3 mg/100g), gallic acid (84.13 ± 1.2 mg/100 g) and flavones (88.18 ± 1.8 mg/100 g) were found in OS, ZO, and PN, respectively. Combined extract was rich in luteolin-7-O-glucoside (266.0 ± 1.80 mg/100 g). Essential oils including methyleugenol (13.96%), 6-shogaol (11.00%), piperine (18.26%), and cyclopentasiloxane (10.06%) were higher in OS, ZO, PN and combined extract. Higher levels of caecal Lactobacillus (1.7–3.4-fold), Bifidobacterium (5.89-28.4-fold), and lower levels of Firmicutes (0.04–0.91-fold), Bacteroides (0.69–0.88-fold) were noted among extracts and FOS supplemented rats. Significant (p < 0.05) decrease in plasma lipid profile and LPS was noted in all supplemented rats.Discussion and conclusionsThe current study could be first of its kind in exploring prebiotic potential of OS, ZO, PN and their effect on native gut bacterial population.     

Moringa oleifera seed ethanol extract and its active component kaempferol potentiate pentobarbital-induced sleeping behaviours in mice via a GABAergic mechanism

ContextMoringa oleifera Lam. (Moringaceae) (MO) is an important food plant that has high nutritional and medical value. However, there is limited information on whether its seeds can improve sleep.ObjectiveThis study investigated the effects of MO seed ethanol extracts (EEMOS) on sleep activity improvement and examined the underlying mechanisms.Materials and methodsMale ICR mice were placed into six groups (n = 12) and treated as follows: Control (sodium carboxymethyl cellulose, 20 mL/kg), estazolam tablets (2 mg/kg), EEMOS (1, 2 g/kg) and kaempferol (1, 2 mg/kg). These samples were successively given intragastric for 14 d. Locomotor activity assay, pentobarbital-induced sleeping and pentetrazol-induced seizures tests were utilized to examine the sedative-hypnotic effects (SHE) of EEMOS.ResultsCompared with the control group, the results revealed that EEMOS (2 g/kg) and KA (2 mg/kg) possessed good SHE and could significantly elevate the levels of γ-aminobutyric acid and reduce the levels of glutamic acid in the mouse hypothalamus (p < 0.05). Moreover, SHE was blocked by picrotoxin, flumazenil and bicuculline (p < 0.05). EEMOS (2 g/kg) and KA (2 mg/kg) significantly upregulated the protein expression levels of glutamic acid decarboxylase-65 (GAD₆₅) and α₁-subunit of GABA_A receptors in the hypothalamus of mice (p < 0.05), not affecting glutamic acid decarboxylase-67 (GAD₆₇) and γ₂-subunit expression levels (p > 0.05). Additionally, they cause a significant increase in Cl^- influx in human cerebellar granule cells at a concentration of 8 µg/mL (p  <  0.05).Discussion and conclusionsThese findings demonstrated that EEMOS could improve sleep by regulating GABA_A-ergic systems, and encourage further clinical trials to treat insomnia.     

Antibacterial,Antifungal, and Cytotoxic Activities of 11 Solanaceae Plants from Colombian Biodiversity

Abstract

The hexane, dichloromethane, and methanol extracts of 11 Solanaceae plants collected in Regional Natural Park Ucumarí (RNPU) Colombia were evaluated for their antibacterial and antifungal activities through the agar-well diffusion method and for cytotoxic activity by the brine shrimp lethality assay. In general, the methanol plant extracts were more bioactive in the three different tests performed in this work. Under conditions and concentrations of the plant extracts evaluated in this research, the cytotoxic activities against brine shrimp Artemia salina. (Leach) larvae were the strongest compared with the antibacterial or the antifungal activities. The strongest cytotoxic activities were observed with the methanol extracts from Browallia speciosa. Hook (LC₅₀ 0.01 mg/ml) and Deprea glabra. (Standl.) A.T. Hunziker (LC₅₀ 0.01 mg/ml). The three extracts from Solanum deflexiflorum. Bitter (MIC 0.31 mg/ml) and the dichloromethane extract from Solanum leucocarpun. Dunal (MIC 0.31 mg/ml) were more bioactive against the Gram-positive bacteria Bacillus subtilis.. The methanol extract from Lycianthes synanthera. (Send.) Bitter exhibited good antimycotic activities against Candida albicans. and Fusarium solani. both with a MIC of 0.62 mg/ml.     

Bioactivity of Extractives from Stachytarpheta urticaefolia

The n-hexane and methanol extracts of Stachytarpheta urticaefolia leaves exhibited significant antinociceptive effects (p &lt; 0.01) in acetic acid-induced writhing model at a dose of 250 mg/kg b.w. Two compounds isolated from the plant, ipolamiide (1) and α-spinasterol (2), were also found to be potent inhibitors of acetic acid-induced writhing on mice at 50 mg/kg b.w. (p &lt; 0.01). Abortifacient activity was demonstrated within 20 h of administration of a methanolic leaf extract at 200 mg/kg b.w. The methanolic leaf extract and compounds 1 and 2 were also tested for in vitro antibacterial activities against 18 bacterial strains. The extract showed mean zones of inhibition ranging from 17 to 30 mm at 500 µg/disk, but the compounds demonstrated only mild or no in vitro antibacterial activity even at 400 µg/disk. Finally, in a cytotoxicity study, the n-hexane and methanol extracts of leaves and root bark of the plant and the purified compounds (1, 2) exhibited LC₅₀ values of 5.42, 4.42, 17.15, 5.38, 3.93, and 13.65 µg/ml, respectively, against the brine shrimp nauplii, whereas the positive control, vincristine sulfate, showed an LC₅₀ of 0.583 µg/ml.     

Brine shrimp toxicity of various polarities leaves and fruits crude fractions of Ziziphus jujuba native to Oman and their antimicrobial potency

Ziziphus jujuba (Z. jujube) is a herb used traditionally for the treatment of different aliment since ancient times, however, the scientific information on this plant is still insufficient. The pure active chemical compounds and crude extracts of Z. jujube can be used in food, formulated pharmaceutical products, natural antioxidant, antibiotics, anticancer agent and preservatives. Therefore, the objective of this work is to determine the cytotoxic and antimicrobial activities of different polarity of crude fractions of locally grown Z. jujube by applying brine shrimp lethality and agar gel disc diffusion bioassay. The cytotoxic result reveals that all prepared crude fractions from the leaves and fruits were lethal to all shrimp larvae at a concentration of 1000 μg/ml. Among the leaves crude fractions, butanol extract showed the highest cytotoxic activity with LC₅₀ value of 8.69 μg/ml, whereas the lowest activity was in chloroform crude extract with LC₅₀ value of 45.12 μg/ml. Similarly, in fruits, the highest activity was in ethyl acetate extract with an LC₅₀ value of 11.62 μg/ml and the lowest was in water extract with an LC₅₀ value of 149.28 μg/ml. The methanol and its corresponding fractions were displayed moderate antimicrobial activity against Gram (+ and ?) bacteria at various concentrations with a zone of inhibition range of 0–17 mm. Therefore, the active polar crude fraction of Z. jujuba or its pure component could be candidates for use as safe, effective and comparatively cheap antibiotics and anticancer agents.     

Evaluation of the Ethnomedical Claims of Murraya koenigii.

Abstract

Based on sethnomedicine, Murraya koenigii. (L.) Spreng. is used as a stimulant, antidysentery, and for the management of diabetes mellitus. Twelve carbazole alkaloids were isolated from the stem, seed, and leaf of the plant growing in Nigeria and Sri Lanka. The methanol extracts were devoid of hypoglycemic activity, and some isolates decreased insulin secretion when they were subjected to both in vivo. and in vitro. (insulin secretion from INS-1 cells) antidiabetic tests. The cytotoxicity of the leaf and stem methanol extracts determined by the brine shrimp lethality bioassay were LC₅₀ 61.5 and 14.5?µg/ml, respectively. These extracts caused CNS depression in albino mice at the dose levels of 25–400?mg/kg. Also, they had an IC₅₀ of 34.0 and 35.0?µg/ml at 24?h, respectively, against trichomonas. These results confirmed the use of the plant as an antidysentery caused by trichomonas but refute the antidiabetic and stimulant ethnomedical claims for the plant. The differences observed in their alkaloidal composition suggested probable influence of geographical location on the elaboration of carbazole alkaloids in the plant and differences in the localization of carbazole alkaloids in the plant parts.     

Comparative pharmacokinetic analysis of raw and steamed Panax notoginseng roots in rats by UPLC-MS/MS for simultaneously quantifying seven saponins

ContextAfter being steamed, the restorative effects of Panax notoginseng (Burk.) F. H. Chen (Araliaceae) will be strengthened. However, the underlying mechanism remains elusive.ObjectiveTo compare the pharmacokinetics of ginsenosides Rg₁, Rb₁, Rd, Re, Rg₅, Rk₁, notoginsenoside R₁ (GRg₁, GRb₁, GRd, GRe, GRg₅, GRk₁ and NGR₁) in the raw and steam-processed P. notoginseng (RPN and SPN).Materials and methodsThe pharmacokinetics of seven components after oral administration of SPN and RPN extracts (1.0 g/kg) were investigated, respectively, in SD rats (two groups, n = 6) using UPLC-MS/MS.ResultsThe approach elicited good linear regression (r² > 0.991). The accuracy, precision and stability were all within ± 15%. The extraction recoveries and matrix effects were 75.0–100.8% and 85.1–110.3%, respectively. Compared with the RPN group, AUC_0–t of GRg₁ (176.63 ± 42.49 ng/h/mL), GRb₁ (5094.06 ± 1453.14 ng/h/mL), GRd (1396.89 ± 595.14 ng/h/mL), and NGR₁ (135.95 ± 54.32 ng/h/mL), along with C_max of GRg₁ (17.41 ± 5.43 ng/mL), GRb₁ (361.48 ± 165.57 ng/mL), GRd (62.47 ± 33.65 ng/mL) and NGR₁ (23.97 ± 16.77 ng/mL) decreased remarkably with oral administration of the SPN extracts, while GRe showed no significantly difference. Of note, GRg₅ and GRk₁ could not be detected in the plasma.ConclusionsInfluence of the processing reduced the systemic exposure levels to GRg₁, GRb₁, GRd and NGR₁. It is the first report of comparative pharmacokinetic study of multiple saponins analysis after oral administration of RPN and SPN extract, which might be helpful for further studies on its steam-processing mechanism.