An anti-mycobacterial bisfunctionalized sphingolipid and new bromopyrrole alkaloid from the Indonesian marine sponge Agelas sp.
AbstractIn the course of our studies on anti-mycobacterial substances from marine organisms, the known dimeric sphingolipid, leucettamol A (1), was isolated as an active component, together with the new bromopyrrole alkaloid, 5-bromophakelline (2), and twelve known congeners from the Indonesian marine spongeAgelas sp. The structure of2 was elucidated based on its spectroscopic data. Compound1 and its bis TFA salt showed inhibition zones of 12 and 7  mm againstMycobacterium smegmatis at 50  μg/disk, respectively, while theN,N ’-diacetyl derivative (1a) was not active at 50  μg/disk. Therefore, fre...
Source: Journal of Natural Medicines - March 31, 2017 Category: Drugs & Pharmacology Source Type: research

Two new polyhydroxyl polyacetylenes from fruits of Herpetospermum caudigerum
AbstractTwo new polyhydroxy polyacetylenes, herpecaudenes A and B (1 and2), were isolated from the ethanol extract of fruits ofHerpetospermum caudigerum, an important Tibetan medicine. The structures of them were elucidated on the basis of extensive spectroscopic methods including UV, IR, HRESIMS,1H and13C NMR, HMBC, HSQC, and1H-1H COSY. Compound2 showed significant inhibitory effects on NO production in LPS-activated RAW 264.7 macrophages with IC50 values of 7.05  ± 1.59 µM. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - March 29, 2017 Category: Drugs & Pharmacology Source Type: research

Bioactive flavonoids from Flos Sophorae
AbstractThree new flavonoid glycosides —soyaflavonosides A (1), B (2), and C (3) —together with 23 known ones were obtained from the 70% EtOH extract of Flos Sophorae (Sophora japonica, Leguminosae). Their structures were elucidated by chemical and spectroscopic methods. Among the known isolates,14,18,20,22, and26 were isolated from the Sophora genus for the first time;12,19,24, and25 were obtained from the species firstly. Moreover, NMR data for compounds18 and26 are reported for the first time here. Meanwhile, compounds4,8–13,15,16,19,21, and22 presented obvious inhibitory effects on TG accumulation in ...
Source: Journal of Natural Medicines - March 29, 2017 Category: Drugs & Pharmacology Source Type: research

Iriomoteolides-9a and 11a: two new odd-numbered macrolides from the marine dinoflagellate Amphidinium species
AbstractIriomoteolides-9a (1) and 11a (2), new 15- and 19-membered macrolides, respectively, have been isolated from the marine dinoflagellateAmphidinium species (strain KCA09052). Compounds1 and2 were obtained from the extracts of the algal cells inoculated in the PES and TKF seawater medium, respectively. The structures of1 and2 were assigned on the basis of detailed NMR analyses. Compounds1 and2 exhibited cytotoxic activity against human cervix adenocarcinoma HeLa cells. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - March 2, 2017 Category: Drugs & Pharmacology Source Type: research

Chemical structures of constituents from the leaves of Polyscias balfouriana
AbstractA new pyrrolidine derivative, (5S)-hydroxyethyl 2-oxopyrrolidine-5-carboxylate (1), a new flavonol glycoside, tamaraxetin 3,7-di-O-α-l-rhamnopyranoside (2), and a new triterpene saponin, polyscioside A methyl ester (3), along with six known compounds (4–9) were isolated from the leaves ofPolyscias balfouriana. Their chemical structures were elucidated on the basis of extensive spectroscopic analysis. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

Two new secolignans with in vitro anti-inflammatory activities from Urtica fissa rhizomes
AbstractTwo new secolignans, urticin A (1) and urticin B (2), were isolated from the ethanol extract ofUrtica fissa rhizomes. Their structures were elucidated on the basis of extensive spectroscopic evidence (UV, IR, HR-ESI –MS, and NMR). Urticin A and urticin B possessed in vitro anti-inflammatory activities, which significantly inhibited the TNF-α and NO release induced by LPS in RAW 264.7 cells. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - February 27, 2017 Category: Drugs & Pharmacology Source Type: research

Taxonomic examination of longgu (Fossilia Ossis Mastodi, “dragon bone”) and a related crude drug, longchi (Dens Draconis, “dragon tooth”), from Japanese and Chinese crude drug markets
AbstractLonggu ( “dragon bone,”Ryu-kotsu, Fossilia Ossis Mastodi, or Os Draconis) is the only fossil crude drug listed in the Japanese Pharmacopoeia. All longgu in the current Japanese market is imported from China, where its resources are being depleted. Therefore, effective countermeasures are urgently needed to prevent resource depletion. One possible solution is the development of a substitute made from bones of contemporary animals that are closely related to the original animal source of the current longgu. However, no research has been conducted on the original animal source of longgu, except for a repor...
Source: Journal of Natural Medicines - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Apium graveolens extract influences mood and cognition in healthy mice
This study investigates the effect of a sub-acute administration ofA. graveolens on cognition and anti-depression behaviors via antioxidant and related neurotransmitter systems in mice brains. Cognition and depression was assessed by various models of behavior. The antioxidant system of glutathione peroxidase (GPx), % inhibition of superoxide anion (O2−), and lipid peroxidation were studied. In addition, neurochemical parameters including acetylcholinesterase (AChE) and monoamine oxidase-type A (MAO-A) were also evaluated. Nine groups of male mice were fed for 30  days with different substances—a control, ...
Source: Journal of Natural Medicines - February 15, 2017 Category: Drugs & Pharmacology Source Type: research

Anti-obesity activity of Yamabushitake ( Hericium erinaceus ) powder in ovariectomized mice, and its potentially active compounds
In this study, using ovariectomized mice as a model of menopause, we investigated the anti-obesity effect of this mushroom in menopause. Mice fed diets containingH. erinaceus powder showed significant decreases in the amounts of fat tissue, plasma levels of total cholesterol, and leptin. To determine the mechanism, groups of mice were respectively fed a diet containingH. erinaceus powder, a diet containing ethanol extract ofH. erinaceus, and a diet containing a residue of the extract. As a result,H. erinaceus powder was found to increase fecal lipid levels in excreted matter. Further in vitro investigation showed that etha...
Source: Journal of Natural Medicines - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Puerarin may protect against Schwann cell damage induced by glucose fluctuation
AbstractPuerarin is one of the major active ingredients in Gegen, a traditional Chinese herb that has been reported to have a wide variety of beneficial pharmacology functions. Previous studies have implicated that the damaging effects of hyperglycemia resulting from oxidative stress and glucose fluctuation may be more dangerous than constant high glucose in the development of diabetes-related complications. The present study focuses on the effects of puerarin on glucose fluctuation-induced oxidative stress-induced Schwann cell (SC) apoptosis in vitro. Primarily cultured SCs were exposed to different conditions and the eff...
Source: Journal of Natural Medicines - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Inhibiting reactive oxygen species-dependent autophagy enhanced baicalein-induced apoptosis in oral squamous cell carcinoma
In this study, we found that baicalein induced significant apoptosis in OSCC cells Cal27. In addition to showing apoptosis induction, we also demonstrated baicalein-induced autophagic response in Cal27 cells. Moreover, pharmacologically or genetically blocking autophagy enhanced baicalein-induced apoptosis, indicating the cytoprotective role of autophagy in baicalein-treated Cal27 cells. Importantly, we found that baicalein triggered reactive oxygen species (ROS) generation in Cal27 cells. Furthermore,N-acetyl-cysteine, a ROS scavenger, abrogated the effects of baicalein on ROS-dependent autophagy. Therefore, we found that...
Source: Journal of Natural Medicines - February 7, 2017 Category: Drugs & Pharmacology Source Type: research

p -Hydroxyacetophenone suppresses nuclear factor- κB-related inflammation in nociceptive and inflammatory animal models
This study investigated the antioxidative, antinociceptive, and anti-inflammatory effects of HAP, and probed its possible molecular mechanisms. Our results revealed that HAP (80  mg/kg, intraperitoneally) in vivo reduced the acetic acid-induced writhing response and formalin-induced licking time. Moreover, in the λ-carrageenan-induced acute-inflammatory paw edema model in mice, HAP significantly improved hind paw swelling and neutrophil infiltration. In a homogenized paw tissue examination, HAP attenuated pro-inflammatory cytokines, such as tumor necrosis factor-α, interleukin-1β, and interleukin-6. ...
Source: Journal of Natural Medicines - February 1, 2017 Category: Drugs & Pharmacology Source Type: research

A novel lectin from Artocarpus lingnanensis induces proliferation and Th1/Th2 cytokine secretion through CD45 signaling pathway in human T lymphocytes
This study demonstrates the involvement of CD45-mediated signaling in ALL-induced T lymphocyte proliferation and Th1/Th2 cytokine secretion through activation of p38 and ERK. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - January 21, 2017 Category: Drugs & Pharmacology Source Type: research

Koumine exhibits anxiolytic properties without inducing adverse neurological effects on functional observation battery, open-field and Vogel conflict tests in rodents
AbstractKoumine, an active alkaloid of neurotoxic plantGelsemium, has been focused on its therapeutic uses, especially in central nervous system. Nevertheless, less is known about the neurological effects of koumine, which hampers its potential therapeutic exploitation. Moreover, as the anxiolytic potential ofGelsemium has raised many critical issues, its active principles on the anxiolytic and other neurological effects need to be further investigated. Here, we used functional observation battery (FOB) of mice to systematically measure the neurological effects of koumine at the effective doses, and then further confirmed ...
Source: Journal of Natural Medicines - January 19, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of oleuropein on pentylenetetrazol-induced seizures in mice: involvement of opioidergic and nitrergic systems
AbstractOleuropein, a well-known olive polyphenol, has been shown to mediate neuroprotection in Alzheimer ’s disease and cerebral ischemia. We investigated the effects of oleuropein on pentylenetetrazole (PTZ)-induced seizures in male NMRI mice, with diazepam as the standard drug. We also examined the possible involvement of opioidergic/nitrergic pathways in the probable effects of oleuropein. Intrape ritoneal (i.p.) administration of different doses of oleuropein (10, 20 and 30 mg/kg) significantly increased the seizure threshold 60 min prior to induction of seizure, in a dose-dependent manner. Administrat...
Source: Journal of Natural Medicines - January 19, 2017 Category: Drugs & Pharmacology Source Type: research

Tubulin polymerization-stimulating activity of Ganoderma triterpenoids
This study was conducted to evaluate the effect ofGanoderma triterpenoids on tubulin polymerization. A total of twenty-four compounds were investigated using an in vitro tubulin polymerization assay. Results showed that most of the studied triterpenoids exhibited microtuble-stabilizing activity to different degrees. Among the investigated compounds, ganoderic acid T-Q, ganoderiol F, ganoderic acid S, ganodermanontriol and ganoderic acid TR were found to have the highest activities. A structure –activity relationship (SAR) analysis was performed. Extensive investigation of the SAR suggests the favorable structural fea...
Source: Journal of Natural Medicines - January 11, 2017 Category: Drugs & Pharmacology Source Type: research

Partial contribution of Rho-kinase inhibition to the bioactivity of Ganoderma lingzhi and its isolated compounds: insights on discovery of natural Rho-kinase inhibitors
AbstractRecent studies identified Rho-kinase enzymes (ROCK-I and ROCK-II) as important targets that are involved in a variety of diseases. Synthetic Rho-kinase inhibitors have emerged as potential therapeutic agents to treat disorders such as hypertension, stroke, cancer, diabetes, glaucoma, etc. Our study is the first to screen the total ethanol extract of the medicinal mushroomGanoderma lingzhi with thirty-five compounds for Rho-kinase inhibitory activity. Moreover, a molecular binding experiment was designed to investigate the binding affinity of the compounds at the active sites of Rho-kinase enzymes. The structure &nd...
Source: Journal of Natural Medicines - January 10, 2017 Category: Drugs & Pharmacology Source Type: research

Stereo- and region-specific biotransformation of physapubescin by four fungal strains
AbstractBiotransformations of physapubescin (1) were performed by four fungal strains —Mucor subtilissimus AS 3.2454,Mucor polymorphosporus AS 3.3443,Aspergillus niger AS 3.795, andSyncephalastrum racemosum AS 3.264. Four metabolites were prepared in the biotransformation process of1, and their structures were elucidated as 15α-acetoxy-5,6β:22,26:24,25-triepoxy-26α-hydroxy-3β-methoxy 4β-hydroxyergost-1-one (2), 15α-acetoxy-5,6β:22,26-diepoxy-4β,24β,25α,26(α,β)-tetrahydroxyergost-3β-methoxy-1-one (3a/3b), 15α-acetoxy-5,6β:22,26-diepoxy-4&...
Source: Journal of Natural Medicines - January 10, 2017 Category: Drugs & Pharmacology Source Type: research

Lupinifolin from Derris reticulata possesses bactericidal activity on Staphylococcus aureus by disrupting bacterial cell membrane
In this study, lupinifolin, a prenylated flavonoid, was isolated fromDerris reticulata stem, identified by NMR spectra and confirmed with mass spectrometry. Lupinifolin was freshly prepared by solubilizing in 0.1  N NaOH and immediately diluted in Müller–Hinton broth for antibacterial testing. The data showed that Gram-positive bacteria were more susceptible to lupinifolin than Gram-negative bacteria. Of four strains of Gram-positive bacteria tested,Staphylococcus aureus was the most susceptible. Using the two-fold microdilution method, it was found that lupinifolin possessed antimicrobial activity againstS...
Source: Journal of Natural Medicines - December 30, 2016 Category: Drugs & Pharmacology Source Type: research

Antidepressant-like effects of ginsenoside Rg3 in mice via activation of the hippocampal BDNF signaling cascade
In conclusion, ginsenoside Rg3 has antidepressant effects via promotion of the hippocampal BDNF signaling pathway. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - December 24, 2016 Category: Drugs & Pharmacology Source Type: research

Shikonin inhibits TNF- α production through suppressing PKC-NF-κB-dependent decrease of IL-10 in rheumatoid arthritis-like cell model
AbstractShikonin, a major effective component in the Chinese herbal medicineLithospermum erythrorhizon Sieb., exhibits an anti-inflammatory property towards rheumatoid arthritis (RA), but the potential mechanism is unclear. Our aim was to investigate the mechanism of shikonin on the lipopolysaccharide (LPS)-induced fibroblast-like synoviocyte (LiFLS) inflammation model. Fibroblast-like synoviocytes (FLSs) were treated with 200  μg/ml of LPS for 24 h to establish the RA-like model, LiFLS. FLSs were pretreated with shikonin (0.1–1 μM) for 30 min in the treatment groups. Quantitative real-time ...
Source: Journal of Natural Medicines - December 9, 2016 Category: Drugs & Pharmacology Source Type: research

Naringenin interferes with the anti-diabetic actions of pioglitazone via pharmacodynamic interactions
AbstractPioglitazone is a peroxisome proliferator-activated receptor gamma (PPAR γ) full agonist and useful for the treatment of type 2 diabetes mellitus. Naringenin is a citrus flavonoid with anti-inflammatory actions, which has been shown to prevent obesity-related diseases and to activate PPARγ. The aim of this study was to investigate whether dietary naringenin affects the actions of pioglitazone. We administered naringenin (100 mg/kg) and pioglitazone (10 mg/kg) to Tsumura Suzuki Obese Diabetes (TSOD) mice for 4 weeks and then conducted an oral glucose tolerance test. We found that oral admi...
Source: Journal of Natural Medicines - December 3, 2016 Category: Drugs & Pharmacology Source Type: research

Pharmacological evaluation for improvement of Kanazawa Sutra, medicinal thread for anal fistula
In this study, we evaluated the ingredients of KanS by measuring nitric oxide (NO) production in murine macrophage-like cell line J774.1 as well as examining cytotoxicity to rat skeletal muscle myoblasts (L6) and L6 differentiation, with a view to improving its pharmacological effect. We focused onMallotus japonicus bark (MJB), which is described in the Japanese Pharmacopeia and belongs to the Euphorbiaceae family. Its biological activities were evaluated in a similar manner to the evaluation of KanS ingredients. We found that MJB extracts showed similar biological activity toEuphorbia neriifolia latex (ENL), an ingredient...
Source: Journal of Natural Medicines - November 29, 2016 Category: Drugs & Pharmacology Source Type: research

Protein tyrosine phosphatase 1B inhibitory properties of seco-cucurbitane triterpenes obtained from fruiting bodies of Russula lepida
AbstractThe known seco-cucurbitane triterpene, (24E)-3,4-seco-cucurbita-4,24-diene-3,26,29-trioic acid (1), has been isolated as a potent protein tyrosine phosphatase (PTP) 1B inhibitor together with a new analogue, (24E)-3,4-seco-cucurbita-4,24-diene-3-hydroxy-26,29-dioic acid (2), from the fruiting bodies ofRussula lepida. Further evaluation of their biological properties against PTPs revealed that compound1 inhibited T-cell PTP activity similarly to PTP1B and exhibited moderate selectivity against PTP1B overvaccinia H-1-related phosphatase. Moreover, the in vitro growth inhibitory effects of1 and2 against three human ca...
Source: Journal of Natural Medicines - November 19, 2016 Category: Drugs & Pharmacology Source Type: research

Gastroprotective effect of palmatine against acetic acid-induced gastric ulcers in rats
AbstractGastric ulcers are one of the most common gastrointestinal disorders. The aim of this study was to investigate the gastroprotective activity and possible underlying mechanisms of palmatine against acetic acid-induced gastric ulcers in rats. Palmatine was administered orally for 7 consecutive days to treat ulcers. The ulcer area, ulcer inhibition rate, histological section, platelet-activating factor (PAF) level in serum, prostaglandin E2 (PGE2) level in gastric tissue, 5-hydroxytryptamine (5-HT) level in the brain and norepinephrine (NE) level in the adrenal glands were analyzed. Histological results showed that th...
Source: Journal of Natural Medicines - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

Securigenin glycosides as hypoglycemic principles of Securigera securidaca seeds
In this study, the antihyperglycemic activity of chloroform and methanol fractions (CF and MF) fromS. securidaca seed extract was investigated and their bioactive constituents were identified. The antidiabetic effects of fractions were assessed by streptozocin-induced diabetic Naval Medical Research Institute mice. The hypoglycemic activity of MF at 100  mg/kg and CF at 400 mg/kg was comparable with glibenclamide (3 mg/kg). MF at 400 mg/kg and CF at 600 mg/kg showed equal hypoglycemic responses to 12.5 IU/kg insulin (P >  0.05). Three cardiac glycosides were isolated as active con...
Source: Journal of Natural Medicines - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of the safety and efficacy of Glycyrrhiza uralensis root extracts produced using artificial hydroponic and artificial hydroponic-field hybrid cultivation systems
AbstractGlycyrrhiza uralensis roots used in this study were produced using novel cultivation systems, including artificial hydroponics and artificial hydroponic-field hybrid cultivation. The equivalency betweenG. uralensis root extracts produced by hydroponics and/or hybrid cultivation and a commercialGlycyrrhiza crude drug were evaluated for both safety and efficacy, and there were no significant differences in terms of mutagenicity on the Ames tests. The levels of cadmium and mercury in both hydroponic roots and crude drugs were less than the limit of quantitation. Arsenic levels were lower in all hydroponic roots than i...
Source: Journal of Natural Medicines - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Nobiletin improves emotional and novelty recognition memory but not spatial referential memory
In this study, 8-week-old male mice were tested using behavioral measurements for working, spatial referential, emotional and visual recognition memory after daily administration of nobiletin. While nobiletin did not induce any change of spontaneous activity in the open field test, freezing by fea r conditioning and novel object recognition increased. However, the effectiveness of spatial navigation in the Y-maze and Morris water maze was not improved. These results mean that nobiletin can specifically improve memories of emotionally salient information associated with fear and novelty, but n ot of spatial information with...
Source: Journal of Natural Medicines - November 9, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of the chemical quality of Sekkoku ( 石斛) in current Japanese commercial crude drugs: constituents of Flickingeria xantholeuca (Rchb. f.) A.D. Hawkes
AbstractIn our investigation, mostShihu ( 石斛; Japanese name,Sekkoku) in current Japanese commercial crude drugs were fromFlickingeria xantholeuca (Orchidaceae). As the index compounds, three newent-pimarane-type diterpenes, flickinxthanthosides A –C (1–3), one known analogue (7), and three newent-kaurane-type diterpenes, flickinxanthosides D (4) and E (5) and flickinxanthol A (6) were isolated from the stem ofF. xantholeuca. The structures of the new compounds were elucidated on the basis of spectroscopic analyses and chemical methods. We attempted to detect these index compounds from the MeOH extracts of o...
Source: Journal of Natural Medicines - November 3, 2016 Category: Drugs & Pharmacology Source Type: research

Hypouricemic effect of flaccidoside II in rodents
AbstractTo investigate the effect of flaccidoside II on the serum uric acid levels in hyperuricemic rodents. Both mice and rats were injected intraperitoneally with potassium oxonate to induce hyperuricemia. Different dosages of flaccidoside II were orally administrated to hyperuricemic and normal rodents for 7  days, respectively. Liver xanthine oxidase (XOD) activities in hyperuricemic mice were determined using the colorimetric method. Acute toxicity of flaccidoside II was also evaluated in mice. Allopurinol, as a positive control, was administered under the same treatment scheme. The results showed th at flaccidos...
Source: Journal of Natural Medicines - October 22, 2016 Category: Drugs & Pharmacology Source Type: research

Hypocholesterolemic effect of sericin-derived oligopeptides in high-cholesterol fed rats
AbstractThe beneficial effect of cholesterol-lowering proteins and/or peptides derived from various dietary sources is continuously reported. A non-dietary protein from silk cocoon, sericin, has also demonstrated cholesterol-lowering activity. A sericin hydrolysate prepared by enzymatic hydrolysis was also expected to posses this effect. The present study was aimed at investigating the cholesterol-lowering effect of sericin peptides, so called “sericin-derived oligopeptides” (SDO) both in vivo and in vitro. The results showed that SDO at all three doses tested (10 mg kg−1 day−1, 50 &n...
Source: Journal of Natural Medicines - October 22, 2016 Category: Drugs & Pharmacology Source Type: research

Involvement of monoaminergic systems in anxiolytic and antidepressive activities of the standardized extract of Cocos nucifera L.
AbstractExtracts from the husk fiber ofCocos nucifera are used in folk medicine, but their actions on the central nervous system have not been studied. Here, the anxiolytic and antidepressant effects of the standardized hydroalcoholic extract ofC. nucifera husk fiber (HECN) were evaluated. Male Swiss mice were treated with HECN (50, 100, or 200  mg/kg) 60 min before experiments involving the plus maze test, hole-board test, tail suspension test, and forced swimming test (FST). HECN was administered orally (p.o.) in acute and repeated-dose treatments. The forced swimming test was performed with dopaminergic and no...
Source: Journal of Natural Medicines - October 21, 2016 Category: Drugs & Pharmacology Source Type: research

Aged garlic extract suppresses platelet aggregation by changing the functional property of platelets
In this study, we examined the effect of AGE on the functional property of platelet by administering AGE to rats and evaluating the platelet aggregation in response to collagen in vitro. We found that AGE treatment significantly reduced the ability of platelet to aggregate and this effect of AGE was manifested on the 14  day, but not 7 day of treatment. In addition, AGE treatment produced platelets that responded to collagen by significantly increasing the amount of both the extracellular ATP and the extra- and intracellular TXB2. AGE treatment also dose-dependently suppressed the phosphorylation of collagen-indu...
Source: Journal of Natural Medicines - October 20, 2016 Category: Drugs & Pharmacology Source Type: research

Chodatiionosides A and B: two new megastigmane glycosides from Chorisia chodatii leaves
AbstractPhytochemical investigation ofChorisia chodatii Hassl. leaves led to the isolation of an unusual rearranged megastigmane glycoside; chodatiionoside A (1) and another new megastigmane glycoside; chodatiionoside B (2), together with three known megastigmane glycosides (3–5) and one known flavonoid glycoside (6). Their structures were elucidated by spectroscopic methods including 1D and 2D NMR experiments (1H,13C, DEPT, COSY, HSQC and HMBC) in combination with HR-ESI –MS, CD and modified Mosher’s method. As a result, chodatiionoside A has been elucidated as a first example of an unusual rearranged fo...
Source: Journal of Natural Medicines - October 19, 2016 Category: Drugs & Pharmacology Source Type: research

The effects of 18 β-glycyrrhetinic acid and glycyrrhizin on intestinal absorption of paeoniflorin using the everted rat gut sac model
In conclusion, the influence of 18β-GA and glycyrrhizin on the PF absorption was related to concentrations and intestinal segments. This might be involved in the intervention of efflux transport of PF mediated by intestinal P-gp. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - October 17, 2016 Category: Drugs & Pharmacology Source Type: research

Screening of promising chemotherapeutic candidates from plants against human adult T-cell leukemia/lymphoma (V): coumarins and alkaloids from Boenninghausenia japonica and Ruta graveolens
AbstractDuring the course of our studies towards the identification of promising chemotherapeutic candidates from plants against two human T-cell lymphotropic virus type I-infected T-cell lines (MT-1 and MT-2), we screened 17 extracts from 9 rutaceous plants against MT-1 and MT-2 cells. The extracts from the aerial parts and roots ofBoenninghausenia japonica, as well as the leaves and roots ofRuta graveolens showed potent antiproliferative effects. After activity-guided fractionation, we isolated 44 compounds from two rutaceous plants, including three new compounds (1 –3), which were classified into 26 coumarin analo...
Source: Journal of Natural Medicines - October 13, 2016 Category: Drugs & Pharmacology Source Type: research

Mangostanaxanthones III and IV: advanced glycation end-product inhibitors from the pericarp of Garcinia mangostana
AbstractAdvanced glycation end-products (AGEs) are associated with a non-enzymatic reaction between the amino group of a protein and the carbonyl group of a sugar during hyperglycemia. The precipitation of AGEs in different tissues leads to many complications, such as endothelial dysfunction, cardiovascular complications, atherosclerosis, retinopathy, neuropathy, and Alzheimer ’s disease.Garcinia mangostana L. (Clusiaceae) (GM) was selected owing to the ability of its polar and non-polar fractions to inhibit AGE formation. For the first time, the bioguided fractionation of its pericarp MeOH extract (GMT) gave rise to...
Source: Journal of Natural Medicines - October 13, 2016 Category: Drugs & Pharmacology Source Type: research

Lignans from guaiac resin decrease nitric oxide production in interleukin 1 β-treated hepatocytes
AbstractGuaiac resin, extracted from the heartwood ofGuaiacum officinale L. orG. sanctum L., is speculated to have anti-inflammatory effects. Lignans were purified from guaiac resin (also known as gum guaiacum) by monitoring the nitric oxide (NO) production in rat hepatocytes treated with an inflammatory cytokine interleukin-1 β (IL-1β). Six lignans were purified from guaiac resin and identified as: dehydroguaiaretic acid (1), (+)-trans-1,2-dihydrodehydroguaiaretic acid (2), furoguaiaoxidin (3),meso-dihydroguaiaretic acid (4), furoguaiacin (i.e., α-guaiaconic acid) (5), and nectandrin B (6). To our knowledg...
Source: Journal of Natural Medicines - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Carbazole alkaloids from Murraya koenigii trigger apoptosis and autophagic flux inhibition in human oral squamous cell carcinoma cells
In this study, we investigated the anticancer properties and mechanisms of action of two carbazole alkaloids derived fromM. koenigii leaves, mahanine and isomahanine, in the OSCC cell line CLS-354. At 15  μM, mahanine and isomahanine were cytotoxic to CLS-354 cells, triggering apoptosis via caspase-dependent and -independent mechanisms. Autophagosomes, visualised using monodansylcadaverine (MDC) labelling, were numerous in carbazole alkaloid-treated cells. Mahanine and isomahanine markedly induced the expression of the autophagosome marker microtubule-associated protein 1 light chain 3, type II (LC3B-II). Genetic a...
Source: Journal of Natural Medicines - September 28, 2016 Category: Drugs & Pharmacology Source Type: research

Quantitative evaluation and discrimination of wild Paris polyphylla var . yunnanensis (Franch.) Hand.-Mazz from three regions of Yunnan Province using UHPLC –UV–MS and UV spectroscopy couple with partial least squares discriminant analysis
In this study, a convenient and accurate method was established using ultra high performance liquid chromatography (UHPLC) for simultaneous determination of four steroid saponins (Pa, Pb, polyphyllin VI, and chonglou saponin VII). Partial least squares discriminant analysis (PLS-DA) according to UHPLC and UV spectroscopy was applied to analyze 30 samples of PPY from three regions of Yunnan Province in China, and identify significant peaks. The results indicated that the correlation coefficients (r2) of all calibration curves were above 0.999, and the inter- and intra-day relative standard deviations (RSD) of retention time...
Source: Journal of Natural Medicines - September 24, 2016 Category: Drugs & Pharmacology Source Type: research

Rapid and simple determination of polyphyllin I, II, VI, and VII in different harvest times of cultivated Paris polyphylla Smith var. yunnanensis (Franch.) Hand.-Mazz by UPLC-MS/MS and FT-IR
In conclusion, FT-IR combined with chemometrics is a promising method to accurately discriminate samples ofP. polyphylla var.yunnanensis harvested in different years and determine the content of polyphyllin I, II, VI, and VII inP. polyphylla var.yunnanensis. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - September 24, 2016 Category: Drugs & Pharmacology Source Type: research

De novo transcriptome assembly and characterization of nine tissues of Lonicera japonica to identify potential candidate genes involved in chlorogenic acid, luteolosides, and secoiridoid biosynthesis pathways
In this study, we performed de novo transcriptome assembly forL. japonica, representing transcripts from nine different tissues. A total of 22  Gbps clean RNA-seq reads from nine tissues ofL. japonica were used, resulting in 243,185 unigenes, with 99,938 unigenes annotated based on a homology search using blastx against the NCBI-nr protein database. Unsupervised principal component analysis and correlation studies using transcript expression data from all nine tissues ofL. japonica showed relationships between tissues, explaining their association at different developmental stages. Homologs for all genes associated wi...
Source: Journal of Natural Medicines - September 14, 2016 Category: Drugs & Pharmacology Source Type: research

Ginsenosides, ingredients of the root of Panax ginseng , are not substrates but inhibitors of sodium-glucose transporter 1
AbstractRecent pharmacokinetic studies have revealed that ginsenosides, the major ingredients of ginseng (the roots ofPanax ginseng), are present in the plasma collected from subjects receiving ginseng, and speculated that ginsenosides might be actively transported via glucose transporters. We evaluated whether ginsenosides Rb1 and Rg1, and their metabolites from enteric bacteria act as substrates of sodium-glucose cotransporter (SGLT) 1, the major glucose transporter expressed on the apical side of intestinal epithelial cells. First, we evaluated the competing effects of ginseng extract and ginsenosides on the uptake of [...
Source: Journal of Natural Medicines - September 12, 2016 Category: Drugs & Pharmacology Source Type: research

Application of a quantitative 1 H-NMR ( 1 H-qNMR) method for the determination of geniposidic acid and acteoside in Plantaginis semen
AbstractA quantitative1H-NMR method (1H-qNMR) was developed to determine the concentration of acteoside and geniposidic acid in Plantaginis semen, which is an important crude drug for diuretic purposes. The purity of geniposidic acid and acteoside was determined by the ratio of the intensity of the H-3 signal at δ 7.51 ppm or the H-7″ signal at δ 7.58 ppm in methanol-d4 to that of a hexamethyldisilane (HMD) signal at 0.04  ppm, respectively. The concentration of HMD was corrected with the International System of Units traceability using potassium hydrogen phthalate of certified reference ma...
Source: Journal of Natural Medicines - September 8, 2016 Category: Drugs & Pharmacology Source Type: research

Ephedra Herb extract activates/desensitizes transient receptor potential vanilloid 1 and reduces capsaicin-induced pain
In this study, the effects of EH extract (EHE) on transient receptor potential vanilloid 1 (TRPV1), a nonselective ligand-gated cation channel, which plays an essential role in nociception on sensory neurons, were investigated using mTRPV1/Flp-In293 cells (stable mouse TRPV1-expressing transfectants). Administration of EHE increased the intracellular Ca2+ concentration in these cells, which was inhibited by the TRPV1 antagonist,N-(4-tert-butylphenyl)-1,2-dihydro-4-(3-chloropyridine-2-yl) tetrahydropyrazine-1-carboxamide (BCTC), indicating that EHE activated TRPV1. Examination of EHE-induced nociceptive pain in vivo reveale...
Source: Journal of Natural Medicines - September 8, 2016 Category: Drugs & Pharmacology Source Type: research

Cytotoxicities of two new isoflavanes from the roots of Dalbergia velutina
AbstractTwo new isoflavanes, dalvelutinanes A (1) and B (2), along with three known isoflavanes (3–5) were isolated from the roots ofDalbergia velutina. Their chemical structures, including their absolute configurations, were determined by spectroscopic analysis (1D and 2D NMR, HRESIMS, and CD). All isolated compounds were evaluated for their in vitro cytotoxicities against five human cancer cell lines (KB, HeLa-S3, MCF-7, HepG-2, and HT-29). Compound5 showed significant cytotoxicity against all of the tested cancer cell lines, with IC50 values in the range 3.47 –9.76 µM. In addition, compound3 showe...
Source: Journal of Natural Medicines - September 7, 2016 Category: Drugs & Pharmacology Source Type: research

Three new ent -kaurane diterpenes from the herbs of Wedelia prostrata
AbstractThree newent-kaurane diterpenes, 3α-angeloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (1), 3α-tigloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (2) and 3α-cinnamoyloxykaur-9(11),16-dien-19-oic acid (3), along with five known compounds (4-8), were isolated from the herbs ofWedelia prostrata (Asteraceae). The structures were determined by extensive analysis of their spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The isolated compounds were evaluated for their cytotoxic activity on human hepatocellular carcinoma HepG2 cells. Among them, all isolates exhibited cytotoxic activities with IC50 value...
Source: Journal of Natural Medicines - September 7, 2016 Category: Drugs & Pharmacology Source Type: research

5 ′-AMP-activated protein kinase plays an essential role in geniposide-regulated glucose-stimulated insulin secretion in rat pancreatic INS-1 β cells
AbstractOur previous work showed that geniposide affected glucose-stimulated insulin secretion (GSIS) via regulating glucose uptake and metabolism in pancreatic β cells; however, the molecular mechanisms remain largely unknown. Substantial evidence suggests that activation of 5′-AMP-activated protein kinase (AMPK) plays a central role in GSIS. Here, we aim to determine the role of AMPK on geniposide-regulated GSIS in rat pancreatic INS-1 cells. The resul ts demonstrated that 6-[4-(2-piperidin-1-yletoxy)-phenyl]-3-pyridin-4-yl-pyrazolo[1,5-α] pyrimidine (Compound C; an AMPK inhibitor) significantly attenuat...
Source: Journal of Natural Medicines - September 7, 2016 Category: Drugs & Pharmacology Source Type: research

Pteleifolols A –E, acetophenone di- C -glycosides and a benzopyran dimer from the leaves of Melicope pteleifolia
AbstractFour new acetophenone di-C-glycosides, pteleifolols A –D (1–4) and a new dimeric benzopyran, pteleifolol E (5), were isolated from the leaves ofMelicope pteleifolia. Seven known compounds, including 2,4,6-trihydroxyacetophenone-3,5-di-C-glucopyranoside (6), were also isolated. Structures of the new compounds (1–5) were established by using spectroscopic and spectrometric techniques, including 1D and 2D nuclear magnetic resonance (NMR), UV, and high-resolution electrospray ionization mass spectrometry (HR-ESI –MS) data. Pteleifolols A–D (1–4) wereE-p-coumaroyl,Z-p-coumaroyl,E-feru...
Source: Journal of Natural Medicines - September 6, 2016 Category: Drugs & Pharmacology Source Type: research

Efficacy of Kaempferia parviflora in a mouse model of obesity-induced dermatopathy
AbstractObesity results from excessive energy intake and physical inactivity, and predisposes one to various diseases. One of these reasons is that enlargement of adipocytes raises the lipid metabolic abnormalities that affect various organs. The skin is one such organ, and it has been reported that subcutaneous adipocyte cells secrete various factors and these factors are involved in reduction of dermal collagen fibers and fragility of the skin in obesity. The present study explored the efficacy ofKaempferia parviflora (KP) in preventing obesity-induced dermatopathy. We used Tsumura Suzuki obese diabetes (TSOD) mice as an...
Source: Journal of Natural Medicines - September 3, 2016 Category: Drugs & Pharmacology Source Type: research