Novel polyacetylene derivatives and their inhibitory activities on acetylcholinesterase obtained from Panax ginseng roots
This study showed, for the first time, that polyacetylene compounds possess acetylcholinesterase inhibitory activities. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - August 27, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation and quantitative analysis of different growth periods of herb –arbor intercropping systems using HPLC and UV–vis methods coupled with chemometrics
In this study, we employed high-performance liquid chromatography (HPLC) and ultraviolet –visible spectroscopy (UV–vis) combined with chemometrics for determination and qualitative evaluation of several kinds of intercropping system withGentiana rigescens Franch. ex Hemsl. (GR), which is used as an hepatic protector in local communities in China. Results revealed that GR in aCamellia sinensis intercropping system contained most gentiopicroside, sweroside, and total active constituents (six chemical indicators), whose content reached 91.09  ± 3.54, 1.03 ± 0.06, and 104.05 &...
Source: Journal of Natural Medicines - August 25, 2016 Category: Drugs & Pharmacology Source Type: research

Dianthosaponins G –I, triterpene saponins, an anthranilic acid amide glucoside and a flavonoid glycoside from the aerial parts of Dianthus japonicus and their cytotoxicity
AbstractExtensive isolation work on the 1-BuOH-soluble fraction of a MeOH extract of the aerial parts ofDianthus japonicus afforded three further triterpene glycosyl estsers, termed dianthosaponins G –I, an anthranilic acid amide glucoside and aC-glycosyl flavonoid along with one known triterpene saponin. Their structures were elucidated from spectroscopic evidence. The cytotoxicity of the isolated compounds toward A549 cells was evaluated. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - August 25, 2016 Category: Drugs & Pharmacology Source Type: research

Constituents from the leaves of Clausena lansium and their anti-inflammatory activity
AbstractFive new acyclic amides, clausenalansamides C-G (1–5), clausenaline G (6) and ( ±)-5-(4-methylphenyl)-γ-valerolactone (7) reported from the natural source for the first time, were characterized from the leaves ofClausena lansium. Their structures were established by spectroscopic and spectrometric methods, and the absolute configurations of new compounds1–5 were determined by electronic circular dichroism and single-crystal X-ray diffraction analyses. Eighteen compounds were evaluated for their anti-inflammatory activity and only imperatorin (11) and wampetin (12) displayed significant inhi...
Source: Journal of Natural Medicines - August 18, 2016 Category: Drugs & Pharmacology Source Type: research

Constituents from Vitex negundo var. heterophylla and their inhibition of nitric oxide production
AbstractAn iridoid glucoside, 10-p-hydroxybenzoyl-6β-hydroxyiridoid 1-O-β-d-(6 ′-O-p-hydroxybenzoyl)-glucopyranoside (1), and a phenol glucoside, 4-hydroxyphenethanol 3-O-β-d-(6 ′-O-p-hydroxybenzoyl)-glucopyranoside (2), along with nine known compounds (3–11) were isolated from the dried leaves ofVitex negundo var.heterophylla. Their structures were elucidated by extensive analysis of NMR spectra. All of the isolated compounds were evaluated for their inhibitory effects on nitric oxide production in RAW 264.7 macrophages. Compounds2 and3 exhibited obvious inhibitory effects on NO production...
Source: Journal of Natural Medicines - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Rapid identification of drug-type strains in Cannabis sativa using loop-mediated isothermal amplification assay
AbstractInCannabis sativa L., tetrahydrocannabinol (THC) is the primary psychoactive compound and exists as the carboxylated form, tetrahydrocannabinolic acid (THCA).C. sativa is divided into two strains based on THCA content —THCA-rich (drug-type) strains and THCA-poor (fiber-type) strains. Both strains are prohibited by law in many countries including Japan, whereas the drug-type strains are regulated in Canada and some European countries. As the two strains cannot be discriminated by morphological analysis, a simple method for identifying the drug-type strains is required for quality control in legal cultivation a...
Source: Journal of Natural Medicines - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Cannabidiolic acid-mediated selective down-regulation of c-fos in highly aggressive breast cancer MDA-MB-231 cells: possible involvement of its down-regulation in the abrogation of aggressiveness
AbstractThe physiological activities of cannabidiolic acid (CBDA), a component of fiber-type cannabis plants, have been demonstrated and include its function as a protector against external invasion by inducing cannabinoid-mediated necrosis (Shoyama et al., Plant Signal Behav 3:1111 –1112,2008). The biological activities of CBDA have been attracting increasing attention. We previously identified CBDA as an inhibitor of the migration of MDA-MB-231 cells, a widely used human breast cancer cell line in cancer biology, due to its highly aggressive nature. The chemical inhibition and down-regulation of cyclooxygenase-2 (C...
Source: Journal of Natural Medicines - August 16, 2016 Category: Drugs & Pharmacology Source Type: research

The action and mechanism of myrislignan on A549 cells in vitro and in vivo
In conclusion, those results reveal a potential mechanism for the anti-cancer effect of myrislignan on human lung cancer, while suggesting that myrislignan may be a promising compound for the treatment of lung cancer. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - August 4, 2016 Category: Drugs & Pharmacology Source Type: research

Structure and hemolytic activity relationships of triterpenoid saponins and sapogenins
AbstractWe evaluated the hemolytic activity of 41 commercially available triterpenoid saponins and sapogenins derived from three types of structural skeletons. Structure –activity relationships were established by comparing the structural characteristics of both the aglycone and sugar moieties among the tested compounds. The majority of oleanane-type sapogenins had stronger hemolytic effects than those of the ursane and dammarane types. The presence of polar regio ns on sapogenins, such as a carboxyl (COOH) at position 28, an α-hydroxyl (α-OH) at position 16, and/or a β-hydroxyl (β-OH) at positi...
Source: Journal of Natural Medicines - August 4, 2016 Category: Drugs & Pharmacology Source Type: research

Green tea cultivar ‘Benifuuki’ potentiates split vaccine-induced immunoglobulin A production
AbstractInfluenza is a widespread disease caused by infection with the influenza virus. Vaccination is considered to be the main countermeasure against influenza. A split vaccine is widely used to avoid severe adverse events, and it induces strong humoral immunity. However, the split vaccine alone cannot elicit mucosal immunity, including IgA production, and its preventative effects are limited. Here, we show that the green tea cultivar ‘Benifuuki’ extract enhanced the effect of a split vaccine on mucosal immunity. The frequency of IgA+ cells was increased in lung and Peyer ’s patch that received Benifuuk...
Source: Journal of Natural Medicines - August 3, 2016 Category: Drugs & Pharmacology Source Type: research

Marine spongean polybrominated diphenyl ethers, selective growth inhibitors against the cancer cells adapted to glucose starvation, inhibits mitochondrial complex II
Abstract In the course of search for selective growth inhibitors against the cancer cells adapted to nutrient starvation, two polybrominated diphenyl ethers, 3,4,5-tribromo-2-(2 ′,4′-dibromophenoxy)-phenol ( 1 ) and 3,5-dibromo-2-(2 ′,4′-dibromophenoxy)-phenol ( 2 ) were isolated from an Indonesian marine sponge of Dysidea sp. Compounds 1 and 2 showed the anti-proliferative activity against PANC-1 cells under glucose-starved conditions with IC 50 values of 2.1 and 3.8  µM, respectively, whereas no growth inhibition was observed up to 30 µM in the general culture conditions...
Source: Journal of Natural Medicines - July 23, 2016 Category: Drugs & Pharmacology Source Type: research

Two new compounds from Trollius chinensis Bunge
Abstract Two new compounds, 2″-O-feruloylisoswertiajaponin (1) and (2E)-2-methyl-1-O-vaniloyl-4-β-d-glucopyranoside-2-butene (2), along with one indole alkaloid and five known flavonoids, were isolated from the flowers of Trollius chinensis Bunge. Their structures were elucidated on the basis of spectroscopic evidence (UV, IR, HR-ESI–MS, NMR). (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - July 15, 2016 Category: Drugs & Pharmacology Source Type: research

Gastrodin reversed the traumatic stress-induced depressed-like symptoms in rats
Abstract Exposure to severe stress can lead to the development of neuropsychiatric disorders such as depression and post-traumatic stress disorder (PTSD) in at-risk individuals. Gastrodin (GAS), a primary constituent of an Oriental herbal medicine, has been shown to effectively treat various mood disorders. Thus, the present study aimed to determine whether GAS would ameliorate stress-associated depression-like behaviors in a rat model of single prolonged stress (SPS)-induced PTSD. Following the SPS procedure, rats received intraperitoneal administration of GAS (20, 50, or 100 mg/kg) once daily for 2 wee...
Source: Journal of Natural Medicines - July 14, 2016 Category: Drugs & Pharmacology Source Type: research

Glycyrrhetinic acid protects H9c2 cells from oxygen glucose deprivation-induced injury through the PI3K/AKt signaling pathway
Abstract Glycyrrhetinic acid (GA) is an ingredient of triterpene saponins found in Gancao (Radix Glycyrrhizae). Here, we investigated the protective effects of GA in H9c2 cells, and explored its possible mechanism of action. Different concentrations of GA were used to treat H9c2 cells under oxygen glucose deprivation. We analyzed cell necrosis and apoptosis using optical microscopy, Hoechst 33342 staining, FITC-annexin V/PI double-staining and lactate dehydrogenase (LDH), creatine kinase-MB (CK-MB) and interleukin (IL)-1β assays. Changes in related pro-apoptosis and anti-apoptosis proteins were detected by We...
Source: Journal of Natural Medicines - July 12, 2016 Category: Drugs & Pharmacology Source Type: research

AU-1 from Agavaceae plants causes transient increase in p21/Cip1 expression in renal adenocarcinoma ACHN cells in an miR-34-dependent manner
Abstract Here, we show that AU-1, spirostanol saponin isolated from Agavaceae plants, causes a transient increase in cyclin-dependent kinase inhibitor (CDKI) p21/Cip1 through the upregulation of miRNAs, miR-34 and miR-21. AU-1 stimulated p21/Cip1 expression without exerting cytotoxicity against different types of carcinoma cell lines. In renal adenocarcinoma ACHN cells, AU-1 transiently elevated the expression level of p21/Cip1 protein without marked increases in p21/Cip1 mRNA levels. Rapid and transient increases in miR-34 and miR-21, both of which are known to upregulate p21/Cip1, were observed in AU-1-treated c...
Source: Journal of Natural Medicines - July 7, 2016 Category: Drugs & Pharmacology Source Type: research

New biofunctional effects of the flower buds of Camellia sinensis and its bioactive acylated oleanane-type triterpene oligoglycosides
Abstract We review the biofunctional effects of the flower buds of Camellia sinensis and C. sinensis var. assamica, such as antihyperlipidemic, antihyperglycemic, antiobesity, and gastroprotective effects in vivo, and antiallergic, pancreatic lipase inhibitory, and amyloid β (Aβ) aggregation inhibitory activities in vitro. Although the biofunctional effects of tea leaves have been extensively studied, less attention has been given to those of the flowers and seeds of the tea plant. Our studies focused on the saponin constituents of the extracts of the flower buds of C. sinensis cultivated ...
Source: Journal of Natural Medicines - July 5, 2016 Category: Drugs & Pharmacology Source Type: research

Treatment of adult and pediatric high-grade gliomas with Withaferin A: antitumor mechanisms and future perspectives
Abstract Resistance mechanisms employed by high-grade gliomas allow them to successfully evade current standard treatment of chemotherapy and radiation treatment. Withaferin A (WA), utilized in Ayurvedic medicine for centuries, is attracting attention for its antitumor capabilities. Here we review pertinent literature on WA as a high-grade glioma treatment, and discuss the cancerous mechanisms it affects. WA is relatively nontoxic and has shown potential in crossing the blood–brain barrier. WA prevents p53 alterations and inactivates overexpressed MDM2 through ARF and ROS production. Furthermore, WA upre...
Source: Journal of Natural Medicines - July 2, 2016 Category: Drugs & Pharmacology Source Type: research

Catalpol reduces the production of inflammatory mediators via PPAR- γ activation in human intestinal Caco-2 cells
Abstract Catalpol, a major iridoid glycoside present in Rehmannia glutinosa , has been reported to show a variety of pharmacological properties. However, the molecular mechanism underlying the anti-inflammatory effect of catalpol in intestinal cells remains poorly understood. The present study was aimed at investigating the effects of catalpol on the production of inflammatory mediators and its underlying signaling pathways in human intestinal Caco-2 cells. Catalpol significantly inhibited IL-1 β-induced mRNA synthesis and protein production of pro-inflammatory cytokines, including IL-6, IL-8, and MCP-1. Further inve...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Anti-oxidative, anti-secretory and anti-inflammatory activities of the extract from the root bark of Lycium chinense (Cortex Lycii) against gastric ulcer in mice
Abstract The evaluation of the antioxidant, anti-secretory and anti-inflammatory potentials of the ethyl acetate fraction (ELC) from the root bark of Lycium chinense against ethanol-induced gastric ulcer in mice and the possible mechanisms underlying this action was performed. The results indicated that oral administration of ELC (50, 100, 200 and 400 mg/kg) before ethanol-induced ulcer increased the gastric mucus content, restored the superoxide dismutase and glutathione levels, reduced malondialdehyde levels and inhibited the activity of myeloperoxidase. Furthermore, ELC displayed its anti-secretory activi...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Efficiently prepared ephedrine alkaloids-free Ephedra Herb extract: a putative marker and antiproliferative effects
Abstract Ephedrine alkaloids (EAs) have been considered the main pharmacologically active substances in Ephedra Herb (麻黄, Mao; EH) since they were first identified by Prof. N. Nagai, and are known to induce palpitation, hypertension, insomnia, and dysuria as side effects. Therefore, the administration of drugs containing EH to patients with cardiovascular-related diseases is severely contraindicated. While our previous studies suggest that some of the effects of EH may not be due to EAs, considering their side effects would be expedient to develop a new EAs-free EH extract (EFE). Here, we established a prepar...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Antithrombosis activity of protocatechuic and shikimic acids from functional plant Pinus densiflora Sieb. et Zucc needles
Abstract Pine needle extract (PE) and fermented pine needle extract (FPE) have been reported to show various biological and pharmacological activities such as antioxidant, anti-inflammatory, anti-bacterial, anti-cholesterol, gastrointestinal motility control, and fibrinolytic effect. The aims of our research were to isolate fibrinolytic compounds from PE and FPE and evaluate their antithrombotic activity in vitro and in vivo. Protocatechuic (1) and shikimic (2) acids were isolated and identified from FPE. 1 and 2 not only have fibrinolysis activity but also inhibit fibrin formation similar to aspirin. Ly...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

New potent accelerator of neurite outgrowth from Lawsonia inermis flower under non-fasting condition
Abstract The methanolic extract of Lawsonia inermis L. (henna) showed accelerative effects on nerve growth factor-induced neurite outgrowth in PC12 cells under non-fasting conditions. To elucidate the active constituents responsible for the neuronal differentiation, we conducted a search of the constituents and examined their accelerative effects on neurite outgrowth in PC12 cells. We isolated a new acetophenone glycoside, inermioside A, which exerted a significant accelerative effect on neurite outgrowth. We also confirmed the activities of nine known compounds, including quercetin and lalioside. In addition, we...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Chemical structures of constituents from the whole plant of Bacopa monniera
Abstract Two new dammarane-type triterpene oligoglycosides, bacomosaponins A and B, and three new phenylethanoid glycosides, bacomosides A, B1, and B2, were isolated from the whole plant of Bacopa monniera Wettst. The chemical structures of the new constituents were characterized on the basis of chemical and physicochemical evidence. In the present study, bacomosaponins A and B with acyl groups were obtained from the whole plant of B. monniera. This is the first report of acylated dammarane-type triterpene oligoglycosides isolated from B. monniera. In addition, dammarane-type triterpene saponins significantly inh...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Inhibitory effects of Leonurus sibiricus on weight gain after menopause in ovariectomized and high-fat diet-fed mice
In this study, the inhibitory effects of L. sibiricus on obesity after the menopause were investigated. Female C57BL/6 mice were ovariectomized and fed high-fat diet (HFD) for 12 weeks. Following an induction period, aqueous extracts of L. sibiricus (LS) were orally administrated for 6 weeks. The body, uterine, and visceral fat weights were measured immediately after the animals were killed. Histological analysis was performed to monitor fat and liver. Serum levels of glucose, triglyceride, total cholesterol, and LDL-cholesterol were evaluated. In addition, the expression of lipases was analyzed. Total body weigh...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Catalpol reduces the production of inflammatory mediators via PPAR-γ activation in human intestinal Caco-2 cells
Abstract Catalpol, a major iridoid glycoside present in Rehmannia glutinosa, has been reported to show a variety of pharmacological properties. However, the molecular mechanism underlying the anti-inflammatory effect of catalpol in intestinal cells remains poorly understood. The present study was aimed at investigating the effects of catalpol on the production of inflammatory mediators and its underlying signaling pathways in human intestinal Caco-2 cells. Catalpol significantly inhibited IL-1β-induced mRNA synthesis and protein production of pro-inflammatory cytokines, including IL-6, IL-8, and MCP-1. Furth...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Atranorin and lecanoric acid antagonize TCDD-induced xenobiotic response element-driven activity, but not xenobiotic response element-independent activity
In this study, we evaluated the aryl hydrocarbon receptor (AhR) antagonistic activity of 17 lichen substances and demonstrated that atranorin (1) and lecanoric acid (2), isolated from Parmotrema tinctorum Hale, showed an inhibitory effect on luciferase activity increased by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), using an XRE-driven pX4TK-Luc reporter gene assay. In addition, CYP1A1 mRNA and protein levels increased by TCDD were also suppressed by 1 and 2. Conversely, neither 1 nor 2 antagonized the suppressive effect of TCDD on interleukin (IL)-1β-induced acute-phase response (APR) gene expression. Thus, we concl...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Lucidumol C, a new cytotoxic lanostanoid triterpene from Ganoderma lingzhi against human cancer cells
Abstract A new oxygenated lanostane-type triterpene, named lucidumol C, together with six known compounds, was isolated from the chloroform extract of the fruiting bodies of Ganoderma lingzhi. Structures were established based on extensive spectroscopic and chemical studies. Potential cytotoxic activities of the isolated compounds were evaluated against human colorectal carcinoma (HCT-116, Caco-2), human liver carcinoma (HepG2), and human cervical carcinoma (HeLa) cell lines using WST-1 reagent. Selectivity was evaluated using normal human fibroblast cells (TIG-1 and HF19). Among the compounds, lucidumol C s...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Epigallocatechin gallate inhibits hepatitis B virus via farnesoid X receptor alpha
Abstract Plants possess various natural antiviral properties. Epigallocatechin-3-gallate (EGCG), a major component of green tea, inhibits a variety of viruses. However, the clinical application of EGCG is currently hindered by a scarcity of information on its molecular mechanism of action. In the present study, we examined the anti-HBV (hepatitis B virus) effects of catechins from green tea at the transcriptional and antigen-expression levels, as well as the associated molecular mechanisms, because HBV-associated liver diseases have become a key public health issue due to their serious impact on human physical a...
Source: Journal of Natural Medicines - July 1, 2016 Category: Drugs & Pharmacology Source Type: research

Anti-melanin deposition activity of ceramicines from Chisocheton ceramicus
Abstract The ceramicines, a series of limonoids from Chisocheton ceramicus (Meliaceae), were evaluated for anti-melanin deposition activity on α-melanocyte stimulating hormone (α-MSH) and 3-isobutyl-1-methylxanthine (IBMX)-treated B16-F10 melanoma cell, and several ceramicines were found to be active. The structure–activity relationship of ceramicines as anti-melanin deposition inhibitors was deduced. Furthermore, the mechanism of anti-melanin deposition activity of ceramicine B, a major constituent of C. ceramicus that showed potent anti-melanin deposition activity, was investigated. Tyrosinase ...
Source: Journal of Natural Medicines - June 29, 2016 Category: Drugs & Pharmacology Source Type: research

Dianthosaponins G–I, triterpene saponins, an anthranilic acid amide glucoside and a flavonoid glycoside from the aerial parts of Dianthus japonicus and their cytotoxicity
Abstract Extensive isolation work on the 1-BuOH-soluble fraction of a MeOH extract of the aerial parts of Dianthus japonicus afforded three further triterpene glycosyl estsers, termed dianthosaponins G–I, an anthranilic acid amide glucoside and a C-glycosyl flavonoid along with one known triterpene saponin. Their structures were elucidated from spectroscopic evidence. The cytotoxicity of the isolated compounds toward A549 cells was evaluated. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - June 28, 2016 Category: Drugs & Pharmacology Source Type: research

Synthesis and stereochemical determination of an antiparasitic pseudo -aminal type monoterpene indole alkaloid
Abstract 5-Nor stemmadenine alkaloids, isolated from the genus Tabernaemontana, display a range of bioactivity. 16-Hydroxy-16,22-dihydroapparicine, the active component of an extract from the Tabernaemontana sp. (dichotoma, elegans, and divaricate), exhibited potent antimalarial activity, representing the first such report of the antimalarial property of 5-nor stemmadenine alkaloids. We, therefore, decided to attempt the total synthesis of the compound to explore its antimalarial activity and investigate structure and bioactivity relationships. As a result, we completed the first total synthesis of 16-hydroxy-16,2...
Source: Journal of Natural Medicines - June 21, 2016 Category: Drugs & Pharmacology Source Type: research

Polygonatum stenophyllum improves menopausal obesity via regulation of lipolysis-related enzymes
Abstract Menopausal women are associated with an increase in obesity accompanying changes in the body's condition and composition. Polygonatum stenophyllum (PS) rhizome, which is a traditional herbal remedy, has been used to treat various diseases including obesity. However, the effect of PS on menopausal obesity remains unclear. Female C57BL/6 mice were ovariectomized (OVX) and fed on high fat diet (HFD) to induce menopausal obesity. Aqueous extract of PS of 1, 10, and 100 mg/kg was orally administrated for 6 weeks after 7 weeks of induction. The weights of body, uterine, and ovarian fat were ...
Source: Journal of Natural Medicines - June 20, 2016 Category: Drugs & Pharmacology Source Type: research

Preface to this special issue “Biologically active natural products from microorganisms and plants”
(Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - June 16, 2016 Category: Drugs & Pharmacology Source Type: research

Tetrahydroxanthones from Mongolian medicinal plant Gentianella amarella ssp. acuta
Abstract Two tetrahydroxanthones, 1,3,5S,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (1) and 1,3,5R,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (2), and six new tetrahydroxanthone glycosides, amarellins A–F (3–8), were isolated from the aerial parts of a Mongolian medicinal plant Gentianella amarella ssp. acuta (Gentianaceae). The structures of 1–8 were elucidated on the basis of spectroscopic analysis, chemical conversion, and ECD calculation. Amarellins A–C (3–5) were assigned as 8-O-β-d-glucoside, 8-O-β-d-xyloside, and 1-O-β-d-glucoside of 1, respectively, while amarel...
Source: Journal of Natural Medicines - June 15, 2016 Category: Drugs & Pharmacology Source Type: research

Medicinal significance of naturally occurring cyclotetrapeptides
Abstract Bioactive natural products are serendipitous drug candidates, which stimulate synthetic approaches for improving and supporting drug discovery and development. Therefore, the search for bioactive metabolites from different natural sources continues to play an important role in fashioning new medicinal agents. Several cyclic peptides were produced by organisms, such as β-defensins, gramicidin S, and tyrocidine A, and exhibited a wide range of bioactivities, such as antiviral activity against HIV-1, influenza A viruses, or antibacterial activity. Cyclic tetrapeptides are a class of natural products tha...
Source: Journal of Natural Medicines - June 14, 2016 Category: Drugs & Pharmacology Source Type: research

Chemical composition and anti-inflammatory activity of the leaves of Byrsonima verbascifolia
This study supports and validates the ethnopharmacological uses of B. verbascifolia as an anti-inflammatory. (Source: Journal of Natural Medicines)
Source: Journal of Natural Medicines - June 8, 2016 Category: Drugs & Pharmacology Source Type: research

Antioxidative activities of 62 wild mushrooms from Nepal and the phenolic profile of some selected species
Abstract Mushrooms have garnered immense popularity for their nutritional as well as medicinal values. The therapeutic potential of mushrooms in Nepal, a country well known for its biodiversity and natural medicinal resources, remains largely unstudied. Therefore, this study attempts to unveil the antioxidative properties of Nepalese wild mushrooms. Sixty-two wild mushroom samples were collected from several forests in different parts of Nepal. Ethanol and water extracts of the dried samples were tested for their antioxidative activities using total phenolic content (TPC), oxygen radical absorbance capacity (ORAC)...
Source: Journal of Natural Medicines - June 4, 2016 Category: Drugs & Pharmacology Source Type: research

A novel α-glucosidase inhibitory constituent from Uncaria gambir
Abstract Bioactivity-guided fractionation of an aqueous methanolic extract of manufactured gambir product from Uncaria gambir with in vitro α-glucosidase inhibitory activity was performed to isolate a novel prenyl resorcinol derivative (1) together with seven known compounds, including two flavone glycosides (2, 3), three catechin analogues (4–6), and two simple phenolics (7, 8). Structures of the isolated compounds were determined by analysis of physical and spectroscopic data (NMR, UV, [α]D, and MS). All isolates were evaluated for in vitro α-glucosidase inhibitory activity. Among the com...
Source: Journal of Natural Medicines - June 4, 2016 Category: Drugs & Pharmacology Source Type: research

Hyperoside reduces albuminuria in diabetic nephropathy at the early stage through ameliorating renal damage and podocyte injury
In this study, we examined the effect of hyperoside, an active flavonoid glycoside, on proteinuria and renal damage in a streptozotocin-induced DN mouse model at the early stage. The results showed that oral administration of hyperoside (30 mg/kg/day for 4 weeks could significantly decrease urinary microalbumin excretion and glomerular hyperfiltration in DN mice, but did not affect the glucose and lipid metabolism. Periodic acid−Schiff staining and transmission electron microscopy showed that glomerular mesangial matrix expansion and podocyte process effacement in DN mice were significantly improved by hype...
Source: Journal of Natural Medicines - June 2, 2016 Category: Drugs & Pharmacology Source Type: research

Artemisinin-based antimalarial research: application of biotechnology to the production of artemisinin, its mode of action, and the mechanism of resistance of Plasmodium parasites
Abstract Malaria is a worldwide disease caused by Plasmodium parasites. A sesquiterpene endoperoxide artemisinin isolated from Artemisia annua was discovered and has been accepted for its use in artemisinin-based combinatorial therapies, as the most effective current antimalarial treatment. However, the quantity of this compound produced from the A. annua plant is very low, and the availability of artemisinin is insufficient to treat all infected patients. In addition, the emergence of artemisinin-resistant Plasmodium has been reported recently. Several techniques have been applied to enhance artemisinin avai...
Source: Journal of Natural Medicines - June 1, 2016 Category: Drugs & Pharmacology Source Type: research

Anti-dormant mycobacterial activity and target molecule of melophlins, tetramic acid derivatives isolated from a marine sponge of Melophlus sp.
Abstract Tuberculosis (TB), caused by Mycobacterium tuberculosis infection, is a major world health problem that is responsible for the deaths of 1.5 million people each year. In addition, the requirement for long-term therapy to cure TB complicates treatment of the disease. One of the major reasons for the extended chemotherapeutic regimens and wide epidemicity of TB is that M. tuberculosis has the ability to persist in a dormant state. We therefore established a new screening system to search for substances with activity against dormant mycobacteria using M. smegmatis and M. bovis BCG cultivated in medium contai...
Source: Journal of Natural Medicines - May 19, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation and quantitative analysis of different growth periods of herb–arbor intercropping systems using HPLC and UV–vis methods coupled with chemometrics
In this study, we employed high-performance liquid chromatography (HPLC) and ultraviolet–visible spectroscopy (UV–vis) combined with chemometrics for determination and qualitative evaluation of several kinds of intercropping system with Gentiana rigescens Franch. ex Hemsl. (GR), which is used as an hepatic protector in local communities in China. Results revealed that GR in a Camellia sinensis intercropping system contained most gentiopicroside, sweroside, and total active constituents (six chemical indicators), whose content reached 91.09 ± 3.54, 1.03 ± 0.06, and 104.05 &...
Source: Journal of Natural Medicines - May 19, 2016 Category: Drugs & Pharmacology Source Type: research

Authentication of the botanical origin of Western herbal products using Cimicifuga and Vitex products as examples
Abstract Various herbal medicines have been developed and used in various parts of the world for thousands of years. Although locally grown indigenous plants were originally used for traditional herbal preparations, Western herbal products are now becoming popular in Japan with the increasing interest in health. At the same time, there are growing concerns about the substitution of ingredients and adulteration of herbal products, highlighting the need for the authentication of the origin of plants used in herbal products. This review describes studies on Cimicifuga and Vitex products developed in Europe and Japan,...
Source: Journal of Natural Medicines - May 17, 2016 Category: Drugs & Pharmacology Source Type: research

Chemical constituents from Inonotus obliquus and their antitumor activities
Abstract Four new lanostane-type triterpenes (inonotusanes D–G, 1–4), including a 24,25,26,27-tetranorlanostane, together with 11 known compounds (5–15), including 7 lanostane derivatives, 2 steroids and 2 aromatic compounds, were isolated from the sclerotia of Inonotus obliquus. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS. To our knowledge, 1 is the first 24,25,26,27-tetranorlanostane-type triterpenoid from fungus, and this is the first time that 31-member lanostane-type triterpenes, 5 and 6, have been isolated from the sclerotia of I. obliquus instead of from its sub...
Source: Journal of Natural Medicines - May 14, 2016 Category: Drugs & Pharmacology Source Type: research

Characterization of α-humulene synthases responsible for the production of sesquiterpenes induced by methyl jasmonate in Aquilaria cell culture
Abstract The resinous portions of Aquilaria and Gyrinops plants are known as ‘agarwood’ and have a distinctive fragrance. To examine the biosynthesis of these fragrant compounds, we previously established cell cultures of Aquilaria crassna in which the production of three sesquiterpenes (α-guaiene, α-humulene, and δ-guaiene) could be induced by methyl jasmonate (MJ), and showed that cloned δ-guaiene synthase from MJ-treated cells is involved in the synthesis of these three compounds, although only very small amounts of α-humulene are produced. In the pre...
Source: Journal of Natural Medicines - May 14, 2016 Category: Drugs & Pharmacology Source Type: research

Acylated oleanane-type triterpene saponins from the flowers of Bellis perennis show anti-proliferative activities against human digestive tract carcinoma cell lines
Abstract Seven oleanane-type triterpene saponin bisdesmosides, perennisaponins N–T (1–7), were newly isolated from a methanol extract of daisy, the flowers of Bellis perennis L. (Asteraceae). The structures were determined based on chemical and physicochemical data and confirmed using previously isolated related compounds as references. The isolates, including 13 previously reported perennisaponins A–M (8–20), exhibited anti-proliferative activities against human digestive tract carcinoma HSC-2, HSC-4, and MKN-45 cells. Among them, perennisaponin O (2, IC50 = 11.2, 14.3, and 6.9&n...
Source: Journal of Natural Medicines - May 13, 2016 Category: Drugs & Pharmacology Source Type: research

Protective effect of Mimosa pudica L. in an l -arginine model of acute necrotising pancreatitis in rats
Abstract Mimosa pudica is used in traditional medicine for treating various disorders such as inflammatory conditions, diarrhoea, insomnia, alopecia, urogenital infections and wounds. The present study investigated the effect of M. pudica extract (MPE) on l-arginine-induced acute necrotising pancreatitis in rats. The ethanolic extract of M. pudica leaves was studied for the presence of quercetin and gallic acid using high-performance liquid chromatography. Four groups were employed—normal control rats, l-arginine control rats (two intraperitoneal [i.p.] injections of 2 g/kg at an interval...
Source: Journal of Natural Medicines - May 10, 2016 Category: Drugs & Pharmacology Source Type: research

Application of a new method, orthogonal projection to latent structure (OPLS) combined with principal component analysis (PCA), to screening of prostaglandin E 2 production inhibitory flavonoids in Scutellaria Root
In this report, extracts of 52 Scutellaria Root (the root of Scutellaria baicalensis Georgi) samples were analyzed by high-performance liquid chromatography (HPLC), and their inhibitory activities towards prostaglandin E2 (PGE2) production in a murine macrophage-like cell line J774.1 were examined. Wogonin and oroxylin A were predicted to be strong inhibitors of PGE2 production by OPLS analysis of the data. However, 6-methoxywogonin, which has been reported to have inhibitory activity, was omitted. Modified PCA was then applied to these data as a filter to exclude compounds less relevant to the activity, and OPLS anal...
Source: Journal of Natural Medicines - May 10, 2016 Category: Drugs & Pharmacology Source Type: research

Application of a quantitative 1 H-NMR method for the determination of paeonol in Moutan cortex, Hachimijiogan and Keishibukuryogan
Abstract Quantitative 1H-NMR (1H-qNMR) was applied to the determination of paeonol concentration in Moutan cortex, Hachimijiogan, and Keishibukuryogan. Paeonol is a major component of Moutan cortex, and its purity was calculated from the ratio of the intensity of the paeonol H-3′ signal at δ 6.41 ppm in methanol-d 4 or 6.40 ppm in methanol-d 4 + TFA-d to that of a hexamethyldisilane (HMD) signal at 0 ppm. The concentration of HMD was corrected with SI traceability by using potassium hydrogen phthalate of certified reference material grade. As a r...
Source: Journal of Natural Medicines - May 10, 2016 Category: Drugs & Pharmacology Source Type: research

Two new lignans and melanogenesis inhibitors from Schisandra nigra
Abstract An acetone extract from the stems of Schisandra nigra Max. (Schisandraceae) exhibited significant inhibition of 3-isobutyl-1-methylxanthine (IBMX)-stimulated melanogenesis in murine B16 melanoma F10 cells. Fractionation and purification of the extract led to the isolation of two new tetrahydrofuran-type lignans, (+)-5-methoxyzuonin A (2) and kadlongirin C (3), along with eight known compounds (1, 4–10). The structures of the new compounds were determined by spectroscopic analyses. Of the isolated compounds (1, 3 –10), (+)-zuonin A (1) showed remarkable inhibition of melanogenesis at conce...
Source: Journal of Natural Medicines - May 3, 2016 Category: Drugs & Pharmacology Source Type: research