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The roots of Achyranthes bidentata Blume are one of the regularly used herbal drugs in Chinese medicine, and has been applied for strengthening the muscle and bone for a long time. However, its effect on muscle remains unclear. This paper aims to explore the anti-muscle atrophy effect of A. bidentata , and to clarify the possible signaling pathways involved. The saponin extract of the roots of A. bidentata (ABSE) was prepared and analyzed, and its activity on myoblast differentiation was assayed with C2C12 cell culture. ABSE was then orally administered at dosage of 35, 70 and 140 mg/kg/day to disuse-induced muscle atrophy mice. The studies on mice body weight and muscle quality were conducted, and Western blot was used for exploring the possible signaling pathways involved in the muscle protective action aided with transcriptome analysis. The total saponin content of ABSE was 59.1%. ABSE promoted the C2C12 cells differentiation to myotube in C2C12 differentiation assay. Further study with disuse-induced muscle atrophy mice model demonstrated that ABSE significantly increased muscle fiber diameter as well as the proportion of slow muscle fibers. Possible mechanism study aided with transcriptome analysis revealed that ABSE alleviated muscle atrophy at least through activation of PI3K/Akt pathway in vivo & vitro. The saponin extract of the root of A. bidentata (ABSE) has a protective effect on muscle atrophy, and showed a considerable potential in prevention and treatment of muscle atrophy. [Display omitted] • The saponin extract of A. bidentata (ABSE) was prepared and analyzed. • ABSE promoted the differentiation of C2C12 cells to myotubes. • ABSE displayed a protective effect on muscle atrophy in vivo. • ABSE activated PI3K/Akt pathway in vivo & in vitro. • ABSE increased protein levels of Myogenin and MyoD. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Da-Huang-Fu-Zi-Tang (DHFZT) is a crucial TCM formula commonly used for the treatment of acute pancreatitis in Chinese clinical application. Our previous work found that DHFZT could act against pancreatic injury in rats with severe acute pancreatitis (SAP). The goal of this paper was to study the underlying correlations between the chemical spectra and the protective effect of DHFZT on pancreatic acinar cell to reveal the real bioactive compounds in DHFZT. Materials and methods: The fingerprint chromatograms of rat serum after oral administration of DHFZT were established by UHPLC-ESI-Q-TOF-MS technique. At the same time, the model of anti-acute pancreatitis on cells was established by adding 10?7 mol/L cerulein to AR42J cell line, and the protective effects of the serum on pancreatic acinar cell from injury was evaluated by detecting the efficacy of amylase. Then, the spectrum–effect relationships between UHPLC fingerprints and anti-acute pancreatitis activities were evaluated using canonical correlation analysis (CCA) statistical method. The chromatogram separation was performed on a C18 reversed phase UHPLC column (2.1mm×100mm, 3.5?m, Agilent), the column temperature was set at 35°C. The mobile phase consisted of 0.1% formic acid and acetonitrile with gradient elution. The serum samples were analyzed both in negative and positive ion mode. The mother and productive ions were scanned within the mass range of m/z 100–1200 and 50–1200, respectively. A thorough analysis of a great deal of information of the constituents in the rat serum was undertaken. The structure identification of the detected compounds was achieved by using high resolution MS values as well as the MS/MS fragments. Results: Eighteen peaks in rat serum after oral administration of DHFZT were detected within only 30min recorded chromatograms. The structure of the 18 compounds were then given out, of which 10 were the original form of compounds absorbed from DHFZT, 8 were the metabolites of the compounds existed in rat serum. According to the CCA results, talatisamine, rhein glucoside, rhein isomer methylation, hypaconine, hydroxyl-chrysophanol, emodin glucuronide conjugation, and chrysophanol glucuronide conjugation were finally found to be the main anti-acute pancreatitis components in DHFZT. Conclusions: The model presented in this paper successfully discovered the spectrum–effect relationships of DHFZT, which showed a representative way to discover the primary active ingredients from the complicated herbal drugs. [Copyright &y& Elsevier]

Ethnopharmacological relevance Metabolomics is the comprehensive assessment of endogenous metabolites of a biological system in a holistic context, and its property consists with the global view of Traditional Chinese Medicine (TCM). Shuihonghuazi Formula (SHHZF) has been used for liver cancer early treatment in clinical for more than thirty years, but its mechanism remains unclear completely. This paper was designed to explore the therapeutic effects of SHHZF on liver cancer and its metabolomic characters. Materials and methods All the rats were given diethylnitrosamine (DEN) at the dosage of 70 mg/kg for 14 weeks. From the 7th weeks, SHHZF was given to the rats which lasted for 10 weeks. Therapeutic effects of SHHZF was compared with that of cyclophosphamide (CTX). High performance liquid-chromatography/electrospray-ionization time of flight mass spectrometer (HPLC/ESI-TOF-MS) combined with pattern recognition approaches including principal component analysis (PCA), partial least squares-discriminant analysis (PLS-DA), was integrated to approximate the comprehensive metabolic signature and discover differentiating metabolites by Agilent MPP 12.1. The changes in metabolic profiling in plasma were restored to their baseline values after SHHZF treatment according to the PLS-DA score plots. Results The results indicated that 23 ions as “differentiating metabolites”. The alterations in those metabolites were associated with perturbations in fatty acid and bile acid metabolism, in response to liver cancer through immune and nervous system. And SHHZF could increase the uptake and utilization of linoleic acid and oleic acid, increase arachidonic acid-like substance content and enhance organism immunity of liver cancer rats. And it also could increase the translation from phosphatidylethanolamine (PE) to phosphatidylcholine (PC), linoleic acid metabolism and inhibits abnormal metabolism of bile acid. Conclusions The mechanism of therapeutic effects of SHHZF on liver cancer by adjusting the activities of PE N-methyl transferase (PEMT), Lysophospholipase D, methylenetetrahydrofolate reductase (MTHFR) and lysophospholipase was elucidated by the method of metabonomics for the first time. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Schizonepeta tenuifolia Briq. (ST) herbs have been used as a Traditional Chinese Medicine (TCM) for treating colds for thousands of years. The volatile oil is considered as the main material basis responsible for the efficacy of ST and has attracted lots of attention on its anti-inflammatory effect recently. Aim of study This paper investigated the anti-inflammatory effects of the distilled volatile oils from Schizonepeta tenuifolia (STVO) that were collected at different harvesting times on carrageenin-induced pleurisy in rats. Based on the anti-inflammatory effects, instead of contents of marker components, we aim to evaluate the quality and determine the appropriate harvesting time of ST. Materials and methods There were eleven groups with eight male rats in each randomly. They were model group, control group, positive group (dexamethasone) and eight groups treated with eight STVOs at different harvesting times. All treatments were performed by gavage and administered once a day on four consecutive days. One hour after the last treatments, except the rats in control group, those in other groups were treated with carrageenin to induce the pleurisy. Four hours later, all the rats were sacrificed and their pleurisy exudates and lung tissues were collected for further analysis. To evaluate the comprehensive anti-inflammatory effect of the eight STVOs, multi-attribute comprehensive index method (MACIM) was used to obtain the integration of various effects. Results All the eight STVOs could decrease the seven indicators relating to pleurisy, which were exudate volume, leukocytes, protein level, myeloperoxidase (MPO), malondialdehyde (MDA), tumor necrosis factor-α (TNF-α) and interleukine-1β (IL-1β). Majority of these decreases were significant (P<0.01, P<0.05). As far as each indicator was concerned, each STVO showed different effect from others. With MACIM, it was found that STVO in Group 6 was the most effective one with the highest V s and appropriate harvesting time of ST was in late September. Conclusions The study may provide scientific basis to further understanding of the mechanism of STVO in anti-inflammatory effect of carrageenin-induced pleurisy. Meanwhile, this study also provides a new access to determining the appropriate harvesting time of TCM and even evaluating the quality of TCM. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Roots of Angelica sinensis ( Oliv. ) Diels (AS) a commonly used herbal, always act as an anti-inflammatory drug in Chinese traditional therapy. In clinical use, AS is always processed before being used for the reason that processing can increase its therapeutic effect. Recent studies have shown that volatile oil of AS (VOAS), an important component in AS, has evident anti-inflammatory activities. Aim of the study In this study, our aim is to evaluate the anti-inflammatory effects of volatile oils from processed products of AS. Materials and methods In this paper, volatile oils from stir-fried AS (C-VOAS), parched AS with alcohol (J-VOAS), parched AS with soil (T-VOAS), and parched AS with sesame oil (Y-VOAS) were applied to intervene the carrageenan-induced acute inflammation model rats. GC–MS based metabolomics was utilized to determine different metabolites in the inflammatory exudate and plasma samples. Results The results showed that VOASs could significantly inhibit the release of PGE2, HIS, 5-HT and TNF- α , among which C-VOAS and J-VOAS expressed better effect. Otherwise, 14 potential biomarkers were identified respectively in inflammatory exudate and plasma, which changed highly significantly ( P <0.01) in C-VOAS and J-VOAS groups. Conclusions We inferred that the anti-inflammatory effect of C-VOAS and J-VOAS were superior to other VOASs. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Pharmacokinetic studies on traditional Chinese medicine are useful to evaluate and predict the drug efficacy and safety. The renal impairment may affect drug clearance and other pharmacokinetic processes which can increase toxicity and drug to drug interactions or cause ineffective therapy. Pharmacokinetic studies in pathological status rats might be meaningful for revealing the action mechanism and improving clinical medication of the herb medicine. Materials and methods A highly sensitive and rapid ultra-performance liquid chromatography–mass spectrometry (UPLC–MS) method with multiple-reaction monitoring (MRM) mode was developed and validated for simultaneous quantitation of morroniside and loganin in normal and doxorubicin-induced chronic kidney disease (CKD) rat plasma after oral administration of Shanzhuyu (fruit of Cornus officinalis ) extract. Results Both calibration curves gave satisfactory linearity ( r >0.99) at linear range of 1.96–1962.5 ng mL −1 for morroniside, 1.53–1531.25 ng mL −1 for loganin. The precision and accuracy of the in vivo study were assessed by intra-day and inter-day assays. The percentages of relative standard deviation (RSD) were all within 9.58% and the accuracy (RE) was in the −6.02% to 8.11% range. The extraction recoveries of morroniside, loganin and internal standard (IS) were all >67.62% and the matrix effects ranged from 95.07% to 102.75%. Conclusions The pharmacokinetic behavior of morroniside and loganin in normal and CKD rat plasma was determined in this paper. The significant different pharmacokinetic parameters might partly result from the changes of P-glycoprotein and metabolic enzymes in the pathological state. The pharmacokinetic research in the pathological state might provide more useful information to guide the clinical usage of the herb medicine. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Schefflera octophylla (Lour.) Harms, a traditional Chinese herb mainly distributed in Southeast Asia, is extensively prescribed to alleviate pain and treat rheumatoid arthritis (RA), influenza, throat swelling, pain, etc. In this paper, the antinociceptive and anti-inflammatory activities of the ethanol extract and its five different polar fractions of this plant were evaluated. Furthermore, the anti-rheumatoid arthritis activity of the ethanol extract and its active fraction (CHCl 3 fraction) were evaluated. And the chemical constituents of the CHCl 3 active fraction displayed significant antinociceptive and anti-inflammatory activities were investigated. Materials and methods Antinociceptive and anti-inflammatory activities were investigated by hot plate test, acetic acid-induced abdominal writhing test and formalin test, xylene-induced ear edema test. The anti-rheumatoid arthritis activity was evaluated through the model of adjuvant-induced arthritis (AA) in rats, paw swelling, pain response, arthritis index and histopathological changes of ankle, the levels of TNF-α, IL-1β, IL-6 and rheumatoid factor (RF) of rats were detected. The chemical constituents of the CHCl 3 fraction were isolated using chromatographic techniques. Their structures were elucidated by spectroscopic data analysis. Results The results showed that the ethanol extract of S. octophylla has significant dose-dependent anti-inflammatory and antinociceptive activities. And its five different polar fractions especially the CHCl 3 fraction significantly inhibited the abdominal writhing induced by acetic acid and ear edema induced by xylene, also increased pain threshold in hot plate test in 120 min and reduced ticking times in formalin test. The ethanol extract of S. octophylla and the CHCl 3 fraction demonstrated an anti-RA effect in a dose-dependent manner. The levels of TNF-α, IL-1β and IL-6 in ethanol extract (600 mg/kg) and CHCl 3 fraction (300 mg/kg) groups were significantly lower than those of the model group. The chemical constituents study of the CHCl 3 fraction from S. octophylla led to six triterpenoids which were identified as taraxerone ( 1 ), 3-epi-taraxerol ( 2 ), aleuritolic acid ( 3 ), 3-oxofriedelan-28-oic acid ( 4 ), 3β,19α -dihydroxy-urs-12-ene- 24,28-dioic acid ( 5 ) and asiatic acid ( 6 ). Compounds 1 – 5 were obtained from this plant for the first time. Conclusion This study proved the antinociceptive, anti-inflammatory and anti-rheumatoid arthritis activities of S. octophylla. Triterpenoids obtained from its CHCl 3 fraction may be responsible for those activities. These results could support the fact that S. octophylla is used traditionally to cure inflammatory and pain diseases. [ABSTRACT FROM AUTHOR]

Our recently published paper demonstrated that ethyl acetate fractions obtained from Cymbopogon citratus (DC.) Stapf (C. citratus) leaves, which are consumed as infusion in folk medicine due to their therapeutic properties, are rich in polyphenols and exhibit promising antioxidant activity by acting through different mechanisms in vitro. However, studies regarding the toxicity of these fractions are necessary to investigate their safe use in future biomedical applications. This study aimed to investigate the toxicity of ethyl acetate (obtained in acidic and basic conditions and after the essential oil removal from the leaves) and chloroform fractions, essential oil, and its pure constituents, citral and geraniol. The toxicity of C. citratus samples was evaluated by using Artemia salina (A. salina) and human blood cells (leukocytes and erythrocytes). The A. salina lethality assay demonstrated that C. citratus fractions were moderately toxic with LC 50 values ranging from 146.12 to 433.15 μg mL−1, whereas the essential oil and isolated compounds were highly toxic with LC 50 lower than 100 μg mL−1. Leukocyte viability decreased after incubation in the presence of the fractions obtained after the essential oil removal from the plant leaves, as well as in the presence of essential oil, citral and geraniol. The same samples increased the osmotic fragility of erythrocytes, and field emission gun scanning electron microscopy (FESEM) analysis revealed significant changes in cell morphology. Interestingly, our results suggest that the previous removal of essential oil from plant leaves facilitated the extraction of cytotoxic compounds from C. citratus. It was demonstrated that C. citratus ethyl acetate and chloroform fractions, essential oil, as well citral and geraniol were considered toxic to A. salina , cytotoxic to human blood cells and showed to induce alterations in the erythrocyte membrane at higher concentrations. These fractions will be further investigated to identify the phytochemicals involved in the observed cytotoxic effects and explored using in vivo models. [Display omitted] • Cymbopogon citratus samples and isolated compounds were toxic for Artemia salina. • Citral, geraniol and essential oil increased osmotic fragility in human erythrocytes. • FESEM analysis showed that some samples changed erythrocytes morphology. • The removal of essential oil from leaves enhanced the extraction of cytotoxic compounds. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The use of medicinal plants in Gabon contributes widely to the primary health care of the people of this area of Central Africa. This paper investigates the pharmacological properties of Dichrostachys cinerea, the plant barks are traditionally used by Gabonese and Ivorian populations to treat bronchial asthma, rheumatism, and other various diseases. Although D. cinerea barks have been reported to be used by population to facilitate childbirth, to the best of our knowledge no scientific evidence has been published. Aim of study In the present study, we investigated the pharmacological properties of D. cinerea methanolic extract, on isolated uterine smooth muscle and compared its effects to those of oxytocin, which is used by obstetricians to facilitate childbirth. We also explored the possible mechanism pathways of the in vitro uterine contraction induced by D. cinerea . Materials and methods The effects of different concentrations (3.2 µg/ml, 16 µg/ml, 80 µg/ml, 400 µg/ml, and 2 mg/ml) of the methanolic extract of D. cinerea on isolated strips of the uteri of pregnant rats were studied. These effects were compared to those of oxytocin (8.4×10 –5 µg/ml, 8.4×10 –4 µg/ml, 8.4×10 –3 µg/ml, 8.4×10 –2 µg/ml). The EC (50) and E (max) was determined graphically and statistically analysed using one-way ANOVA and Dunnett post hoc test. Results Cumulative concentrations of D. cinerea have caused rise in the contractile force of the uterine fragments that were isolated from the pregnant rats, as seen with oxytocin concentrations. We observed contractions amplitude of 30.41 mN (12%) at 80 µg/ml and amplitude of 39.68 mN (14.17%) at 400 µg/ml for D. cinerea. In parallel, oxytocin concentration of 8.4×10 –3 µg/ml induced contractions of 45.82 mN with the highest concentration (8.4×10 –2 µg/ml) that induced contractions of 55.82 mN. Conclusions Our results revealed that D. cinerea increased the contractile force and the frequency of muscle contractions. These findings support the use of D. cinerea to facilitate childbirth, as it has been used in traditional medicine. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Triticum vulgare has been extensively used in traditional medicine thanks to its properties of accelerating tissue repair. The aqueous extract of Triticum vulgare (TVE) is currently an active component used by Farmaceutici Damor in the manufacture of certain pharmaceutical products already marketed in Italy and abroad under the brand name Fitostimoline ® , in the formulation of cream and medicated gauze and is commonly used for the treatment of decubitus ulcers, sores, burns, scarring delays, dystrophic diseases, and, more broadly, in the presence of problems relating to re-epithelialization or tissue regeneration. The active components of Fitostimoline ® -based products determine a marked acceleration of tissutal repairing processes, stimulate chemotaxis and the fibroblastic maturation, and significantly increase the fibroblastic index, which are crucial points in the repairing processes. The aim of the present paper was to identify and characterize the active fractions of TVE responsible for the pharmacological effect in tissutal repairing processes. Materials and methods Several fractions obtained from TVE by ultrafiltration procedures and HPAE chromatography were tested to measure their growth-enhancing activity on NIH-3T3 fibroblasts. The healing action of the same fractions, prepared as cream formulation, was assessed in rat subjected to two different models of skin lesion, skin scarification and excision. Results Our results showed a pro-proliferative effect of the fractions ST-98 and K>1000 in NIH-3T3 fibroblasts. Moreover these fractions formulated as cream preparations were effective also in in vivo models of skin lesion. Conclusions The results of the present study showed that these active fractions of TVE are responsible for its pro-proliferative effect. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Alismatis rhizoma or Alisma orientale (Zexie in Chinese), the dried rhizome of Alisma orientale Juzepzuk (Alismataceae), is a well-known traditional Chinese medicine and is used as an agent for diuresis and for excreting dampness in China and Japan. In this paper, we report the diuretic activities of the petroleum ether fraction, the ethyl acetate fraction, the n-buthanol fraction, and the remaining fraction, of the ethanol extract of Alismatis rhizoma (AR). Materials and methods The single dose of the petroleum ether fraction, the ethyl acetate fraction, the n-buthanol fraction, and the remaining fraction, of the ethanol extract of AR were orally administered to rats. Urinary excretion rate, pH and electrolyte excretion were measured in the urine of saline-loaded rats. Results In this study, the 100 and 400 mg/kg doses of the ethyl acetate fraction and the 12.5, 25 and 50 mg/kg doses of the n-butanol fraction all produced an increase in urine volume excretion, and all produced a remarkable increase in urine electrolyte excretion. Although the 800 mg/kg doses of the ethyl acetate fraction, the 75 and 100 mg/kg doses of the n-butanol fraction and the 12.5, 25 and 50 mg/kg doses of the remaining fraction significantly decreased the urine output in 6 h, the urine Na + and Cl − excretion were markedly decreased with the n-butanol fraction (75 and 100 mg/kg doses) and the remaining fraction (12.5, 25 and 50 mg/kg doses) while the ethyl acetate fraction at 800 mg/kg doses had slight effect on urine electrolyte excretion. The petroleum ether fraction did not show remarkable diuretic activity in comparison with control group. Conclusions Our present study determined that the ethyl acetate fraction and the n-butanol fraction present notable diuretic effects, and we found a dual effect on renal function showed by AR, including promoting diuretic activity and inhibiting diuretic activity. The components with strong polarities in AR may have anti-diuretic activities, which might be an effect of promoting the sodium-chloride co-transporter in the distal tubule. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Sandpaper [ Ficus exasperata Vahl (Moraceae)] leaf has been reportedly used in folklore for the management/treatment of cardiovascular diseases with little/or no scientific basis for their action. This study sought to investigate the effect of dietary supplementation of sandpaper leaf on angiotensin-I converting enzyme (ACE) activity in hypercholesterolemia as well as the effect of their phenolic extract on this enzyme in vitro . Materials and methods The phenolic extract was prepared, then, the inhibitory effect of the leaf extract on ACE was determined in vitro . Thereafter, the effect of dietary supplementation of sandpaper leaf on angiotensin-I converting enzyme (ACE) activity in high cholesterol diet fed rats for 14 days was evaluated as well as some biochemical parameters. Results The result revealed that under in vitro condition, the phenolic extract inhibited ACE (IC 50 =14.7 µg/mL) in a dose-dependent manner (0–10 µg/mL). Feeding high cholesterol diets to rats caused a significant ( P <0.05) increase in the ACE activity. However, there was a significant ( P <0.05) decrease in the ACE activity as a result of supplementation with the sand paper leaves. Furthermore, there was a significant ( P <0.05) increase in the plasma lipid profile with a concomitant increase in malondialdehyde (MDA) content in rat liver and heart tissues. However, supplementing the diet with sandpaper leaf (either 10% or 20%) caused a significant ( P <0.05) decrease in the plasma total cholesterol (TC), triglyceride (TG), very low density lipoprotein-cholesterol (VLDL-C), and low-density lipoprotein-cholesterol levels (LDL-C), and in MDA content in the tissues. Conversely, supplementation caused a significant ( P <0.05) increase in plasma high-density lipoprotein-cholesterol level when compared with the control diet. Reversed phase HPLC analysis of the extract revealed Quercitrin (43.7 mg/g), chlorogenic acid (42.8 mg/g) and caffeic acid (33.9 mg/g) as the major phenolics in the leaf. Conclusion The inhibition of ACE activity and prevention of hypercholesterolemia by sandpaper leaf could be part of the possible mechanism underlying its anti-hypertensive property which could lay credence to its use in folk medicine. However, these activities may be directly/indirectly attributed to the polyphenolics present. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Acorus tatarinowii Schott (AT), belong to the family Araceae, is perennial herbaceous plant mainly present in China, Japan and India. The rhizomes of AT have been used as a famous traditional Chinese medicine for the treatment of central nervous system related diseases. Aim of the study A selective, accurate and sensitive method using gas chromatography-mass spectroscopy (GC–MS) for the simultaneous determination and pharmacokinetic study of β -asarone, α -asarone, elemicin and cis -methyl isoeugenol in rat plasma was developed and validated. Materials and methods The GC–MS system was operated under selected ion monitoring (SIM) mode. The samples were prepared by protein precipitation with acetonitrile after being spiked with an internal standard (1-naphthol). The GC separation was achieved on a DB-1701 column (60 m × 0.25 mm ID, and 0.25 µm film thickness). Results The current GC/MS assay was validated for linearity, intra-day and inter-day precisions, accuracy, extraction recovery and stability. The analyte calibration curves were linear over a wide concentration range and the lowest limit of quantifications (LLOQ) were 5.53 ng/mL ( β -asarone), 6.50 ng/mL ( α -asarone), 3.10 ng/mL (elemicin) and 7.60 ng/mL ( cis -methyl isoeugenol). After oral administration 0.9 g /Kg of AT rhizomes, the maximum plasma concentration (Cmax) was 2508.6±498.7 ng/mL for β-asarone, 257.5±37.1 ng/mL for α -asarone, 345.5±33.4 ng/mL for elemicin and 452.7±59.1 ng/mL for cis-methyl isoeugenol, respectively. The time to reach the maximum plasma concentration ( T max ) was 1.42±0.18 h for β -asarone, 1.58±0.19 h for α -asarone, 1.67±0.24 h for elemicin and 1.75±0.38 h for cis -methyl isoeugenol, respectively. Conclusion This paper described a simple, sensitive and validated GC–MS method for simultaneous determination of four phenylpropanoids in rat plasma after oral administration of the essential oil of AT rhizomes and investigated on their pharmacokinetics studies as well. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Jiao-Tai-Wan (JTW), an important herbal formula consists of Rhizoma coptidis and Cortex cinnamomi powder, is a famous prescription which has been used for centuries to treat insomnia in Traditional Chinese Medicine. The purpose of this study is to compare the pharmacokinetic properties of five protoberberine-type alkaloids (i.e. berberine, palmatine, coptisine, epiberberine and jatrorrhizine), the main bioactive constituents in JTW, between normal and insomnic rats. We also investigate the differences between single-dose and multiple-dose pharmacokinetics of five protoberberine-type alkaloids. Materials and methods: The insomnic rat models were induced by intraperitoneal injection of one-dose para-chlorophenylalanine acid (PCPA). Quantification of five protoberberine-type alkaloids in rat plasma was achieved by using a rapid LC–MS/MS method. Plasma samples were collected at different time points to construct pharmacokinetic profiles by plotting drug concentration versus time and estimate pharmacokinetic parameters. An unpaired Student׳s t test was used for comparisons with SPSS 17.0. Results: The five protoberberine-type alkaloids of single-dose normal groups had slow absorption and low bioavailability, as well as a delay of peak time. In the single-dose oral administration, the C max and T max of five ingredients in insomnic rats had significant differences compared with those of normal rats. In the multiple-dose oral administration, the pharmacokinetic parameters of five protoberberine-type alkaloids varied greatly in insomnic rats. In the normal rats, there were significant differences (P<0.05) in the principal pharmacokinetic parameters such as C max and T max between single-dose and multiple-dose oral administration. In the insomnic rats, the five ingredients of multiple-dose groups showed better absorption than the single-dose groups. Particularly, three peaks were observed in multiple-dose model group of plasma–concentration curves. Conclusions: The pharmacokinetic behavior of five protoberberine-type alkaloids was described in this paper. In both normal groups and model groups, the pharmacokinetic behavior of multiple-dose had significant differences comparing with the single-dose; either single-dose or multiple-dose, the pharmacokinetic behavior of insomnic rats had significant differences comparing the normal rats. Multiple dosing may improve the absorption of JTW in insomnic rats, which will increase the bioavailability and bring into active role in therapeutical effect. [Copyright &y& Elsevier]

Premna microphylla turcz is traditionally used as a folk remedy. Its roots, stems and leaves can be invoked as medicines, which have the functions of detoxification, swelling and hemostasis. It belongs to the Premna in the Verbenaceae and is mainly distributed in the mountains of southeastern China. However, there are few reports of in-depth studies on the anti-inflammatory effects of polysaccharide, which was the main component in Premna microphylla turcz. The flies were fed with standard corn flour-yeast medium to cause inflammation by sodium lauryl sulfate (SDS). The treatment group contained Premna microphylla turcz polysaccharide (pPMTLs) extract. The survival rate was obtained by feeding a vial containing five layers of filter paper, which was infiltrated with the 5% sucrose solution contaminated with SDS or SDS polysaccharide. The microvilli and nucleus of the midgut epithelial cells of different treatments were observed by transmission electron microscope, and the expression of inflammation-related genes was detected by real-time quantitative PCR (qRT-PCR). Finally, 16S rDNA analysis was conducted on the differences in the composition of the intestinal microbes of Drosophil a. In the current study, we showed that pPMTLs significantly prolonged the life span of SDS-inflamed flies from 5 days to 6 days. And pPMTLs reduced the rupture of microvilli in the midgut and restored the nuclear structure. In addition, pPMTLs significantly improved expression level of immune-related genes in Inflammation Drosophila especially the defensin (4.32 ± 0.75 vs 9.97 ± 0.52 SDS-polysaccharide group: SDS group, p < 0.001). The analysis of intestinal microbiota showed that pPMTLs decreased the relative abundance of Raoultella while Wolbachia increased (p < 0.05). Collectively, our results revealed the potential application of pPMTLs in enhancing inflammation defense, which would be enormous significance for the inflammation-related disorders treatment. • PMTLs polysaccharides showed excellent immunomodulatory activity in vivo. • Intestinal immunity was significantly enhanced by PMTLs polysaccharides. • Polysaccharides effectively reduced harmful intestinal bacteria. • Polysaccharides could significantly improve the expression of AMPs. [ABSTRACT FROM AUTHOR]

According to the theory of traditional Chinese medicine, the main pathogenesis of severe hand, foot and mouth disease (HFMD) is that the heat and wet poisons are deeply trapped in the viscera, which causes the deficiency of Qi and Yin in the patient's body. Ginsenoside Rb1 (Rb1) is the most abundant triterpenoid saponin in Panax quinquefolius L., which has the function of Qi-invigorating and Yin-nourishing. Enterovirus 71 (EV71) is one of the causative pathogens of HFMD, especially the form associated with some lethal complications. Therefore, the therapeutic effect of Rb1 on this disease caused by EV71 infection is worth exploring. We explored the effective antiviral activities of Rb1 against EV71 in vitro and in vivo and investigated its preliminary antiviral mechanisms. EV71-infected two-day-old suckling mice model was employed to detect the antiviral effects of Rb1 in vivo. To detect the antiviral effects of Rb1 in vitro, cytopathic effect (CPE) reduction assay was performed in EV71-infected Rhabdomyosarcoma (RD) cells. Interferon (IFN)-β interference experiment was employed to detect the antiviral mechanism of Rb1. In this paper, we first found that Rb1 exhibited strong antiviral activities in EV71-infected suckling mice when compared to those of ribavirin. Administration of Rb1 reduced the CPE of EV71-infected RD cells in a dose-dependent manner. Moreover, EV71-induced viral protein-1 (VP-1) expression was significantly reduced by Rb1 administration in vitro and in vivo. Furthermore, Rb1 treatment could induce high cellular and humoral immune responses in vivo. Meanwhile, Rb1 contributed to the enhanced Type I IFN responses and IFN-β knockdown reversed the antiviral activity of Rb1 in vitro. In summary, our findings suggest that Rb1 is an immune-stimulatory agent and provide an insight into therapeutic potentials of Rb1 for the treatment of EV71 infection. Image 1 [ABSTRACT FROM AUTHOR]

Dalbergia pinnata (Lour.) Prain (D. pinnata) is a plant widely distributed in tropical and subtropical regions of Asia, Africa, and the Americas. In humans, it is used in the prevention and treatment of diseases such as respiratory system, digestive system, cardiovascular and cerebrovascular diseases. This study was aim to evaluate chemical composition, antioxidant activities, antimicrobial, and anti-melanogenesis properties of Essential oils (EO) from D. pinnata. In this paper, the EO of D. pinnata were extracted using the supercritical CO 2 extraction method and purified by molecular distillation. The volatile compounds of EO were characterized using Gas Chromatography-Mass Spectrometer (GC-MS). The antioxidant activities were evaluated by the methods of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, 2, 2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging assays. And two Gram-positive bacteria, three Gram-negative bacteria and a fungus were employed to evaluate the antimicrobial activity. The zebrafish was used as experimental model to evaluate the anti-melanogenesis effect of the EO from D. pinnata. The EO of D. pinnata were obtained in a yield of 4.75% (v/w) calculated on dry weight basis. 14 volatile compounds could be detected and the predominant components include elemicin (91.06%), methyl eugenol (3.69%), 4-allyl-2,6-dimethoxyphenol (1.16%), and whiskey lactone (0.55%). The antioxidant assay showed that the EO could scavenge DPPH (IC50 values of 0.038 mg/mL) and ABTS (IC50 value of 0.032 mg/mL) free radical, indicating that the EO had strong antioxidant activity. The results of antimicrobial test showed that Staphylococcus aureus was most sensitive to EO with minimal inhibitory concentration (MIC) of 0.78 μL/mL, followed by Streptococcus pyogenes (6.25 μL/mL) and Candida albicans (12.5 μL/mL). Gram-negative strains, including Escherichia coli , Pseudomonas aeruginosa and Salmonella typhimurium , were slightly affected by the EO. Additionally, EO from D. pinnata could reduce tyrosinase activity and melanin synthesis of zebrafish embryos in dose-dependent manner. And EO exhibited the more obvious anti-melanogenic effect compared with the positive control arbutin at the same dose (30 mg/L). Our results validated the main activities attributed to D. pinnata for its antimicrobial and antioxidant. In addition, the potent inhibitory impacts of EO on the pigmentation provides a theoretical basis for the in-depth study of the EO from D. pinnata and their application in pharmaceutical and cosmetic industries. Image 1 [ABSTRACT FROM AUTHOR]

The use of herbal medicines is increasing in developed countries as alternative and/or supportive therapy to conventional health care medicines. Malva neglecta Wallr. (Family: Malvaceae) has been reported as wound healing remedy in traditional medicines, however no experimental data is available on its wound healing potentials. The aim of this study was to explore phytochemistry and validate wound healing potentials of the plant using animal models. M. neglecta crude methanolic extract (Mn.Cme) was chemically characterized using HPLC-DAD and GCMS analysis. Acute dermal toxicity was determined in albino rats following Organization of Economic Co-operation and Development (OECD) 402 established standards. Wound healing potentials were evaluated in rats using excision wound model. Wounds (177 mm2) were made by an excision on the skin of rats which were placed individually in cages. Mn.Cme was formulated in ointment form and was applied topically onto the wound area once daily for 14 days. The wound area was measured with translucent paper and thereafter estimated on a 1 mm2 graph sheet every 3rd day until epithelialization and complete wound closure was recorded. Wound contraction was calculated as a percentage of the original wound size. Antioxidant potentials were also evaluated via FRAP, DPPH and H 2 O 2 free radicals scavenging assays. HPLC-DAD analysis revealed 25 phenolic compounds with higher amounts of hydrotyrosol (109.3 mg/g), coumaroylhexoside (97.4 mg/g), kaempferol-3-(p-coumaroyldiglucoside)-7-glucoside (37.2 mg/g), quercetin-3- O -rutinoside (31.5 mg/g) and epicatechin-3- O -(4- O -methyl)-gallate (31.3 mg/g). In GC-MS analysis, oleic acid (19.67%), taurine (17.60%), ethylene dimercaptan (14.67%), isoeugenol (14.61%), patchoulane (10.36%), methyl 12-methyltetradecanoate (8.47%) and isopropyl myristate (7.02%) were highly abundant compounds. No sign of toxicity was observed in the acute dermal toxicity test. Our test sample (Mn.Cme) exhibited considerable wound healing tendency at all doses (1 g, 1.5 g, 2 g per 10 g of ointment base) with reduced epithelialization period in a dose–related manner. Absolute healing was observed after application of 2 g of Mn.Cme ointment. Further, Mn.Cme exhibited considerable anti-radical potential in all assays. It may be concluded that M. neglecta possess very potent secondary metabolites which are previously reported for wound healing potentials. The plant has considerable antioxidant and wound healing properties and thus warrant further studies to uncover the molecular mechanism its wound healing potentials. Image 1 [ABSTRACT FROM AUTHOR]