Based on literature data, related specimens, commercial samples and field investigation, botanical origin of "bolingguazi" was clarified. Boling guazi was found to be used as a Tibetan medicine in China from 8th century, it was derived from Herpetospermum pedunculosum of cucurbitaceae, and main species of bolingguazi used in most areas of China were H. pednculosura, while seeds of Momordica charantia, Thladiantha setispina and M. cohinchinensis were also available in some areas of China.
A novel molecular iodine-catalyzed protocol for the construction of thiocarbamates from readily available sodium sulfinates, isocyanides, and water has been described. The present methodology offers a facile and practical route to a variety of thiocarbamates in moderate to good yields with favorable functional group tolerance by use odorless sodium sulfinates as the sulfur source. The mechanistic studies suggest the present transformation involves a radical process.
A novel and efficient visible-light-induced C(sp2)-H/N-H cross-dehydrogenative coupling (CDC)-amination with both primary and secondary aliphatic amines at room temperature in air is developed. This photocatalytic reaction allows the direct formation of 3-aminoquinoxalin-2(1 H)-ones via CDC-amination in the absence of any external oxidant added from outside. Preliminary mechanistic studies reveal that the present reaction proceeds through a radical process.
A facile I2O5-mediated direct oxidative coupling of aromatic alkenes with thiols toward vinyl sulfones has been developed under metal-free conditions. This methodology provides a convenient and efficient approach to various (E)-vinyl sulfones from readily available starting materials with excellent regioselectivity. The present oxidative coupling reaction, not only expands the scope of functionalization of alkenes with thiols, but also makes it a practical and powerful complement to traditional methods for the synthesis of (E)-vinyl sulfones.
<bold>Background: </bold>Tong Luo Hua Shi (TLHS) is a new formulation of the traditional Tibetan medicine Wu-wei-gan-lu that has been used for the treatment of rheumatoid arthritis (RA) for hundreds of years in China. This study aimed to evaluate the efficacy and safety of TLHS in patients with RA.<bold>Methods: </bold>This was a randomized, double-blind, placebo-controlled, dose-finding study performed in patients with active RA from five medical centers. Patients received three doses (4.8, 3.6, or 2.4 g/day po) of TLHS or placebo (tid po) for 8 weeks. Blood sampling, physical examination, and assessment of the American College of Rheumatology (ACR) 20 % improvement (ACR20) criteria were performed before and every 2 weeks after starting treatment. The primary endpoint was the ACR20. The secondary endpoints included safety.<bold>Results: </bold>A total of 240 participants were screened and 236 patients were randomized (n = 59/group); 20 dropped out. After 8 weeks, ACR20 improvements in the TLHS 4.8 g and 3.6 g groups were significantly higher than in the placebo group (P < 0.01 and P < 0.05, respectively). ACR50 improvement in the TLHS 4.8 g group was significantly higher compared with the placebo group (P < 0.01). Symptoms of RA were significantly relieved in the TLHS groups. In the TLHS groups, insomnia (n = 1), gastroenteric reactions (n = 2), arrhythmia (n = 1), and minor hepatic lesion (n = 1) were reported; in the placebo group, hepatic dysfunction (n = 1) was reported (P = 0.878).<bold>Conclusions: </bold>TLHS improved the symptoms of patients with RA according to the ACR20. Moreover, TLHS was safe.<bold>Trial Registration: </bold>Chinese Clinical Trial Registry: ChiCTR-TRC-12003871 . Registered on 1 January 2012. [ABSTRACT FROM AUTHOR]
<br>Display Omitted<br>• Response surface methodology was applied to optimize supercritical fluid extraction conditions of alantolactone and isoalantolactone. • The optimized extraction conditions were pressure 20 MPa, extraction temperature 50 °C, carbon dioxide flow rate of 17 × 10−5 kg/s and extraction time of 40 min. • Freezing purification greatly improve the content of the target compounds by 30.7 wt.%.<br><b>Inula racemose</b> Hook.f. (<b>I</b>. <b>racemosa</b>) is a traditional herbal medicine with strong anti-fungal and anti-inflammation activity while alantolactone (AL) and isoalantolactone (IAL) are the major active compounds of this plant. The aim of this paper was obtaining AL and IAL from the radix of <b>I</b>. <b>racemosa</b> by supercritical fluid extraction (SFE) which was optimized by response surface methodology (RSM). Our results showed that, the optimal conditions for maximum extraction efficiency were as follows: pressure 20 MPa, extraction temperature 50 °C, carbon dioxide (CO2) flow rate of 17.0 × 10−5 kg/s and extraction time of 40 min. Subsequently, an efficient freezing method was developed for purification of AL and IAL in the crude extract obtained from SFE. After purification by freezing, the total content of the target compounds was greatly improved by 30.7%. The results demonstrate that SFE coupled with freezing would be a powerful technique for extraction and purification of AL and IAL from the radix of <b>I</b>. <b>racemosa</b>.
It was estimated that about 428 species of genus Corydalis are distributed all worldwide, with about 298, especially 10 groups and 219 species being uniquely spread in China. The genus Corydalis have been widely employed as folk medicines in China, especially as traditional Tibetan medicines, for treatment of fever, hepatitis, edema, gastritis, cholecystitis, hypertension and other diseases. The phytochemical studies revealed that isoquinoline alkaloids are its major bioactive ingredients. The extensive biological researches suggested its pharmacological activities and clinic applications against cardiovascular diseases and central nervous system, antibacterial activities, analgesic effects, anti-inflammatory, anti-oxidation and anti-injury for hepatocyte, and so on. As an effort in promoting the research of pharmacodynamic ingredients, this article presents an overview focusing on the distribution, phytochemical and pharmacological results of Corydalis species that have been applied in traditional Tibetan medicinal, hopefully to provide a reference for the new Tibetan medicine development from Corydalis plant resource.
Traditional Tibetan medicine (TTM) has been valuable for the identification of new therapeutic leads. Nevertheless, reports about the chemical constituents of TTM are meager owing to the lack of suitable purification techniques. In this study, an off-line two-dimensional reversed-phase/hydrophilic interaction liquid chromatography (2D RP/HILIC) technique guided by on-line HPLC-DPPH has been established for the isolation of pure antioxidants from the extract of Dracocephalum heterophyllum . According to the chromatographic recognition outcome of the HPLC-DPPH system, the first-dimensional (1D) separation on the Megress C18 preparative column yielded 6 antioxidative fractions (61.4% recovery) from the ethyl acetate fraction (6.1 g). In the second-dimensional (2D) separation, a HILIC XAmide preparative column was employed. In total, 8 antioxidants were isolated from D. heterophyllum with a purity of >95%, which indicated the efficiency of the developed method to prepare antioxidative compounds with high purity from plant extracts. In addition, this method was highly efficient for the preparation of structural analogues of the antioxidative polyphenols and could be applied for the purification of structural analogues from other resources. [ABSTRACT FROM AUTHOR]
Rheumatoid arthritis(RA) is a chronic autoimmune disease, belonging to the "Arthromyodynia (Bi Zheng)" category in traditional Chinese medicine. However, the ethnomedicine has a unique understanding of RA, with a long-term clinical experience accumulation and significant efficacy in the treatment of RA, and it has now become one of the important means in treatment of RA. On the basis of literature research, the understanding of RA and commonly used Tibetan medicine, Mongolian medicine, Hui medicine and other herbs and preparations were reviewed in this paper, with the aim of providing a reference for its clinical treatment of RA and research and development of innovative drugs.
Chrysosplenium nudicaule,Tibetan name " Yajima",is recorded as an effective medicine for the treatment of liver and gallbladder diseases by Tibetan Pharmacopoeia published in the past dynasties,but its traditional efficacy has not yet been investigated by means of modern pharmacological research methods. In this paper,the protective effect of extract of C. nudicaule(ECN) on liver injury in mice was observed by using the mice model of intrahepatic cholestasis(IC) induced by α-naphthyl isothiocyanate(ANIT) and the possible mechanism by which ECN work as the therapeutic agent was discussed. The results showed that the serum levels of AST,ALT,ALP,DBIL,TBIL and TBA of the model mice were notably reduced in dose-dependent manner(P<0. 01,P<0. 05). The activity of SOD and GSH-Px in the liver homogenate of mice was increased,while the content of MDA was decreased(P<0. 01,P<0. 05).Pathological examination of liver in mice showed that ECN could improve the pathological changes of liver tissue in mice. The mRNA expression level of genes related to bile acid metabolism were detected by RT-PCR and the results suggested that ECN could significantly increase the expression of genes such as BSEP,FXR and MRP2(P<0. 01,P<0. 05),meanwhile significantly reduce the expression of CYP7 A1(P<0. 01,P<0. 05). These results confirmed the protective effect of ECN on intrahepatic cholestasis-induced liver injury in mice,and indicated that the mechanism may be related to activating FXR and its target genes,reducing bile acid synthesis and increasing bile acid excretion. This study provides a modern pharmacological basis for the clinical application of Yajima in Tibetan medicine.
MCM-48 mesoporous silica was functionalized with dimethyloctadecyl[3-(trimethoxysilyl)propyl]ammonium chloride, a quaternary ammonium salt with a long hydrophobic chain, to prepare a new sorbent for the dispersive solid-phase extraction (DSPE) of seven endocrine disrupting compounds (EDCs) including 4-hexylphenol, 4-octylphenol, 4-nonylphenol, bisphenol A, estrone, 17β-estradiol and estriol in water. A series of differently functionalized MCM-48 materials were also synthesized, and they served as reference materials to study the mechanism. The developed DSPE method was combined with HPLC with fluorescence detection to evaluate the adsorption performance. The results indicated that the quaternary ammonium-functionalized MCM-48 mesoporous silica can be used as ideal sorbent for EDCs in water with recoveries of higher than 95% due to the electrostatic interactions and hydrophobic effect. Hydrogen bonding and π-π interactions in other synthesized materials could lead to about 25-30% increase in recoveries, but the results for polyhydroxy compounds were still not satisfying. The quaternary ammonium-functionalized MCM-48 mesoporous silica was successfully applied to the DSPE of EDCs in real water samples. The optimum extraction conditions were sorbent amount, 15 mg; desorption time; 5 min; elution volume, 0.8 mL; sample pH 3.0; and salt addition, 5 g/L. The limits of detection were in the range of 1.2-2.6 ng/L, while the limits of quantitation were in the range of 4.3-8.3 ng/L.
With the development of Tibetan medicine industry, the demands for Tibetan medicine were rising sharply. In addition, with the eco-environment vulnerability of Qinghai-Tibet Plateau region and the phenomenon of synonymies and homonymies in Tibetan medicine, there were a lack of resources and varieties in the clinical application of Tibetan medicine. At present, the shortage of Tibetan medicine and the inadequacy of its quality standard have become the two major problems that seriously restricted the sustainable development of Tibetan medicine industry. Therefore, it is important to develop the resources investigation and quality evaluation for Tibetan medicine, which were contribute to its resources protection and sustainable utilization. In this paper, current status of resources investigation, quality standardization, artificial breeding and germplasm resources of Tibetan medicine were presented by the integrated application of the new technologies, such as DNA barcoding and 1H-NMR, which provided a reference information for resources protection, sustainable utilization, variety identification and quality standardization of Tibetan medicine resources in Qinghai-Tibet Plateau.
The regulation of postprandial blood glucose (PBG) levels is an effective therapeutic method to treat diabetes and prevent diabetes-related complications. Resveratroloside is a monoglucosylated form of stilbene that is present in red wine, grapes, and several traditional medicinal plants. In our study, the effect of resveratroloside on reducing PBG was studied in vitro and in vivo. In comparison to the starch treatment alone, the oral administration of resveratroloside-starch complexes significantly inhibited the PBG increase in a dose-dependent pattern in normal and diabetic mice. The PBG level treated with resveratrol (30 mg/kg) was not lower than that of resveratroloside. Further analyses demonstrated that resveratroloside strongly and effectively inhibited α-glucosidase, with an 50% inhibitory concentration value of 22.9 ± 0.17 μM, and its inhibition was significantly stronger than those of acarbose and resveratrol (264 ± 3.27 and 108 ± 2.13 μM). Moreover, a competitive inhibition mechanism of resveratroloside on α-glucosidase was determined by enzyme kinetic assays and molecular docking experiments. The molecular docking of resveratroloside with α-glucosidase demostrated the competitive inhibitory effect of resveratroloside, which occupies the catalytic site and forms strong hydrogen bonds with the residues of α-glucosidase. Resveratrol was also determined to be a competitive inhibition mechanism on α-glucosidase by enzyme kinetic assays and molecular docking experiments. This study suggested that resveratroloside had the ability to regulate PBG levels and can be considered a potential agent for the treatment of diabetes mellitus.
Five phenylethanoid glycosides (PhGs), forsythoside B, verbascoside, alyssonoside, isoverbascoside, and leucosceptoside B, were isolated and purified from Lamiophlomis rotata (Benth.) Kudo by high-speed counter-current chromatography (HSCCC) combined with macroporous resin (MR) column separation. In the present study, the two-phase solvent system composed of ethyl acetate/n-butanol/water (13:3:10, v/v/v) was used for HSCCC separation. A total of 27 mg of forsythoside B, 41 mg of verbascoside, 29 mg of alyssonoside, 23 mg of isoverbascoside, and 13 mg of leucosceptoside B with purities of 97.7, 99.2, 99.5, 99.3, and 97.3%, respectively, were obtained in a one-step separation within 4 h from 150 mg of crude extract. The recoveries of the five PhGs after MR-HSCCC separation were 74.5, 76.5, 72.5, 76.4, and 77.0%, respectively. The chemical structures of all five compounds were identified by (1) H and (13) C NMR spectroscopy.
Five phenylethanoid glycosides (PhGs), forsythoside B, verbascoside, alyssonoside, isoverbascoside, and leucosceptoside B, were isolated and purified from Lamiophlomis rotata (Benth.) Kudo by high-speed counter-current chromatography (HSCCC) combined with macroporous resin (MR) column separation. In the present study, the two-phase solvent system composed of ethyl acetate/n-butanol/water (13:3:10, v/v/v) was used for HSCCC separation. A total of 27 mg of forsythoside B, 41 mg of verbascoside, 29 mg of alyssonoside, 23 mg of isoverbascoside, and 13 mg of leucosceptoside B with purities of 97.7, 99.2, 99.5, 99.3, and 97.3%, respectively, were obtained in a one-step separation within 4 h from 150 mg of crude extract. The recoveries of the five PhGs after MR-HSCCC separation were 74.5, 76.5, 72.5, 76.4, and 77.0%, respectively. The chemical structures of all five compounds were identified by (1) H and (13) C NMR spectroscopy.
Four iridoid glucosides, shanzhiside methyl ester, phloyoside II, chlorotuberside, and penstemonoside, were isolated and purified from an herbal medicinal plant for the first time by high-speed counter-current chromatography (HSCCC) using a two-phase solvent system composed of ethyl acetate-n-butanol-water (5:14:12, v/v/v). A total of 37mg of shanzhiside methyl ester, 29mg of phloyoside II, 27mg of chlorotuberside, and 21mg of penstemonoside with the purity of 99.2%, 98.5%, 97.3%, and 99.3%, respectively, were obtained in one-step separation within 4h from 150mg of crude extract. To the best of our knowledge, this is the first report of separation and purification of iridoid glucosides from natural sources by HSCCC. The chemical structures of all the four compounds were identified by ESI-MS, (1)H NMR, and (13)C NMR.
A new stable isotope labeling (SIL) reagent pair, 10-methyl-acridone-2-sulfonohydrazide (MASH) and its deuterated counterpart d3-MASH was synthesized and successfully applied to the analysis of perfluorinated carboxylic acids (PFCAs) in serum samples. The limits of detection (LODs) were in the range of 0.07-0.42μg/L, and the limits of quantitation (LOQs) were in the range of 0.25-1.38μg/L. Besides ionization enhancing effect, MASH also showed excellent fluorescence property. Therefore, the mass spectrometer operation cost was greatly lowered by carrying out parameter optimization experiments on HPLC which is easier to operate and maintain. The SIL strategy was confirmed to be effective in reducing matrix effect. The developed multiple-reaction monitoring (MRM) condition of PFCAs was also suitable for other carboxylic acid due to the introduction of MASH which is more prone to fragmentation than the analytes. With the MRM conditions obtained from PFCAs, fatty acids were also found in serum samples. This feature made the proposed method show powerful potential in the identification of acidic compounds in complex samples in the absence of corresponding standard.
The 1H-NMR fingerprints of three different species tibetan medicine sea buckthorn were established by 1H-HMR metabolomics to find out different motablism which could provide a new method for the quality evaluation of sea buckthorn. The obtained free induction decay (FID) signal will be imported into MestReNova software and into divide segments. The data will be normalized and processed by principal component analysis and.partial least squares discriminant analysis to perform pattern recognition. The results showed that 25 metabolites belonging to different chemical types were detected from sea buckthorn,including flavonoids, triterpenoids, amino acids, carbohydrates, fatty acids, etc. PCA and PLS-DA analysis showed three different varietiest of sea buckthorn that can be clearly separated by the content of L-quebrachitol, malic acid and some unidentified sugars, which can be used as the differences metabolites of three species of sea buckthorn. 1H-NMR-based metabonomies method had a holistic characteristic with sample preparation and handling. The results of this study can offer an important reference for the species identification and quality control of sea buckthorn.
The effective, energy-saving and green subcritical fluid extraction (SFE) technology was applied to obtain the oil from <i>Lycium ruthenicum</i> seeds (LRSO). The optimal conditions of extraction parameters were found using response surface methodology with Box-Behnken experimental design. The maximum extraction yield of 21.20% was achieved at raw material particle size of 0.60 mm, extraction pressure of 0.63 MPa, temperature of 50 °C and time of 48 min. Other traditional extraction technologies were comparatively used. The physicochemical property of LRSO was analysed and the chemical compositions indicated that they were rich in unsaturated fatty acid, β-carotene, tocopherols and total phenolics. Furthermore, the antioxidant activity of LRSO was evaluated by scavenging activity of three kinds of radicals (DPPH·, ·OH and O₂⁻·) and lipid peroxidation <i>in vitro</i>. And its results showed the oil had the potential to be a novel antioxidant agent for using in the field of food, pharmaceuticals and cosmetics.<br>Lycium ruthenicum seeds oil (LRSO) was obtained by subcritical fluid extraction (SFE), and the process of SFE was optimized using response surface methodology. LRSO was evaluated by determination of physicochemical property, lipophilic compositions and antioxidant activity. The study revealed the possibility of LRSO as a potential source of valuable product for commercial ventures (food, pharmaceuticals or cosmetics).
Tai Chi Chuan (TCC) practice is currently intentionally applied in clinical populations, especially those with cardiovascular diseases because of its potential benefits on the autonomic nervous system. The long-term effect of TCC practice on heart rate variability (HRV) remains largely unknown. In this study, we recruited 23 TCC practitioners whose experience averaged approximately 21 years and 19 controls matched by age, sex and education to examine the effect of TCC practice on the autonomic nervous system during a resting state and during an abdominal breathing state. HRV was measured by traditional electrocardiogram (ECG) recording. The results showed that the low frequency, total power frequency, and normalized low frequency components and the low-frequency/high-frequency ratio were significantly higher, whereas the normalized high frequency was significantly lower in the TCC practitioners relative to controls during the abdominal breathing state. However, we did not detect any significant difference in the HRV measures during the resting state between the two groups. Additionally, TCC experience did not correlate with HRV components either in the abdominal state or the resting state in the TCC group. Considering all of these findings, we suggest that TCC improves vagal activity and the balance between sympathetic and parasympathetic activity during the relaxation state. This study also provides direct physiological evidence for the role of TCC practice in relaxation.
An orthogonally (80.3%) preparative two-dimensional hydrophilic interaction chromatography/reversed-phase liquid chromatography method has been established for the isolation and purification of flavonoids from Saxifraga tangutica. Initially, flavonoids were enriched by means of a middle-pressure chromatographic tower (containing middle chromatogram isolated gel). In the first dimension, a XION preparative column was used to separate the flavonoid fractions under the guidance of characteristic ultraviolet absorption spectra of flavonoids and nine flavonoid fractions were obtained. Then, the coeluted flavonoid fractions were selected for further purification via reversed-phase liquid chromatography with the parent ion peak of quercetin (303), kaempferol (287), or isorhamnetin (317). Several flavonoids could be separated from each hydrophilic interaction chromatography fraction; furthermore, flavonoids with poor resolution in one-dimensional liquid chromatography were isolated in two-dimensional liquid chromatography due to the orthogonality. In addition, this technique was valuable for trace flavonoids, which were concentrated in the first stage and separated in the second stage. In total, 18 flavonoids with either quercetin, kaempferol, or isorhamnetin parent nuclei were targetedly obtained, and 15 flavonoids were obtained for the first time from S. tangutica. These results established that the off-line two-dimensional hydrophilic interaction chromatography/reversed-phase liquid chromatography technique was efficient for the isolation of flavonoids from Saxifraga tangutica.
An orthogonally (80.3%) preparative two-dimensional hydrophilic interaction chromatography/reversed-phase liquid chromatography method has been established for the isolation and purification of flavonoids from Saxifraga tangutica. Initially, flavonoids were enriched by means of a middle-pressure chromatographic tower (containing middle chromatogram isolated gel). In the first dimension, a XION preparative column was used to separate the flavonoid fractions under the guidance of characteristic ultraviolet absorption spectra of flavonoids and nine flavonoid fractions were obtained. Then, the coeluted flavonoid fractions were selected for further purification via reversed-phase liquid chromatography with the parent ion peak of quercetin (303), kaempferol (287), or isorhamnetin (317). Several flavonoids could be separated from each hydrophilic interaction chromatography fraction; furthermore, flavonoids with poor resolution in one-dimensional liquid chromatography were isolated in two-dimensional liquid chromatography due to the orthogonality. In addition, this technique was valuable for trace flavonoids, which were concentrated in the first stage and separated in the second stage. In total, 18 flavonoids with either quercetin, kaempferol, or isorhamnetin parent nuclei were targetedly obtained, and 15 flavonoids were obtained for the first time from S. tangutica. These results established that the off-line two-dimensional hydrophilic interaction chromatography/reversed-phase liquid chromatography technique was efficient for the isolation of flavonoids from Saxifraga tangutica.
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