Unveiling the Pharmacological Mechanisms of Davidiin's Anti-Diabetic Efficacy in Streptozotocin-Treated Rats: A Comprehensive Analysis of Serum Metabolome.

Background: Polygonum capitatum Buch.-Ham. ex D. Don (P. capitatum), a traditional herb used in Miao medicine, is renowned for its heart-clearing properties. Davidiin, the primary bioactive component (approximately 1%), has been used to treat various conditions, including diabetes. Given its wide range of effects and the diverse biomolecular pathways involved in diabetes, there is a crucial need to study how davidiin interacts with these pathways to better understand its anti-diabetic properties. Materials and Methods: Diabetic rats were induced using a high-fat diet and streptozotocin (STZ) administered intraperitoneally at 35 mg/kg. Out of these, 24 rats with blood glucose levels ≥ 11.1 mmol/L and fasting blood glucose levels ≥ 7.0 mmol/L were selected for three experimental groups. These groups were then treated with either metformin (gavage, 140 mg/kg) or davidiin (gavage, 90 mg/kg) for four weeks. After the treatment period, we measured body weight, blood glucose levels, and conducted untargeted metabolic profiling using UPLC-QTOF-MS. Results: Davidiin has been shown to effectively treat diabetes by reducing blood glucose levels from 30.2 ± 2.6 mmol/L to 25.1 ± 2.4 mmol/L (P < 0.05). This effect appears stronger than that of metformin, which lowered glucose levels to 26.5 ± 2.6 mmol/L. The primary outcomes of serum metabolomics are significant changes in lipid and lipid-like molecular profiles. Firstly, davidiin may affect phosphatide metabolism by increasing levels of phosphatidylinositol and sphingosine-1-phosphate. Secondly, davidiin could influence cholesterol metabolism by reducing levels of glycocholic acid and glycochenodeoxycholic acid. Lastly, davidiin might impact steroid hormone metabolism by increasing hepoxilin B3 levels and decreasing prostaglandins. Conclusion: Our study demonstrates that davidiin modulates various lipid-related metabolic pathways to exert its anti-diabetic effects. These findings offer the first detailed metabolic profile of davidiin's action mechanism, contributing valuable insights to the field of Traditional Chinese Medicine in the context of diabetes treatment.

Chaihu-Guizhi-Ganjiang Decoction is more efficacious in treating irritable bowel syndrome than Dicetel according to metabolomics analysis.

BACKGROUND: Chaihu-Guizhi-Ganjiang Decoction (CGGD) is a traditional Chinese medicine (TCM) prescription used to treat viral influenza. There is evidence that CGGD can be used to treat irritable bowel syndrome (IBS) but the potential mechanism of action and metabolites produced upon CGGD treatment remains elusive. METHODS: Patients with IBS were treated with pinaverium bromide (Dicetel™) and then CGGD after a washout period of 1 week. Both treatments lasted for 30 days. The efficacy and changes of metabolites in plasma after the two treatments were compared. Plasma samples were acquired before and after each treatment, and untargeted metabolics analysis was performed. RESULTS: Efficacy was measured according to the Rome IV criteria and TCM theory. Our results indicated that CGGD showed significantly better efficacy than Dicetel in the treatment of IBS utilizing each criterion. CGGD exerted greater effects on plasma metabolism than Dicetel. Dicetel treatment led to increased tryptophan metabolism (increased levels of 5-Hydroxyindoleacetaldehyde) and increased protein metabolism (increased levels of L-arginine). CGGD treatment significantly (p < 0.05) increased carnitine metabolism, with elevated levels of L-carnitine and acylcarnitine in plasma. Such changes in these metabolites could exert effects against IBS by improving gastrointestinal motility and suppressing pain, depression, and inflammation. CONCLUSIONS: CGGD appeared to be more efficacious than Dicetel for treating patients with IBS. The findings provide a sound support for the underlying biomolecular mechanism of CGGD in the prevention and treatment of IBS.

Corrigendum: Integrated chemical interpretation and network pharmacology analysis to reveal the anti-liver fibrosis effect of Penthorum chinense.

[This corrects the article DOI: 10.3389/fphar.2022.788388.].

Integrated Chemical Interpretation and Network Pharmacology Analysis to Reveal the Anti-Liver Fibrosis Effect of Penthorum chinense.

Liver fibrosis is a disease with complex pathological mechanisms. Penthorum chinense Pursh (P. chinense) is a traditional Chinese medicine (TCM) for liver injury treatment. However, the pharmacological mechanisms of P. chinense on liver fibrosis have not been investigated and clarified clearly. This study was designed to investigate the chemicals in P. chinense and explore its effect on liver fibrosis. First, we developed a highly efficient method, called DDA-assisted DIA, which can both broaden mass spectrometry (MS) coverage and MS2 quality. In DDA-assisted DIA, data-dependent acquisition (DDA) and data-independent acquisition (DIA) were merged to construct a molecular network, in which 1,094 mass features were retained in Penthorum chinense Pursh (P. chinense). Out of these, 169 compounds were identified based on both MS1 and MS2 analysis. After that, based on a network pharmacology study, 94 bioactive compounds and 440 targets of P. chinense associated with liver fibrosis were obtained, forming a tight compound-target network. Meanwhile, the network pharmacology experimental results showed that multiple pathways interacted with the HIF-1 pathway, which was first identified involved in P. chinense. It could be observed that some proteins, such as TNF-α, Timp1, and HO-1, were involved in the HIF-1 pathway. Furthermore, the pharmacological effects of P. chinense on these proteins were verified by CCl4-induced rat liver fibrosis, and P. chinense was found to improve liver functions through regulating TNF-α, Timp1, and HO-1 expressions. In summary, DDA-assisted DIA could provide more detailed compound information, which will help us to annotate the ingredients of TCM, and combination with computerized network pharmacology provided a theoretical basis for revealing the mechanism of P. chinense.

Analgesic and Anti-Arthritic Activities of Polysaccharides in Chaenomeles speciosa.

Chaenomeles speciosa (Sweet) Nakai has been long used as a folk medicine for rheumatic diseases treatment. This study aimed to investigate the effects and underlying mechanism of polysaccharides in Chaenomeles speciosa (CSP) on the pro-inflammatory cytokines and MAPK pathway in complete Freund's adjuvant (CFA)-induced arthritis and LPS-induced NR8383 cells. We used acetic acid (HAc)-induced writhing and CFA induced paw edema to determine the analgesic activity and anti-inflammatory activity, respectively. CFA rats were administered CSP (12.5, 25.0, and 50.0 mg/kg) daily for 3 weeks via oral gavage. The analgesic test was done using three different doses of the extract (50, 100, and 200 mg/kg). The anti-arthritic evaluation involved testing for paw swelling, swelling inhibition, and histological analysis in CFA rats. Finally, ELISA, western blot, qRT-PCR were done to determine the effect of CSP on the activation of MAPK pathway, production of pro-inflammatory cytokines in lipopolysaccharide (LPS)-stimulated NR838 macrophage cells. In pain models, oral uptake of CSP greatly reduced pain perception. Furthermore, in CFA rats, CSP substantially decreased paw swelling as well as synovial tissue proliferation and inflammatory cell infiltration. In addition, CSP was shown to inhibit pro-inflammatory cytokines (TNF-α, IL-1ß, and COX-2) as well as JNK and ERK1/2 phosphorylation in LPS-stimulated NR8383 cells. Thus, pro-inflammatory cytokine secretion and MAPK signaling downregulation promoted the analgesic and anti-arthritic effects of CSP.

Computational Workflow to Study the Diversity of Secondary Metabolites in Fourteen Different Isatis Species.

The screening of real features among thousands of ions remains a great challenge in the study of metabolomics. In this research, a workflow designed based on the MetaboFR tool and "feature-rating" rule was developed to screen the real features in large-scale data analyses. Seventy-four reference standards were used to test the feasibility, with 83.21% of real features being obtained after MetaboFR processing. Moreover, the full workflow was applied for systematic characterization of 14 species of the genus Isatis, with the result that 87.72% of real features were retained and 69.19% of the in-source fragments were removed. To gain insights into metabolite diversity within this plant family, 1697 real features were tentatively identified, including lipids, phenylpropanoids, organic acids, indole derivatives, etc. Indole derivatives were demonstrated to be the best chemical markers with which to differentiate different species. The rare existence of indole derivatives in Isatis cappadocica (cap) and Isatis cappadocica subsp. Steveniana (capS) indicates that the biosynthesis of indole derivatives could play a key role in driving the chemical diversity and evolution of genus Isatis. Our workflow provides the foundations for the exploration of real features in metabolomics, and has the potential to reveal the chemical composition and marker metabolites of secondary metabolites in plant fields.

Biosynthesis-based spatial metabolome of Salvia miltiorrhiza Bunge by combining metabolomics approaches with mass spectrometry-imaging.

Defining the spatial distributions of metabolites and their structures are the two key aspects for interpreting the complexities of biosynthesis pathways in plants. As a means of obtaining information on the spatial distribution of metabolites, a strategy is needed that has high sensitivity and allows visualization. Toward this goal, we carried an untargeted metabolomics to obtain detailed metabolic information on different plant parts of Salvia miltiorrhiza, the roots of which are widely used in traditional Chinese medicine. Systematic optimization of desorption electrospray ionization mass spectrometry imaging (DESI-MSI) including parameter selection and sample preparation were carried out to improve the sensitivity of the method for plant samples. Guided by the metabolomics data, the spatial distributions of diverse metabolites, including phenolic acids, flavonoids, tanshinones, carbohydrates, and lipids, were characterized and visualized for both the underground and aerial parts. To integrate the information pertaining to the spatial distribution of metabolites, the flavonoids and phenolic acids (phenylpropanoid metabolic pathway) were chosen as examples for in-depth study the biosynthesis pathways in S. miltiorrhiza. The complementary data obtained from the metabolomics study and mass spectrometry imaging enabled the identification of key reactions involved in flavonoid biosynthesis in flowers, which lead the changes in metabolite distribution. The analysis also identified the core precursor for phenolic acid biosynthesis in Salvia species. Therefore, the powerful combination of metabolomics and mass spectrometry imaging provides a basis for obtaining detailed information on spatial metabolome and constitutes a platform for deep understanding the biosynthesis of bioactive metabolites in plants.

Bio-Guided Isolation of Two New Hypoglycemic Triterpenoid Saponins from Polygonum capitatum.

PURPOSE: Diabetes is a common disease caused by a combination of genetic and environmental factors, which was the top three diseases threatening human health. Therefore, it is necessary to seek more efficient hypoglycemic drugs. The main objective of this study was to investigate the potential hypoglycemic effects of compounds from Polygonum capitatum. MATERIALS AND METHODS: Our experiments were divided into three steps: (1) α-amylase test and oral starch tolerance test (OSTT) for screening the biological extract part of P. capitatum; (2) chemical isolation and identification using various separation techniques, and spectrum methods; and (3) evaluation of α-amylase inhibitory activity of isolates and in silico analysis for mechanism investigation. RESULTS: The n-butanol fractioned part of P. capitatum was confirmed to be the biological part according to α-amylase test. Then, two new triterpenoid saponins were isolated from the n-butanol part, which were also the first isolated triterpenoid saponins from P. capitatum. The activities of compounds 1 and 2 against α-amylase were 51.9±2.8% and 38.1±2.2%, respectively, which was consistent with the molecular docking analysis. In which, 1 and 2 showed the binding affinity energy for α-amylase was -9.4 kcal/mol and -7.8 kcal/mol, respectively. CONCLUSION: Two new triterpenoid saponins were firstly isolated from P. capitatum, and displays potency as a hypoglycemic agent through blocking α-amylase.

The LC-MS/MS-Based Measurement of Isopimaric Acid in Rat Plasma and Application of Pharmacokinetics.

Isopimaric acid (IPA) exhibits a diverse array of pharmacological activities, having been shown to function as an antihypertensive, antitumor, antibacterial, and hypocholesterolemic agent. However, few studies of the pharmacokinetics of IPA have been performed to date, and such analyses are essential to explore the in vivo mechanisms governing the biological activity of this compound. As such, we herein designed a selective LC-MS approach capable of quantifying serum IPA levels in model rats using an Agilent HC-C18 column (250 mm × 4.6 mm, 5 µm) via isocratic elution with a mobile phase composed of methanol 0.5% formic acid (91 : 9, v/v) at a 1 mL/min flow rate. Ion monitoring at m/z 301.2 [M-H]- was used to quantify IPA levels in plasma samples from these rats, while internal standard (IS) levels were assessed at m/z 455.3 [M-H]-. After validation, this approach was employed to conduct a pharmacokinetic analysis of rats administered IPA via the oral (p.o. 50, 100, or 200 mg/kg) and intravenous (i.v. 5 mg/kg) routes. Analyses of noncompartmental pharmacokinetic parameters revealed that IPA underwent secondary absorption following oral administration to these animals, with the two tested oral doses (50 and 100 mg/kg) being associated with respective absolute bioavailability values of 11.9% and 17.5%. In summary, this study may provide a foundation for future efforts to explore the mechanistic basis for the pharmacological activity of IPA, offering insights to guide its subsequent clinical utilization.

[Historical evolution of Salviae Miltiorrhizae Radix et Rhizoma processing methods].

China has a long history of Salviae Miltiorrhizae Radix et Rhizoma processing with multiple methods available. The pre-sent study collated and summarized the Salviae Miltiorrhizae Radix et Rhizoma processing methods recorded in 23 related herbal medicine books, all editions of Chinese Pharmacopoeia, the 1988 edition of National Regulations for Processing of Chinese Medicine, and 20 current local processing specifications and standards. The results demonstrated various processing methods of Salviae Miltiorrhizae Radix et Rhizoma, such as removing residual part of stem, plantlet, or soil, smashing, filing, cutting, decocting, washing with wine, soaking in wine, and stir-frying with wine or blood from pig heart, while raw and wine-processed products are mainly used in modern times. Due to the lack of unified standards, the phenomena of multiple methods adopted in one place and different methods in different places have led to uneven quality of Salviae Miltiorrhizae Radix et Rhizoma pieces, even affecting the safety and effectiveness of its clinical medication. This study is expected to provide a reference for the development of Salviae Miltiorrhizae Radix et Rhizoma processing and its rational medication.

Selection of appropriate post-harvest processing methods based on the metabolomics analysis of Salvia miltiorrhiza Bunge.

Post-harvest processing is a leading cause of metabolic changes and quality loss in food products. An untargeted metabolomics approach based on UHPLC-QTOF-MS was conducted to explain metabolic changes during post-harvest processing of Salvia miltiorrhiza. A rapid identification method was established for comprehensive characterization of 56 phenolic acids and 45 tanshinones. Enzymatic browning was found to be the primary factor impacting the metabolic profile. A decreasing in free phenolic acids along with increasing in bound polyphenols was observed correlated with the deepening of browning degree. The various substructures of bound polyphenols were explored to interpret the composition of browning-associated products. It has also been found that the steaming process and control of the moisture content during slicing can effectively reduce the influence of enzymatic browning. This metabolomics study will contribute to select the optimal post-harvest processing methods for S. miltiorrhiza and provide information for post-harvest processing of similar products.

Two neolignans from Penthorum Chinense and their antiproliferative activities.

Chemical investigation of Penthorum chinense resulted in the isolation of two neolignans (1 and 2) together with two known compounds (3 and 4). The structures of compounds 1 and 2 were determined by interpretation of spectroscopic data, and absolute configurations were made based on electronic circular dichroism (ECD). All compounds were evaluated for their antiproliferative activity on hepatic stellate T6 cells (HSC-T6 cells), and 1 and 2 showed moderate activity with IC50 values of 15.3 and 10.1 µM, respectively.

Constituents from the Roots of Actinidia chinensis and Their Cytochrome P450 Enzyme Inhibitory Activities.

A newly discovered triterpenoid, (2α,3ß)-2,3,23-trihydroxyurs-13(18)-en-28-oic acid (1), along with twelve known compounds (2 - 13), were isolated from the roots of Actinidia chinensis Planch (Actinidiaceae). Their chemical structures were determined by 1D- and 2D-NMR spectra and mass spectrometry (MS). The crude extracts and six main constituents (8 - 13) were tested for cytochrome P450 (CYPs) enzyme inhibitory activity. The results showed that, except for compound 8, compounds 9 - 13 had different inhibitory effects on the cytochrome P450 (CYPs) enzyme, and compound 9 significantly inhibited the catalytic activities of CYP3A4 to < 10% of its control activities.

Anti-inflammatory constituents from the root of Litsea cubeba in LPS-induced RAW 264.7 macrophages.

Context Litsea cubeba (Lour.) Pers. (Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) for the treatment of rheumatic diseases. Previous studies from our laboratory indicated that L. cubeba extract showed anti-arthritic activity in rats. Objective To study L. cubeba chemically and biologically and to find the potential constituents responsible for its anti-arthritic effect. Materials and methods The compounds were isolated from the root of L. cubeba by column chromatography which eluted with PE:EtOAc gradient system, and the structures were elucidated by detailed spectroscopic data analysis; the anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide (LPS)-induced RAW 264.7 cells and the TNF-α and NO level were measured by ELISA (commercial kit); The iNOS and COX-2 mRNA expression were measured by RT-PCR and the phosphorylation of IκBα, IKKß, P38 and Akt were determined by western blots. Results A novel 9-fluorenone, 1-ethoxy-3,7-dihydroxy-4,6-dimethoxy-9-fluorenone (1), together with 4 known compounds, namely pinoresinol (2), syringaresinol (3), 9,9'-O-di-(E)-feruloyl-meso-5,5'-dimethoxysecoisolariciresinol (4) and lyoniresinol (5) were isolated from the root of L. cubeba for the first time. The IC50 for NO inhibition on compounds 1 and 4 were 56.1 ± 1.2 and 32.8 ± 2.3 µM, respectively. The IC50 for TNF-α inhibition were 28.2 ± 0.9 and 15.0 ± 1.0 µM, respectively. Both 1 and 4 suppress mRNA expression of iNOS, COX-2 and protein phosphorylation of IκBα, IKKß in LPS-induced RAW 264.7 cells. Discussion and conclusion Compounds 1 and 4 isolated from L. cubeba exhibited potent anti-inflammatory activity through the NF-κB signal pathway.

Anti-inflammatory effects of the extract of Gnaphalium affine D. Don in vivo and in vitro.

ETHNOPHARMACOLOGICAL RELEVANCE: Gnaphalium affine D. Don (GA) has been traditionally used as a medicinal herb in China for the treatment of many ailments including rheumatoid arthritis. However, the anti-arthritic mechanism of GA has still not been demonstrated. This study aims to reveal the anti-inflammatory activity and anti-arthritic mechanism of ethanol extract of G. affine D. Don. MATERIALS AND METHODS: Anti-inflammatory potential of GA was analyzed in vivo in carrageenan induced mice paw edema (acute study). Also, in vivo study was applied in collagen-induced arthritis (CIA) rats. In vitro experiments for analyzing the anti-inflammatory potential of GA were performed on rat alveolar macrophages cell line (NR8383). Analysis of nitric oxide release in NR8383 cells was done by Griess reaction. RT-PCR and western blotting experiment was performed to analyze the expression of phosphorylated p65 and IκBα/ß-actin in NF-κB pathway. The production of TNF-α, IL-1ß, and COX-2 in NR8383 cells were measured by enzyme-linked immunosorbent assay. The chemical profile of GA was analyzed by HPLC-VWD. RESULTS: GA significantly reduced the paw volume in carrageenan induced rat paw edema rat at different doses (300 and 600 mg/kg), compared with the standard indomethacin treatment. In CIA, GA can obviously ameliorate the inflammatory symptom, including cytokine, histological symptom and paw swelling. In the vitro study, GA was able to reduce the nitric oxide (NO) levels in NR8383 cells that had been stimulated with lipopolysaccharide (LPS). The level of TNF-α, IL-1ß, and COX-2 was also decreased with GA treatment in NR8383 cells that had been stimulated with lipopolysaccharide (LPS). Interestingly, GA was found to decrease the level of phosphorylated p65 and IκBα in NR8383 cells. Fifteen compounds were identified by HPLC-VWD with the reference substances and verified by LC-MS. CONCLUSIONS: The results of the experiment scientifically validated its traditional use in inflammatory conditions.

Carthami flos: a review of its ethnopharmacology, pharmacology and clinical applications

ABSTRACTCarthami flos, the dried floret of Carthamus tinctorius L., Asteraceae (safflower), has been widely used in traditional Chinese medicine to treat a broad range of ailments, such as coronary heart disease, angina pectoris, gynecologic disease, stroke, and hypertension. However, although several studies on Carthami flos have been done consecutively, the results are usually scattered across various documents. This review aims to provide up-to-date information on the traditional uses, pharmacology, clinical applications, and toxicology of Carthami flos in China and thereby to provide a basis for further investigation of its use to treat dissimilar diseases. Various ethnomedical uses of Carthami flos have been documented in many ancient Chinese books. Crude extracts and isolated compounds from Carthami flos show a broad range of pharmacological properties, such as protective effects on brain tissue, on osteoblasts, and in myocardial ischemia, as well as anti-inflammatory, antithrombotic, antitumor, and antidiabetic activities. To date, safflower and safflor yellow injections have been used to treat coronary heart disease, chronic pulmonary heart disease, cerebrovascular diseases, orthopedic diseases, and diabetes mellitus. Regarding the toxicology of Carthami flos, among the side effects that have been observed are allergic reaction, spermatogenetic failure, fatty liver, and nephrotoxicity.

Simultaneous determination of multiple platycosides with a single reference standard in Platycodi Radix by high-performance liquid chromatography coupled with evaporative light scattering detection.

A traditional external standard method using HPLC coupled with evaporative light scattering detection has been developed for fast and accurate determination of seven platycosides in Platycodi Radix. However, inevitable difficulties in reference standards preparation process, which are quite costly and time consuming, have made its application limited. To avoid this inconvenience, a simultaneous determination of multiple components with a single reference standard strategy, which could be realized by calibrating the standard curve with internal standard and response factors, was introduced to the HPLC coupled with evaporative light scattering detection method. This is the first time that an incorporation of these two methods has been realized. Among seven ingredients, platycodin D was selected as the internal standard for its relatively easy preparation and low cost. Moreover, according to the investigation on concentration-dependent effects over response factors and robustness test, platycoside E, deapioplatycodin D, platycodin D, and polygalacin D2 were chosen to be the indicators for this novel method. The present method has not shown statistically significant differences with a traditional external standard method as verified sample analysis by the F-test (p = 95%, n = 6).

Prenylated phenylpropanoid compounds from the stem bark of Illicium burmanicum.

Ten new prenylated phenylpropanoid compounds, burmanicumols A-G (1-6) and illifrognones D-G (7-10), and seven known prenylated phenylpropanoid compounds, were isolated from the stem bark of Illicium burmanicum. The structures of the new compounds were determined on the basis of 1D and 2D NMR, HRESIMS, and CD experiments. Compounds 3, 8, 10, and 14 were moderately potent inhibitors of the NF-κB pathway, with IC50 values ranging from 10.31 to 35.16µg/mL tripterygium glycosides and pavlin were used as the positive controls.

Evaluation of hypoglycemic effects of polyphenols and extracts from Penthorum chinense.

ETHNOPHARMACOLOGICAL RELEVANCE: Penthorum chinense Pursh has a long history of use as a health food and folk medicine to alleviate "heat"-associated disorders, promote circulation and diuresis, and to treat liver problems, and to protect the spleen. In this study we provide experimental evidence for the clinical use of Penthorum chinense in the treatment of diabetes mellitus. The aim of the study was to investigate the hypoglycemic effects of extracts and active constituents from Penthorum chinense. MATERIALS AND METHODS: High fat diet and STZ (35mg/kg) induced diabetic rats were administered with Penthorum chinense extract at graded oral doses (150 and 300mg/kg/day, ig.) for 2 weeks. A range of parameters, including blood glucose and lipid, serum insulin, glucose tolerance, were tested to evaluate its anti-hyperglycemic effects. Moreover, oral starch tolerance test (OSTT) was performed to test the level of postprandial glucose after administrating Penthorum chinense extract. In vitro study, the Penthorum chinense extracts and purified Penthorum chinense polyphenols were tested for α-amylase inhibitory activity. The polyphenols were determined by UPLC-Q-TOF mass spectrometry and NMR. RESULTS: The Penthorum chinense extract possessed anti-hyperglycemic activities as shown by the decreased serum levels of glycosylated hemoglobulin A1C (HbA1c), triglyceride(TG), total cholesterol (TC), and low density lipoprotein-cholesterol (LDL-C), as well as increased serum levels of high density lipoprotein-cholesterol (HDL-C) and insulin. Penthorum chinense extract also improved the oral glucose tolerance test (OGTT) to a certain degree. Moreover, the OSTT study showed that in diabetic rats, the extract (600mg/kg) caused a significant hypoglycemic effect with a blood glucose reduction of 42% at 60min. To identify the active constituents, three polyphenols, pinocembrin-7-O-[4″,6″-hexahydroxydiphenoyl]-ß-d-glucose (1), pinocembrin-7-O-[3″-O-galloyl-4″, 6″-hexahydroxydiphenoyl]-ß- d-glucose (2), and thonningianin A (3) were isolated from Penthorum chinense. Compounds 1-3 moderately inhibited α-amylase activity, with IC50 values of 0.14, 0.03, and 0.08µmol/ml, respectively. CONCLUSIONS: The folk medicinal plant, Penthorum chinense produced a moderated anti-hyperglycemic effect on STZ-induced diabetic rats and starch induced postprandial hyperglycemic mice.

Constituent analysis and quality control of Lamiophlomis rotata by LC-TOF/MS and HPLC-UV.

In the present study, chemical profile analysis for Lamiophlomis rotata, a classic Tibetan folk medicine, was illustrated by an ultra-high performance liquid chromatography quadrupole time-of-flight mass spectrometry (LC-TOF/MS) method, which provided evidence for the certain identification of the main constituents, including iridoids, flavonoids and phenylethanoid glycosides. Among these compounds, nine of them were regarded as marker compounds for the quantitative evaluation of L. rotata, using a simple and reliable method by HPLC with ultraviolet, in combination of chromatographic fingerprint analysis. Separation was achieved on a Waters SunFire C18 analytical column with linear gradient elution of acetonitrile and 0.1% formic acid aqueous solution. The validated method was successfully applied to evaluate twelve batches of L. rotata. Assay results showed that nine compounds did not vary significantly from the aerial parts and the whole plant for each batch, and was consistent with the fingerprint analysis, which confirmed the medicine parts alteration in Chinese Pharmacopoeia from the perspective of chemical components.