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Ginseng is a very commonly used natural product in the world, and its two main species are Asian ginseng and American ginseng. Ginseng is an adaptogenic botanical that reportedly protects the body against stress, stabilizes physiological processes, and restores homeostasis. Previously, different animal models and contemporary research methodologies have been used to reveal ginseng's biomedical activities in different body systems and the linked mechanisms of actions. However, human clinical observation data on ginseng effects have attracted more attention from the general public and medical community. In this paper, after an introduction of the phytochemistry of ginseng species, we review positive ginseng clinical studies, mainly conducted in developed countries, performed over the past 20 years. The reported effects of ginseng are presented in several sections, and conditions impacted by ginseng include diabetes; cardiovascular disorders; cognition, memory, and mood; the common cold and flu; cancer fatigue and well-being; quality of life and social functioning, etc. Administration of ginseng demonstrated a good safety record in humans. Although encouraging beneficial effects obtained from clinical data, using the study treatment regimen, the reported ginseng effects in general only ranged from mild to moderate. Nonetheless, these beneficial effects of ginseng could be a valuable add-on therapy for patients receiving standard drug treatments. Additionally, as a dietary supplement, ginseng possesses an important role in maintaining and promoting human health. We believe that the quality of future ginseng trials should be improved, particularly by providing detailed herbal phytochemistry and quality control information. With solid effectiveness data obtained from a well-designed, carefully executed ginseng clinical trial, this meritoriously herbal medicine will be widely used by consumers and patients.

Ulcerative colitis (UC) has become a global epidemic, and the lack of an effective cure highlights the necessity and urgency to explore novel therapies. Sijunzi Decoction (SJZD), a classical Chinese herbal formula, has been comprehensively applied and clinically proven effective in treating UC; however, the pharmacological mechanism behind its therapeutic benefits is largely obscure. Here, we find that SJZD can restore microbiota homeostasis and intestinal barrier integrity in DSS-induced colitis. SJZD significantly alleviated the colonic tissue damage and improved the goblet cell count, MUC2 secretion, and tight junction protein expressions, which indicated enhanced intestinal barrier integrity. SJZD remarkedly suppressed the abundance of phylum Proteobacteria and genus Escherichia - Shigella , which are typical features of microbial dysbiosis. Escherichia-Shigella was negatively correlated with body weight and colon length, and positively correlated with disease activity index and IL-1[Formula: see text]. Furthermore, through gut microbiota depletion, we confirmed that SJZD exerted anti-inflammatory activities in a gut microbiota-dependent manner, and fecal microbiota transplantation (FMT) validated the mediating role of gut microbiota in the SJZD treatment of UC. Through gut microbiota, SJZD modulates the biosynthesis of bile acids (BAs), especially tauroursodeoxycholic acid (TUDCA), which has been identified as the signature BA during SJZD treatment. Cumulatively, our findings disclose that SJZD attenuates UC via orchestrating gut homeostasis in microbial modulation and intestinal barrier integrity, thus offering a promising alternative approach to the clinical management of UC.

Ethnopharmacological Relevance: Duijinsan (DJS) is a famous Chinese medicine prescription composed of Radix scutellariae (RS) and Rhei Radix (RRR), which has been mainly used for treating migraine., Aim of the Study: This study aimed to uncover the anti-migraine active compounds from DJS and preliminary predicted the pharmacological mechanism by evaluating the spectrum-effect relationship between high-performance liquid chromatography (HPLC) fingerprints and anti-migraine effects of Duijinsan (DJS) extract combined with molecular docking., Materials and Methods: HPLC and LC-MS were applied for chemical analyses of DJS extracts in different proportions. Inhibition of DJS extracts on trigeminal nerve cell releasing calcitonin gene related peptide (CGRP) experiment was performed. The active compounds were screened by spectrum-effect relationship analysis and confirmed by molecular docking and the activities of major predicted compounds were validated in vitro., Results: Twenty-six common peaks were assigned and identified from the fingerprints of different proportions DJS extracts. In vitro experimental results showed that DJS extracts inhibited inflammation and release of CGRP from trigeminal nerve cells. Five predicted active compounds, Chrysin 6-C-arabinoside 8-C-glucoside, Chrysin 6-C-glucoside 8-C-arabinoside, baicalin, Chrysin-7-O-Beta-D-glucoronide and Oroxylin A 7-O-glucuronide were sorted out according to spectrum-effect relationship analysis and molecular docking comprehensively. In vitro validation experiments showed that all the predicted compounds inhibited the CGRP releasing and the activation of TRPV1 channel. Baicalin, chrysin-7-O-β-D-glucuronide and Oroxylin A-7-glucoronide significantly inhibited the activation of TRPV1 channel., Conclusion: Chrysin 6-C-arabinoside 8-C-glucoside, Chrysin 6-C-glucoside 8-C-arabinoside, baicalin, Chrysin-7-O-Beta-D-glucoronide and Oroxylin A 7-O-glucuronide which can inhibit the CGRP releasing and the activation of TRPV1 channel were screened as the anti-migraine active compounds by spectrum-effect relationship analysis and molecular docking., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Headings Ethnopharmacological Relevance: Coronary heart disease (CHD) usually refers to myocardial ischemia or myocardial necrosis caused by coronary artery stenosis. GeGen and DanShen (GD) are popular Chinese herbs for the treatment of angina pectoris and myocardial infarction (MI). This sentence needs to be a separate paragraph., Aim of the Study: This study was to investigate the role of GD extract in promoting ischemic myocardial angiogenesis, and to explore its signaling mechanism, so as to provide a more reliable scientific basis for the clinical treatment of ischemic cardiovascular disease., Materials and Methods: GD extract was initially analyzed by HPLC-Q-TOF MS. In vitro, migration assay and tube formation assay were subsequently used to detect the angiogenesis activity of GD extract in human umbilical vein endothelial cells (HUVECs). Following the in vitro study, an MI rat model was established by ligating the left anterior descending coronary artery (LAD), immediately followed by a 4-week daily GD extract treatment by intragastric administration. After the animal sacrifice, hematoxylin-eosin (HE) staining was conducted to observe the pathological changes of the infarct margin. Besides, the MI area was measured by 2,3,5-triphenyltetrazoliumchloride (TTC) staining. The microvascular density (MVD) was also quantified through CD31 immunohistochemistry. Moreover, the levels of VEGF, TXB2 and 6-keto-PGF1α in serum were detected by enzyme-linked immunosorbent assay. The expression of VEGFR2 and ERK were detected by immunohistochemistry as well., Results: In vitro study, GD extract was found to induce significant angiogenesis in HUVECs. In vivo, smaller infarct size was found in treatment groups than that of the model group, and the protein expression of VEGFR2 as well as ERK in the marginal zone of MI in treatment groups were significantly increased. The morphological changes of myocardium were observed with a significant growth in the number of new blood vessels. Regarding the effect of GD extract, the serum levels of CK, LDH and TXB2 were consequently reduced, whereas the levels of VEGF, 6-keto-PGF1α were significantly increased., Conclusions: Based on the findings of this study, GD extract had a protective effect against MI in rats. The possible mechanism is to promote angiogenesis by regulating the VEGF/VEGFR2 signaling pathway after MI occurrence., (Copyright © 2020. Published by Elsevier B.V.)

Daphne genkwa Sieb. et Zucc., as a traditional oriental herb, has been widely distributed and employed in China. The major bioactive components in D. genkwa are flavonoid compounds, which showed pharmacological activities such as anti-inflammatory, analgesic, anti-tumor and immunomodulatory activities. In this study, we analyzed total flavonoids in D. genkwa and their metabolites in normal and adjuvant arthritis (AA) rat plasma, urine and feces samples by liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (LC-Q-TOF-MS). A total of 4 metabolites in plasma, 9 metabolites in urine and 15 metabolites in feces were characterized respectively by LC-Q-TOF-MS technology in normal rat. And 9 of the metabolites were observed in the AA rat urine, while there was no prototype drug or its metabolites detected in plasma and fecal samples. The metabolic pathway mainly involves hydroxylation, methylation, glucuronide, sulfate conjugation, oxidation and reduction, during the phase I and phase II biotransformation pathway. All the information gained here will be greatly helpful in elucidating the potential biological and pharmacological mechanism of flavonoid in D. genkwa, thus providing new ideas for drug development., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Pain is an unpleasant sensory and emotional experience in many diseases and is often caused by intense or damaging stimuli. Pain negatively affects the quality of life and increases high health expenditures. Drugs with analgesic properties are commonly used to relieve pain, but these Western medications could be overwhelmed by side effects including tolerance and addiction. Herbal medicines may provide alternative measures for pain management. In this review paper, after introduction of Chinese medicine theory and treatment modality, emphasis is placed on the application of Chinese herbs and herbal formulations in pain management. Three of the most commonly used herbs, i.e., Corydalis yanhusuo , Ligusticum chuanxiong , and Aconitum carmichaeli , are reviewed. Subsequently, using this ancient medical remedy, Chinese herbal formulation in treating common medical conditions associated with pain, such as headache/migraine, chest pain, abdominal pain, low back pain, neuropathic pain, osteoarthritis, and cancer pain, is presented. Chinese herbal medicines could be considered as a complementary and integrative approach in the modern armamentarium in combating pain.

An efficient method combined with fingerprint and chemometric analyses was developed to evaluate the quality of the traditional Chinese medicine plant Penthorum chinense Pursh. Nine samples were collected from different regions during different harvest periods, and 17 components in the form of extracts were simultaneously examined to assess quality by using high-performance liquid chromatography. The hepatoprotective effects of components were investigated by assessing the inhibition of SMMC-7721 cell growth. The results indicated that the quality control method was accurate, stable, and reliable, and the hierarchical heat-map cluster and the principle component analyses confirmed that the classification of all nine samples was consistent. Quercetin and ellagitannins including pinocembrin-7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-glucose (PGHG), thonningianin A, thonningianin B, and other flavonoids were abundant in the extracts, and significantly contributed to the hepatoprotective effects.

The root of Oplopanax elatus (Nakai) Nakai has a well-known history of use for the treatment of diseases such as neurasthenia, cardiovascular disorders, and cancer by the native people in northeast China. It is important to screen and identify the bioactive molecules from its root rapidly. Hereby, an off-line two-dimensional high performance liquid chromatography coupled with diode array detection and tandem time-of-flight mass spectrometry together with 2,2'-diphenyl-1-picrylhydrazyl was established to screen antioxidants from the root of O. elatus. A Waters cyanogen column (150 × 3.9 mm, id, 4 μm) was used for the first dimensional liquid chromatography, while a Hypersil BDS-C18 column (250 × 4.6 mm, id, 5 μm) was installed for the second dimension liquid chromatographic analysis. Twenty-eight compounds had been tentatively identified from the methanol extract of the air-dried root of O. elatus including six polyynes and eight phenolic derivatives were screened with antioxidant activity. The developed method could be expedient for screening and identifying antioxidants from O. elatus., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Background: Metformin plays an important role in diabetes treatment. Studies have shown that the combined use of oral hypoglycemic medications is more effective than metformin monotherapy. In this double-blind, randomized, placebo-controlled, multicenter trial, we evaluated whether Jinlida, a Chinese herbal medicine, enhances the glycemic control of metformin in type 2 diabetes patients whose HbA1c was ineffectively controlled with metformin alone., Methods: A total of 186 diabetes patients were enrolled in this double-Blind, randomized, placebo-controlled, multicenter trial. Subjects were randomly allocated to receive either Jinlida (9 g) or the placebo TID for 12 consecutive weeks. All subjects in both groups also continuously received their metformin without any dose change. During this 12-week period, the HbA1c, FPG, 2 h PG, body weight, BMI were assessed. HOMA insulin resistance (HOMA-IR) and β-cell function (HOMA-β) were also evaluated., Results: At week 12, compared to the HbA1c level from week 0, the level of the Jinlida group was reduced by 0.92 ± 1.09% and that of the placebo group was reduced by 0.53 ± 0.94%. The 95% CI was 0.69-1.14 for the Jinlida group vs. 0.34-0.72 for the placebo group. There was a very significant HbA1c reduction between the two groups after 12 weeks (p < 0.01). Both FG and 2 h PG levels of the Jinlida group and placebo group were reduced from week 0. There were a very significant FG and 2 h PG level reductions between the two groups after 12 weeks (both p < 0.01). The Jinlida group also showed improved β-cell function with a HOMA-β increase (p < 0.05). No statistical significance was observed in the body weight and BMI changes. No serious adverse events were reported., Conclusion: Jinlida significantly enhanced the hypoglycemic action of metformin when the drug was used alone. This Chinese herbal medicine may have a clinical value as an add-on medication to metformin monotherapy., Trial Registration: Chinese Clinical Trial Register ChiCTR-TRC-13003159.

Ethnopharmacological Relevance: Salvia miltiorrhiza (Danshen in Chinese) is a common traditional Chinese herbal medicine often used to treat many medical conditions. The Compound Danshen Dripping Pill (CDDP) is a danshen-containing Chinese herbal product for the treatment of cardiovascular diseases. However, to date, no controlled clinical studies have been conducted to evaluate the effects of CDDP on diabetic retinopathy (DR)., Aim of the Study: The present large-scale clinical trial was designed to assess the effectiveness and safety of CDDP in treating patients with non-proliferative diabetic retinopathy (NPDR)., Materials and Methods: 223 NPDR patients were enrolled in this controlled trial. Subjects received oral study medications three times daily for 24 weeks. The four groups were placebo, low-dose (270 mg), mid-dose (540 mg) and high dose (810 mg herbal medicine). Primary endpoints were changes in fluorescence fundus angiography (FFA) and fundoscopic examination parameters., Results and Discussion: At 24 weeks, for the FFA, the percent of "Excellent" and "Effective" in the high-dose and mid-dose CDDP groups was 74% and 77%, respectively, very significantly higher than 28% in the placebo group (P<0.001). For fundoscopic examination, the percent of "Excellent" and "Effective" in the high-dose and mid-dose CDDP groups was 42% and 59%, respectively, very significantly higher than 11% in the placebo group (P<0.001). No adverse events with clinical significance were observed., Conclusions: DR is a severe microvascular complication of diabetes and a major cause of adult blindness worldwide. Our clinical trial data demonstrated the therapeutic value and safety of a danshen-containing Chinese herbal medicine in patients with diabetic retinopathy., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

Ethnopharmacological Relevance: The roots and rhizomes of Smilax riparia are called "Niu-Wei-Cai" in traditional Chinese medicine (TCM). This botanical has been used in treating the symptoms of gout and other hyperuricemic-related conditions in TCM. Allopurinol is a commonly used medication to treat hyperuricemia and its complications. In this study, we evaluated whether Smilax riparia could enhance allopurinol׳s effects by decreasing the serum uric acid level in a hyperuricemic mouse model induced by potassium oxonate., Materials and Methods: We examined the effects of allopurinol (5mg/kg) administration alone or in combination with Smilax riparia saponins (SRS, 500 mg/kg) on the serum uric acid (SUA), serum creatinine (SCr) and blood urea nitrogen (BUN) levels in a hyperuricemic mouse model. The effects of allopurinol alone or those of allopurinol plus SRS on the XOD activities were measured. Western blot analysis was used to measure the levels of mURAT1, mGLUT9 and mOTA1 in the mice., Results: Compared with allopurinol alone, the combination of allopurinol and SRS significantly decreased the serum uric acid level and increased the urine uric acid level (both P<0.05), leading to the normalized serum and urine uric acid concentrations. Data on serum and urine creatinine and BUN supported these observations. The attenuation of hyperuricemia-induced renal dysfunction was linked to the inhibition of both serum and hepatic xanthine oxidase (XOD), the down-regulation of renal mURAT1 and mGLUT9, and the up-regulation of mOAT1., Conclusion: The anti-hyperuricemia effects of allopurinol are improved by Smilax riparia co-administration. The results were supported by the measurement of uric acid, creatinine, BUN, XOD, mURAT1, mGLUT9 and mOAT1. Our data may have a potential value in clinical practice in the treatment of gout and other hyperuricemic conditions., (Copyright © 2015. Published by Elsevier Ireland Ltd.)

To improve the transdermal delivery of ligustrazine, Foeniculum vulgare food origin anisole compounds were employed as promoters. Transdermal fluxes of ligustrazine were determined by Franz-type diffusion cells. Fourier transform-infrared (FT-IR) spectra were used to detect the biophysical changes of the stratum corneum and to explore the mechanism of permeation enhancement. A scanning electron microscope (SEM) was used to monitor the morphological changes of the skin. Among the three anisoles, anisic acid increased the penetration flux of ligustrazine significantly. The ligustrazine flux with anisic acid (11.9 μg/cm(2)/h) was higher than that any other group (p < 0.05). Spectra observations revealed that these anisole enhancers were able to disturb and extract the stratum corneum lipids. In addition, apparent density was used to describe the desquamation extent of the scutella. Multiple mechanisms are involved in the permeation enhancement of ligustrazine, including disturbing and extracting stratum corneum lipid, forming a competitive hydrogen bond. All data suggested that anisole compounds could be a group of safe and active penetration enhancers for transdermal delivery of ligustrazine.

Background: Previous data indicate that purified components of ginseng can inhibit HIV reverse transcriptase in vitro, suggesting that ginseng components in plasma may interfere with HIV-1 RNA detection assays., Methods: Pre- and post-dose plasma from three volunteers dosed with 3000 mg American ginseng was spiked with HIV and analyzed by the Roche COBAS Ampliprep/Taqman v2.0 HIV-1 RNA assay., Results: Presence of American ginseng had no significant effect on measured HIV-1 RNA concentration. Variation within pre- and post-dose plasma pair was insignificant and within assay performance limits., Conclusion: Plasma from subjects dosed with 3000 mg American ginseng does not interfere with the Roche COBAS Ampliprep/Taqman v2.0 HIV-1 RNA assay. This implies that in vitro inhibition of HIV reverse transcriptase by American ginseng components is unlikely to be clinically relevant.

The chemical constituents were isolated and purified by various chromatographic techniques indluding silica gel, reverse phase silica gel, sephadex LH-20 and pre-HPLC and identified by their physicochemical properties and spectral data. Sixteen phenolic compounds had been isolated and n-butanol extracts which were fractionated from the ethanol extract of Oplopanax horridus roots bark. Their structures were identified as below, including 7 phenylpropanoid compounds, ferulic acid (1), 3-acetylcaffeic acid (2), caffeic acid (3), homovanillyl alcohol 4-O-beta-D-glucopyranoside (4), 3-hydroxyphenethyl alcohol 4-O-beta-D-glucopyranoside (5), 3, 5-dimethoxycinnamyl alcohol 4-O-beta-D-glucopyranoside (6), and 3-dimethoxycinnamyl alcohol 4-O-beta-D-glucopyranoside (7). Three coumarins, scopoletin (8), esculetin (9) and 3'-angeloyl-4'-acetyl-cis-knellactone (10). And 6 lignan compounds, (+)-isolaricires-inol-9'-O-beta-D-glucopyranoside (11), 3, 3'-dimethoxy-4, 9, 9'-trihydroxy-4', 7-epoxy-5', 8-lignan-4, 9-bis-O-beta-D-glucopyranoside (12), (+)-5, 5'-dimethoxylariciresinol 4'-O-beta-D-glucopyranoside (13), (-)-5,5'-dimethoxylariciresinol 4'-O-beta-D-glucopyranoside (14), (-)-pinoresinol 4'-O-beta-D-glucopyranoside (15), and (+)-5, 5'-dimethoxylariciresinol 9'-O-beta-D-glucopyranoside (16). All compounds were isolated and identified for the first time from this plant All the constituents except compounds 4, 6, 12 and 13 were obtained for the first time from the genus Oplopanax.

Context: Living in a prediabetes state significantly increases a patient's risk for both diabetes and cardiovascular disease. Tianqi capsule, containing 10 Chinese herbal medicines, is used in China for the treatment of type 2 diabetes mellitus (T2DM)., Objective: The purpose of this study was to assess whether Tianqi prevented T2DM in subjects with impaired glucose tolerance (IGT) over the course of a 12-month treatment., Methods: Individuals with IGT were randomly allocated in a double-blind manner to receive Tianqi (n = 210) or a placebo (n = 210) for 12 months. Oral glucose tolerance tests were conducted every 3 months to assess the development of diabetes or restoration to normal glucose tolerance. All subjects received the same lifestyle education. The primary endpoint was the conversion of IGT to T2DM. Body weight and body mass index were observed. Adverse effects were monitored., Results: Of the 420 enrolled subjects with IGT, 389 completed the trial (198 in the Tianqi group and 191 in the placebo group). At the end of the 12-month trial, 36 subjects in the Tianqi group (18.18%) and 56 in the placebo group (29.32%) had developed diabetes (P = .01). There was a significant difference in the number of subjects who had normal glucose tolerance at the end of the study between the Tianqi and placebo groups (n = 125, 63.13%, and n = 89, 46.60%, respectively; P = .001). Cox's proportional hazards model analysis showed that Tianqi reduced the risk of diabetes by 32.1% compared with the placebo. No severe adverse events occurred in the trial. There were no statistical differences in body weight and body mass index changes between the Tianqi group and the placebo group during the 12-month trial., Conclusions: Treatment with a Tianqi capsule for 12 months significantly decreased the incidence of T2DM in subjects with IGT, and this herbal drug was safe to use.

From the twigs and leaves of Pseuduvaria indochinensis Merr., a new benzopyran derivative, pseudindochin (1), was isolated together with three known compounds, oligandrol (2), (6E,10E)-isopolycerasoidol (3) and polycerasoidol (4). The structure of compound 1 was elucidated on the basis of extensive spectroscopic data interpretation, including 1D, 2D NMR, HR-ESI-MS, UV and IR. Moreover, compounds 1-4 were evaluated in vitro for their cytotoxic activities against HL-60 and SMMC-7721 cell lines, but these compounds were essentially non-cytotoxic (IC50>30 μg/mL).

Aim: TM81 (or Tang-Min-Ling-Wan) is a Chinese medicine. Previous studies suggested that this medicine is effective for treating type 2 diabetes. This controlled trial evaluated the safety and effectiveness of TM81 in the treatment of type 2 diabetic patients., Methods: This study was a large-scale controlled clinical trial to evaluate the safety and effectiveness of TM81 on type 2 diabetes. After a 2-week run-in period, 480 overweight type 2 early-stage diabetic patients [35-65 years old, HbA1c ≥ 7.0%, fasting plasma glucose (FPG) 7.0-13.9 mM or 2 h plasma glucose (PG) > 11.1 mM, body mass index (BMI) ≥ 24 kg/m(2)] were enrolled. These patients were divided into a TM81 group and placebo group in a 3 : 1 ratio. The subjects received 6 g TM81 or placebo, three times daily for 12 weeks., Results: After treatment, the HbA1c decrease was 1.02% in the TM81 group versus 0.47% in the placebo group. The FPG decreased 0.8 ± 0.1 mM in the TM81 group versus an increase of 0.2 ± 0.2 mM in the placebo group. The PG decreased 2.7 ± 0.3 mM in the TM81 group versus a decrease of 0.9 ± 0.4 mM in the placebo group (all p < 0.05). The TM81 was more effective for patients with higher baseline HbA1c levels. The TM81 group also showed improved β-cell function and increased homeostatic model assessment (HOMA)-β. In addition, body weight, BMI and waist circumference of subjects in the TM81 group were reduced, and the symptoms related to diabetes were improved. There were no significant differences in the types and frequency of adverse reactions between the two groups., Conclusions: The data showed that TM81 is effective in controlling blood glucose level and is safe to use in patients with early-stage type 2 diabetes., (© 2012 Blackwell Publishing Ltd.)

Inflammatory bowel disease increases the risks of human colorectal cancer. In this study, the effects of Salvia miltiorrhiza extract (SME) on chemically-induced colitis in a mouse model were evaluated. Chemical composition of SME was determined by HPLC analysis. A/J mice received a single injection of AOM 7.5 mg/kg. After one week, these mice received 2.5% DSS for eight days, or DSS plus SME (25 or 50 mg/kg). DSS-induced colitis was scored with the disease activity index (DAI). Body weight and colon length were also measured. The severity of inflammatory lesions was further evaluated by colon tissue histological assessment. HPLC assay showed that the major constituents in the tested SME were danshensu, protocatechuic aldehyde, salvianolic acid D, and salvianolic acid B. In the model group, the DAI score reached its highest level on Day 8, while the SME group on both doses showed a significantly reduced DAI score (both p < 0.01). As an objective index of the severity of inflammation, colon length was significantly shorter in the model group than the vehicle group. Treatment with 25 and 50 mg/kg of SME inhibited the shortening of colon in a dose-related manner (p < 0.05 and p < 0.01, respectively). SME groups also significantly reduced weight reduction (p < 0.05). Colitis histological data supported the pharmacological observations. Thus, Salvia miltiorrhiza could be a promising candidate in preventing and treating colitis and in reducing the risks of inflammation-associated colorectal cancer.

In the present study, rapid resolution liquid chromatography was coupled with quadrupole time-of-flight tandem mass spectrometry (RRLC-Q-TOF-MS) to identify the absorbed components and metabolites in rat urine after oral administration of Buyang Huanwu decoction (BYHWD). After oral administration of BYHWD, urine samples were collected and pretreated by solid phase extraction. The mass measurements were accurate within 5 ppm of error for all the protonated molecules, and subsequent fragment ions offered higher quality structural information for interpretation of the fragmentation pathways of various compounds. A total of 50 compounds were detected in rat urine samples within 20 min, including 12 parent compounds and 38 metabolites. Except for three prototype components (Hydroxysafflor yellow A, Paeoniflorin, and Amygdalin), the metabolites identified mainly came from Radix Astragali, Radix Angelicae Sinensis, and Rhizoma Chuanxiong. The results indicated that glucuronidation and sulfation were the major metabolic pathways of isoflavonoids, while glutathione conjugation, glucuronidation and sulfation were the main metabolic pathways of phthalides. No saponin-related metabolites were detected. The present study provided important structural information on the metabolism of BYHWD. Furthermore, the results of this work have demonstrated the feasibility of the RRLC/ESI-Q-TOF-MS approach for rapid and reliable characterization of metabolites from herbal medicines., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Spinosin, a major bioactive herbal ingredient isolated from Semen Ziziphi Spinosae, plays an important role in sedation and hypnosis. However, the pharmacokinetic behavior of spinosin in special sites has not been reported. Microdialysis (MD) technique, as a continuous, realtime monitoring sampling technique, is very suitable for the evaluation of the disposition of diverse drugs. To obtain more useful information on spinosin, an in vivo microdialysis sampling technique with High Performance Liquid Chromatography-mass spectrograph (HPLC-MS) method was developed to investigate the pharmacokinetics of spinosin and its interaction with cyclosporin A (CsA) in the brain, blood and bile of rats. The method was validated in terms of selectivity, linearity and sensitivity, and showed advantages in monitoring the pharmacokinetic behavior of drugs. The results revealed that CsA has obvious effects on the pharmacokinetic process of spinosin. When co-administered, the area under the curve (AUC) of spinosin in blood, bile and brain increased from 205.70 to 673.51 mg min/L, 7.77 × 10(4) to 1.25 × 10(5) mg min/L, and 2.09 to 5.58 mg min/L, respectively. The t(1/2) values of spinosin in blood, bile and brain also changed from 48.07 to 95.04 min, from 97.20 to 152.21 and from 42.18 to 73.83 min, respectively. These results demonstrated that the CsA decreased the efflux of spinosin through the inhibition of P-glycoprotein (P-gp) efflux transporter and it might be used as a group of P-gp substrate. Other transporters or pathways may also be involved in the metabolism of spinosin., (Copyright © 2011 Elsevier B.V. All rights reserved.)

Ten new tirucallane-type triterpenoids, represented by a rearranged skeleton dysolenticin A (1), dysolenticin B (2), a rare trinortriterpenoid dysolenticin C (3), three tirucallane triterpenoid derivatives with a hemiketal moiety dysolenticins D-F (4-6), dysolenticins G-I (7, 9, 10), and the new alkaloid dysolenticin J (12), together with seven known analogues were isolated from the twigs and leaves of Dysoxylum lenticellatum. Their structures were elucidated by extensive spectroscopic methods, and those of compounds 1, 3, 4, 6, and 10 were confirmed by single-crystal X-ray diffraction experiments. Dysolenticin J (12) showed significant vasodilative effects on intact rat aortic rings with a diastolic degree of 87.4% at 10 μg/mL.

Furanodiene is a sesquiterpene extracted from the essential oil of the rhizome of Curcuma wenyujin Y.H. Chen et C. Ling (Wen Ezhu). Furanodiene is the primary component in Wen Ezhu's essential oil, accounting for more than 20% by weight. In vitro, MTT assay was used to compare the inhibitory effects of furanodiene and Wen Ezhu's essential oil on 11 human cancer cell lines. Compared to the essential oil, furanodiene showed stronger growth inhibitions on Hela, Hep-2, HL-60, PC3, SGC-7901 and HT-1080 cells with IC(50) between 0.6-4.8 microg/ml. In vivo, furanodiene was also found to exhibit inhibitory effects on the growth of uterine cervical (U14) and sarcoma 180 (Sl80) tumors in mice. Our data suggests that furanodiene, an active component from the essential oil of Wen Ezhu, possesses efficacy against uterine cervical cancer.

Colorectal cancer remains one of the most prevalent cancer and a leading cause of cancer related death in the US. Many currently used chemotherapeutic agents are derived from botanicals. Identifying herbal sources, including those from ginseng family, to develop better anti-cancer therapies remains an essential step in advancing the treatment of the cancer. In this article, potential roles of ginseng herbs, especially American ginseng and notoginseng, in colorectal cancer therapeutics are presented. The major pharmacologically active constituents of ginsengs are ginsenosides, which can be mainly classified as protopanaxadiol and protopanaxatriol groups. Structure-activity relationship between their chemical structures and pharmacological activities are discussed. In addition, various steaming temperature and time treatment of the ginseng herbs can change ginsenoside profiles, and enhance their anti-cancer activities. This heat treatment process may increase the role of ginseng in treating colorectal cancer.

In this study, we evaluated the effects of Panax notoginseng root extract (NGRE) and its major constituents on SW480 human colorectal cancer cells. We used high performance liquid chromatography to determine the contents of major saponins in NGRE. The anti-proliferative effects were evaluated by the cell counting method, and concentration-related anti-proliferative effects were observed. At 1.0 mg/ml, NGRE inhibited cell growth by 85.8% (P<0.01), probably linked to the higher concentration of ginsenosides Rb1 and Rg1. The pharmacologic activities of notoginsenoside R1 and ginsenosides Rg1 and Rb1 on the cells were antiproliferative. We tested the effects of NGRE on DNA synthesis by measuring [3H]-thymidine incorporation. NGRE induced cell apoptosis at 0.5 and 1 mg/ml. Two-day treatment with 300 microM of notoginsenoside R1, ginsenosides Rg1 and Rb1 increased cell apoptosis significantly. Cell cycle and cyclin A assay showed that NGRE arrested cells in the synthesis phase and increased the expression of cyclin A remarkably. NGRE also enhanced the actions of two chemotherapeutic agents, 5-fluorouracil and irinotecan. Cell growth decreased more with the combined treatment of NGRE and 5-fluorouracil (or irinotecan) than with the chemotherapy agent applied alone, suggesting that notoginseng can reduce the dose of 5-fluorouracil (or irinotecan) needed to achieve desired effects. Further in vivo and human trials are warranted to test whether notoginseng is a valuable chemo-adjuvant with clinical validity.

Bulbus Fritillariae (BF) is the most commonly used antitussive herb in China. There are nine species of Fritillaria recorded as the drug BF in the Chinese Pharmacopoeia. Bulbus Fritillariae cirrhosae (BF cirrhosae) is a group that includes four species of BF; these four species come from wild sources with higher efficiency and lower toxicity compared to the other five species of BF. Due to reasons of carelessness and reduced costs, the other five species are often sold as BF cirrhosae. Analysis through appearance, microscopic and chemical techniques has limitations. Identifying botanical resources is a primary step in the standardization of herbal medicine. In the present article, the internal transcribed spacer 1 (ITS1) regions of the nuclear ribosomal DNA (nrDNA) of nine species and one variety of Fritillaria genus have been sequenced. A mutation site in the ITS1 region among BF cirrhosae and other species of BF has been found and can be recognized by the restriction endonuclease SmaI. Polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) analysis of the nuclear ribosomal ITS1 region was used to differentiate BF cirrhosae from other species of BF and is a successful method in distinguishing the subgroups.

Ganoderma lucidum is a herbal medicine commonly used in oriental countries as a remedy for treating various medical conditions. In this controlled study, we evaluated the safety and tolerance of oral administration of Ganoderma lucidum in 16 human volunteers who received 2 grams of the extract or placebo twice daily for 10 consecutive days. During the study, information from subjective questionnaires were obtained, electrocardiograms, complete blood counts, blood chemistry analysis and urinalysis were performed. In addition, blood tests reflecting immunity were done. Our data showed that compared to placebo group, no adverse effects were observed after the extract intake. Although there were no obvious changes in CD4, CD8, and CD19 levels after the extract, CD56 cell count increased during the study and returned to baseline 10 days after the herbal intake. However, due to relatively high variability and small sample size, this CD56 increase did not achieve statistical significance, and remains to be re-evaluated in the future. It appears that an additional long-term safety and tolerance trial with herbal dose-escalating design is warranted.

Chemotherapy is highly cytotoxic, causing a number of severe adverse effects such as nausea and vomiting. Herbal medicines, which can often be used on a daily basis for prolonged treatment, may be clinically beneficial. Ganoderma lucidum or Lingzhi mushroom has been recognized as a remedy in treating a number of medical conditions, including balancing immunity and decreasing drug-induced side effects. It has been shown that rats react to emetic stimuli, like the chemotherapy agent cisplatin, by increased consumption of kaolin, known as pica; and this rat model has been utilized to evaluate novel anti-emetic compounds. In this study, we evaluated the effects of a G. lucidum extract (SunRecome, the most commonly used Lingzhi mushroom extract in China) in attenuating cisplatin-induced nausea and vomiting in the rat pica model. We observed that intraperitoneal cisplatin injection caused a significant increase in kaolin intake at 24, 48, 72 and 96 hours, reflecting cisplatin's nausea and vomiting action. This cisplatin-induced kaolin intake dose-dependently decreased after 1, 3 and 10 mg/kg G. lucidum extract injection (p < 0.01). In addition, there was a significant reduction of food intake after cisplatin. The cisplatin-induced food intake reduction improved significantly after G. lucidum extract administrations in a dose-related manner (p < 0.01), suggesting a supportive effect of the extract on general body condition. Future controlled clinical trials are needed to evaluate the safety and effectiveness of this herbal medication.

Ephedra has been commonly used in traditional Chinese medicine (TCM) without significant adverse effects. Ephedra-containing dietary supplements are widely used in the United States to promote weight reduction and energy enhancement. However, there are significant safety concerns regarding the use of ephedra-containing dietary supplements, especially when such use occurs by consumers without medical supervision. This article reviews and contrasts the usage of ephedra as a dietary supplement in the US against an herbal medication in TCM. The potential adverse effects of ephedra-containing dietary supplements are also reviewed.

Purpose: Nausea/vomiting are significant side effects associated with the use of chemotherapy in cancer patients. Treatment of nausea/vomiting caused by cisplatin, a potent chemotherapeutic agent and one of the most emetogenic stimuli, requires a combination of different antiemetic drugs. In this study, we investigated the effects of Scutellaria baicalensis, an antioxidant herbal medicine, on cisplatin-induced nausea using a rat model., Methods: Rats react to emetic/nausea-producing stimuli, such as cisplatin, with altered feeding habits, manifested by pica or increased consumption of kaolin (a type of clay). We measured pica in rats to quantify cisplatin-induced nausea, and to evaluate the antinausea effect of pretreatment with S. baicalensis extract (SbE) given intraperitoneally., Results: Cisplatin at 3 mg/kg induced significant pica accompanied by reduced food intake, suggesting the presence of nausea. Hence, this cisplatin dose was selected for testing the antinausea activity of SbE. Cisplatin-induced pica decreased significantly when animals were pretreated with SbE at doses of 1 mg/kg and 3 mg/kg ( P<0.01). At a higher SbE dose (10 mg/kg), kaolin consumption increased, rather than further decreased, and was significantly different from that in the groups treated with low SbE doses., Conclusions: SbE pretreatment decreased cisplatin-induced kaolin intake in the rat model of simulated nausea, suggesting that SbE and its active constituent(s) may play a therapeutic role in chemotherapy-induced emesis. Absence of therapeutic effect at the highest tested SbE dose could have been a result of prooxidant activity often associated with excess antioxidant concentration.

The acquired immunodeficiency syndrome (AIDS) is a result of human immunodeficiency virus (HIV) infection which subsequently leads to significant suppression of immune functions. AIDS is a significant threat to the health of mankind, and the search for effective therapies to treat AIDS is of paramount importance. Several chemical anti-HIV agents have been developed. However, besides the high cost, there are adverse effects and limitations associated with using chemotherapy for the treatment of HIV infection. Thus, herbal medicines have frequently been used as an alternative medical therapy by HIV positive individuals and AIDS patients. The aim of this review is to summarize research findings for herbal medicines, which are endowed with the ability to inhibit HIV. In this article, we will emphasize a Chinese herbal medicine, Scutellaria baicalensis Georgi and its identified components (i.e., baicalein and baicalin), which have been shown to inhibit infectivity and replication of HIV. Potential development of anti-AIDS compounds using molecular modeling methods will also be discussed.

Qian-kun-nin is a Chinese herbal formulation considered to have anti-infection, anti-tumor and immuno-enhancing properties. Data from previous investigations showed that qian-kun-nin causes HIV growth inhibition and immunomodulation in vitro, suggesting that this formula has the ability to inhibit HIV and modulate impaired immune functions in humans. We conducted this pilot study to evaluate the anti-retroviral and immunological enhancing effects of this formula on HIV positive subjects. Eight subjects completed the study, receiving oral qian-kun-nin capsules for 24 consecutive weeks in a single blind design. Compared to baseline level, the plasma virus load decreased significantly at the end of week 12 (p < 0.01) and week 24 (p < 0.01), respectively. Four weeks after cessation of qian-kun-nin treatment, plasma virus load was still significantly lower compared to baseline (p < 0.01). Blood CD4 cell counts were increased significantly at the end of the 12th week compared to the baseline level (p < 0.01). No adverse effects were observed, and no significant side effects were recorded in any subjects. These data suggest that qian-kun-nin has therapeutic potential in the treatment of HIV positive patients.

Chan su (dried toad venom) is a traditional Chinese medicine obtained from the skin venom gland of the toad. Chan su has long been used as a therapeutic agent in China and other Asian countries. Recent reports indicate that Chan su toxicity carries a high mortality rate in the United States. This study focused upon the cardiac electrophysiological and electro-toxicity effects of resibufogenin (RBG), one of the major components in Chan su. Action potentials of isolated sheep and canine heart Purkinje fibers were studied using glass microelectrode recording techniques. The results indicate that RBG significantly affected all parameters of transmembrane action potential, induced delayed after depolarization, and triggered arrhythmias in sheep and canine Purkinje fibers.

Shi-Quan-Da-Bu-Tang is a traditional Chinese herbal medicine formula used to increase vital energy, and strengthen health and immunity. Data from previous studies demonstrated that this formula also has the ability to attack tumor tissue. The Erkang capsule is a modified formula of Shi-Quan-Da-Bu-Tang, with the addition of four other herbs to increase the adaptogen effects and ergogenic properties. Results from this study in mice indicated that the Erkang treated group had significant differences in mortality, body weight change, fatigue, cold temperature endurance, and immune function related organ weight change, compared to the control animals.

From pericarps of Rosa davurica (Rosaceae), a traditional Chinese medicine, eight known tetracyclic triterpene acids, three known flavonoids, ethyl beta-fructopyranoside and methyl 3-O-beta-glucopyranosyl-gallate were isolated.