Mingqiu Shan

Anti-inflammatory effects of Huangqin tang extract in mice on ulcerative colitis

ETHNOPHARMACOLOGICAL RELEVANCE HuangqinTang (HQT) is a traditional Chinese formula which is composed of Scutellaria baicalensis Georgi, Paeonia lactiflora Pall, Glycyrrhiza uralensis Fisch, and Ziziphus jujube Mill. HQT has been used in China for a wide range of disorders, especially in gastrointestinal inflammation with symptoms of nausea, vomiting, diarrhea, abdominal cramps and so on. AIM OF THE STUDY To investigate the protective effects of HQT extract on 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) induced colitis in mice. MATERIALS AND METHODS Different doses of HQT extract (1, 2 and 4 g/kg/day) and salicylazosulfapyridine (SASP, 500 mg/kg/day) were administered by gavage for 7 days after the induction of colitis with TNBS. The effects were studied by macroscopic score, histological analysis, immunohistochemical study of Cyclo-oxygenase-2 protein expression, as well as by determination of inflammation markers such as myeloperoxidase (MPO) and mRNA expression levels of pro-inflammatory cytokines, including TNF-α, IL-1β and IL-6. RESULTS In TNBS induced group, mice body weight decreased gradually and did not recover at the end of the experiment, as compared with that of control group (p<0.01). Edema and redness were also discovered in the colons profoundly and scores representing inflammation were all high in this group (p<0.01). The level of colonic MPO activity and the tissue levels of TNF-α, IL-1β and IL-6 were markedly increased (p<0.01). The mice treated with HQT extract and SASP recovered significantly compared with the TNBS group (p<0.01). CONCLUSION Our results suggested that the efficacy of HQT extract, especially at the higher dose, was analogous to that of SASP, which implicated its potential application as a natural alternative medicine in colitis treatment.

A Review on the Phytochemistry, Pharmacology, and Pharmacokinetics of Amentoflavone, a Naturally-Occurring Biflavonoid

Amentoflavone (C30H18O10) is a well-known biflavonoid occurring in many natural plants. This polyphenolic compound has been discovered to have some important bioactivities, including anti-inflammation, anti-oxidation, anti-diabetes, and anti-senescence effects on many important reactions in the cardiovascular and central nervous system, etc. Over 120 plants have been found to contain this bioactive component, such as Selaginellaceae, Cupressaceae, Euphorbiaceae, Podocarpaceae, and Calophyllaceae plant families. This review paper aims to profile amentoflavone on its plant sources, natural derivatives, pharmacology, and pharmacokinetics, and to highlight some existing issues and perspectives in the future.

Application of UHPLC-ESI-Q-TOF-MS to Identify Multiple Constituents in Processed Products of the Herbal Medicine Ligustri Lucidi Fructus

Ligustri Lucidi Fructus (LLF), the fruit of Ligustrum lucidum Ait. (Oleaceae), has been used as a common herbal medicine in clinical practice in China for nearly 2000 years. In most cases, LLF is prescribed in decoctions in the form of processed products rather than crude drugs. In this study, an ultra-high performance liquid chromatography coupled with electrospray ionization-quadrupole-time of flight-mass spectrometry (UHPLC-ESI-Q-TOF-MS) method was established for rapid separation and identification of multiple constituents in the 80% methanol extract of processed-LLF. A total of 50 compounds (one phenylethanoid, seven phenylethanoid glycosides, seven flavonoids, 25 iridoids, nine triterpenoids and one cyclohexanecarboxylic acid) were either unambiguously identified or tentatively characterized with the aid of authentic standards or published data. Luteolin-7-O-rutinoside, oleoside and secologanoside were detected in LLF for the first time. This study enriches the chemical profiling of processed-LLF and could provide valuable information for the quality control and further investigation of processed-LLF and crude LLF.

Anti-inflammatory effect of volatile oil from Schizonepeta tenuifolia on carrageenin-induced pleurisy in rats and its application to study of appropriate harvesting time coupled with multi-attribute comprehensive index method

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

Acute and subacute toxicity and genotoxicity of schizonepetin, a naturally occurring monoterpene with antiviral activity

In the present study, the acute, subacute and genetic toxicity of schizonepetin was assessed. The median lethal dose (LD(50)) of schizonepetin after oral administration was 478 mg/kg body weight in mice. Studies on dose toxicity were repeatedly conducted at 0, 60, 120, and 240 mg/kg bw/day in rats for 35 days after oral administration. Based on the results of this study, a dose level of 120 mg/kg bw/day is considered the no-observed-adverse-effect-level (NOAEL) in rats. Schizonepetin was negative in Salmonella typhimurium tester strains TA97, TA98, TA100, TA102 and TA1535, nonclastogenic in Chinese hamster lung (CHL) cells in the mammalian chromosome aberration test, and micronucleus formation were observed and no clinical signs or adverse effects were detected, and our results illustrated that schizonepetin is not genotoxic.

A Review on the Phytochemistry, Pharmacology, Pharmacokinetics and Toxicology of Geniposide, a Natural Product

Iridoid glycosides are natural products occurring widely in many herbal plants. Geniposide (C17H24O10) is a well-known one, present in nearly 40 species belonging to various families, especially the Rubiaceae. Along with this herbal component, dozens of its natural derivatives have also been isolated and characterized by researchers. Furthermore, a large body of pharmacological evidence has proved the various biological activities of geniposide, such as anti-inflammatory, anti-oxidative, anti-diabetic, neuroprotective, hepatoprotective, cholagogic effects and so on. However, there have been some research articles on its toxicity in recent years. Therefore, this review paper aims to provide the researchers with a comprehensive profile of geniposide on its phytochemistry, pharmacology, pharmacokinetics and toxicology in order to highlight some present issues and future perspectives as well as to help us develop and utilize this iridoid glycoside more efficiently and safely.

A Review of the Botany, Phytochemistry, Pharmacology and Toxicology of Rubiae Radix et Rhizoma

Rubia cordifolia Linn (Rubiaceae) is a climbing perennial herbal plant, which is widely distributed in China and India. Its root and rhizome, Rubiae Radix et Rhizoma (called Qiancao in China and Indian madder in India), is a well known phytomedicine used for hematemesis, epistaxis, flooding, spotting, traumatic bleeding, amenorrhea caused by obstruction, joint impediment pain, swelling and pain caused by injuries from falls. In addition, it is a kind of pigment utilized as a food additive and a dye for wool or fiber. This review mainly concentrates on studies of the botany, phytochemistry, pharmacology and toxicology of this Traditional Chinese Medicine. The phytochemical evidences indicated that over a hundred chemical components have been found and isolated from the medicine, such as anthraquinones, naphthoquinones, triterpenoids, cyclic hexapeptides and others. These components are considered responsible for the various bioactivities of the herbal drug, including anti-oxidation, anti-inflammation, immunomodulation, antitumor, effects on coagulation-fibrinolysis system, neuroprotection and other effects. Additionally, based on these existing results, we also propose some interesting future research directions. Consequently, this review should help us to more comprehensively understand and to more fully utilize the herbal medicine Rubiae Radix et Rhizoma.

Anti-thrombotic and pro-angiogenic effects of Rubia cordifolia extract in zebrafish

ETHNOPHARMACOLOGICAL RELEVANCE Rubia cordifolia is a common traditional Chinese medicine that promotes blood circulation and eliminates blood stasis, and has been used to cure diseases related to blood stasis syndrome (BSS) clinically for many years. It has been previously demonstrated that anti-thrombosis and pro-angiogenesis can improve BSS. However, the anti-thrombotic and pro-angiogenic activities of Rubia cordifolia have not been well investigated. AIM OF STUDY To determine the potential anti-thrombotic and pro-angiogenic activities of Rubia cordifolia and to elucidate the underlying mechanisms. In addition, the major chemical constituents of Rubia cordifolia extract (QC) were qualitatively analysed by UPLC-Q-TOF/MS to explore the association between pharmacological activity and chemical constituents. MATERIAL AND METHODS The QC samples were composed of a 95% ethanol extract and an aqueous extract following extraction using 95% ethanol. UPLC-Q-TOF/MS was used to analyse the major chemical constituents of QC. For the anti-thrombotic experiment of QC, a phenylhydrazine (PHZ)-induced AB strain zebrafish thrombosis model was used. The zebrafish larvae were stained using O-dianisidine, and the heart and caudal vein of the zebrafish were observed and imaged with a fluorescence microscope. The staining intensity of erythrocytes in the heart (SI) of each group and the morphology of thrombus in the caudal vein were used to assess the anti-thrombotic effect of QC. For the pro-angiogenic assay of QC, the intersegmental blood vessel (ISV) insufficiency model of Tg(fli-1: EGFP)y1 transgenic zebrafish (Flik zebrafish), which was induced by the VEGF receptor tyrosine kinase inhibitor II (VRI), was used. The morphology of the intact ISVs and defective ISVs was observed to evaluate the pro-angiogenic activity of QC. The mechanism involved in promoting angiogenesis was studied with real-time PCR. RESULTS A total of 12 components in QC were identified based on standard compounds and references, including nine anthraquinones and three naphthoquinones. After treatment with QC, the PHZ-induced thrombosis in AB strain zebrafish larvae decreased to a certain degree, which we believe was related to its dosages, and the therapeutic effect within the 50-200 µg/mL QC treatment groups was especially prominent (P < 0.01, P < 0.001) compared to that in the PHZ model group. Similarly, QC also recovered the loss of the ISVs, which was induced by VRI in Flik zebrafish larvae, which have a certain dose-effect relationship. The pro-angiogenic activity of QC was also conspicuous (P < 0.01, P < 0.001) compared to that of the VRI model group. The following real-time PCR assay proved that QC significantly restored the VRI-induced downregulation of vWF, VEGF-A, kdrl, and flt-1 in Flik zebrafish (P < 0.05, P < 0.01, P < 0.001). CONCLUSIONS A total of 12 compounds from QC were analysed by UPLC-Q-TOF/MS. The data of the pharmacological experiments demonstrated that QC presented anti-thrombotic and pro-angiogenic activities in zebrafish, and the principal active components were likely anthraquinones and naphthoquinones. Thus, the current study provided a theoretical basis for the clinical use of Rubia cordifolia as a traditional Chinese medicine in promoting blood circulation and eliminating stasis.

Correlation of Antioxidant Activity and Volatile Oil Chemical Components from Schizonepeta tenuifolia Herbs by Chemometric Methods

ABSTRACT In this paper, 15 batches of volatile oil from Schizonepeta tenuifolia herbs (STVO) originating from different areas of China were used to identify and quantify eight main components by GC-MS and to evaluate the antioxidant activity with 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging capacity by the HPLC method. The results indicated that with respect to the antioxidant activity and the contents of the main compounds, there were notable differences among the STVOs. IC50 values of the STVOs ranged from 0.016 to 1.518 mg/mL. To determine the correlation of the chemical components and the antioxidant activities, multiple linear regression analysis (MLRA) and partial least square analysis (PLSA) were performed. As a result, (+)-pulegone and (-)-menthone showed much closer relationships than the other components in each analysis. Hence, it was concluded that (+)-pulegone and (-)-menthone were the characteristic components that may exhibit potent antioxidant activities in STVO.