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Ethnopharmacological Relevance: Qingxin Lianzi Yin Decoction (QXLZY), a Chinese classical formula, has been widely used in the treatment of various chronic kidney diseases over 1,000 years. However, the current studies on QXLZY were mostly focused on its clinical efficacy, lacking systematic material basis research on constituents., Aim of the Study: This work aims to elucidate and quantify the chemical constituents, clarify the blood-absorbed components and excretion pathways, predict major bioactive constituents and discover potential therapeutic targets., Materials and Methods: UHPLC-LTQ-Orbitrap HRMS was employed to clarify the chemical constituents and metabolites of QXLZY. The extraction of diagnostic ion and neutral loss fragment was aimed for searching specific type of constituents. The plasma, urine, bile and feces samples of rats after oral administration of QXLZY were systematically studied. UHPLC-QQQ-MS/MS was employed to simultaneously detect different types of constitutes. Based on the analysis of ingredients in vivo, the bioactive constituents and potential therapeutic targets in the treatment of diabetic nephropathy (DN) was investigated by using network pharmacological analysis., Results: Totally, 220 compounds were identified or tentatively characterized by UHPLC-LTQ-Orbitrap HRMS. Among them, 59 compounds were confirmed by reference standards. Meanwhile, 21 representative components were simultaneously determined within 15 min by UHPLC-QQQ-MS/MS. 123 components (74 prototypes as well as 49 metabolites) were identified or tentatively characterized. By using network pharmacological analysis, baicalein, liquiritigenin, succinic acid, formononetin, wogonin might be the major effective constituents in QXLZY during the treatment of DN., Conclusions: Flavonoids, saponins and organic acids were the major chemical ingredients of QXLZY. Flavonoids were the main components absorbed into blood, followed by organic acids. Phase II conjugation reaction was the major metabolic type. The pathways that QXLZY in the treatment of DN were probably related to glucose and lipid metabolism, oxidative stress and inflammation., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Crotonis Fructus is the mature fruit of Croton tiglium L. (Euphorbiaceae), which has been used in traditional Chinese medicine for the treatment of gastrointestinal (GI) diseases, such as constipation, abdominal pain, peptic ulcer, and intestinal inflammation for thousands of years. The aim of this study was to investigate the pharmacological effect of extracts and fractions from Crotonis Fructus on GI tract., Materials and Methods: The activities of methanol extract and fractions from Crotonis Fructus on the smooth muscle contractions were evaluated using isolated rabbit jejunum model., Results: The results suggest that the n-BuOH and H(2)O fractions showed spasmolytic activity, while the MeOH extract, PE and EtOAc fractions exerted spasmogenic effect. Moreover, bioassay-guided fractionation verified that the EtOAc fraction was more potent than others, followed by PE fraction and methanol extract. Additionally, atropine (10μM), 4-DAMP (10μM) and verapamil (0.1μM) produced a significant inhibition of contractions caused by EtOAc fraction, while either hexamethonium (10μM) or methoctramine (10μM) was inactive. Additionally, a HPLC fingerprint of EtOAc fraction was appraised to ensure its chemical consistency and the main component has been identified as phorbol 12-acetate-13-tiglate., Conclusions: These data indicate that the regulatory effect of EtOAc fraction on GI motility are medicated via the activation of M3 muscarinic receptor and Ca(2+) influx through L-type Ca(2+) channel. These provide a scientific basis for the traditional use of Crotonis Fructus in GI disorders., (Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.)

Aim of Study: Croton oil is the fruit oil of Croton tiglium L., which is well known in folk medicine for the treatment of gastrointestinal (GI) diseases, including constipation, abdominal pain, peptic ulcer, and intestinal inflammation for a long period. This study was to investigate the pharmacological effect of croton oil on GI tract., Materials and Methods: The effect of croton oil on the smooth muscle contractions was investigated in vitro using the isolated rabbit jejunum model., Results: Croton oil has a biphasic action contracting and relaxing intestinal tissue. At the concentrations of 20-80 microg/mL, croton oil produced a concentration-dependent increase in the amplitude and tension of muscle contractions, whereas at high concentrations (>200 microg/mL) it decreased the contractile amplitude and had no impact on the tension. Moreover, croton oil was less effective in increasing muscle amplitude and tension than Ach, confirming that the effect of croton oil on muscle contractions is not a simply stimulatory or inhibitory action, but a unique modulatory process depending on the concentration of croton oil. In addition, croton oil concentration-dependently suppressed the frequency of muscle contractions. On the other hand, atropine (10 microM) and 4-DAMP (10 microM) produced a significant inhibition of contractions caused by croton oil, while either hexamethonium (10 microM) or methoctramine (10 microM) was inactive, implying that the regulatory effects of croton oil on GI motility are mediated via the activation of M3 muscarinic receptor. Furthermore, muscle contractions induced by croton oil were dramatically reduced by verapamil (0.1 microM) but not by NE (1 microM), suggesting that the action of croton oil on GI motility is also mediated by Ca(2+) influx through L-type Ca(2+) channel., Conclusions: The results suggest that croton oil possesses spasmogenic and spasmolytic properties and the regulatory effects of croton oil on GI motility are mediated via the activation of M3 muscarinic receptor and Ca(2+) influx through L-type Ca(2+) channel., (Copyright 2010 Elsevier Ireland Ltd. All rights reserved.)

Aim of the Study: Wei-Chang-An-Wan (WCAW), a traditional pharmaceutical preparation, has been used for treating various gastrointestinal (GI) diseases for several decades, but it is still poorly understood how it works on those disorders. This study was to investigate the effects of WCAW extract on GI tract., Materials and Methods: The activities of the methanol extract (ME) of WCAW on castor oil-induced diarrhoea, gastrointestinal transit (GIT) in mice, and contractions of isolated rabbit jejunum were investigated. We further assessed the safety of ME in vivo. Additionally, a HPLC fingerprint of ME was appraised to ensure its chemical consistency., Results: Ten peaks were identified in the HPLC fingerprint of ME. At the doses of 400 and 800 mg/kg, ME significantly protected mice against castor oil-induced diarrhoea as well as the number of faeces and wet faeces. Interestingly, administration of ME significantly accelerated GIT in normal mice and reduced stimulated GIT induced by neostigmine. ME also dose-dependently attenuated spontaneous contractions of the isolated rabbit jejunum, and those induced by acetylcholine (Ach) and neostigmine. Moreover, oral administration of ME up to 5 g/kg did not produce any toxic effects. Taken together, ME is able to inhibit diarrhoea, increase normal GIT, and decrease GIT induced by neostigmine, which indicate that ME might play a bidirectional role in GI tract., Conclusions: Our study provides a scientific basis for the clinical use of WCAW.

Xuan-Ju agent is an herbal formula containing aqueous extract of Formica fusca, Herba epimedii, Fructus cnidii, and Fructus lycii, all of which are reputed for their beneficial effects in the treatment of the immunodeficient diseases such as rheumatoid arthritis. We performed a study on the anti-inflammatory effects of this agent using carrageenan- and adjuvant-induced paw edema in rats. Xuan-Ju agent showed a marked inhibitory effect on edema in two models of inflammation in rats, at the dose of 0.20, 0.40 and 0.80g/kg. Based on this study, Xuan-Ju agent is considered to be a potentially useful drug suitable for further evaluation for rheumatoid arthritis.