The Prokinetic,Laxative, and Antidiarrheal Effects of Morus nigra: Possible Muscarinic,Ca2+ Channel Blocking,and Antimuscarinic Mechanisms

Morus nigra Linn. (black mulberry) is used in gastrointestinal ailments. This study demonstrates gut modulatory properties of M. nigra. The prokinetic, laxative, and antidiarrheal activities of M. nigra were assessed in mice, while isolated rabbit jejunum and guinea‐pig ileum were used to explore insight into mechanism(s). At 30 and 70 mg/kg, the crude extract of M. nigra (Mn.Cr) exhibited atropine‐sensitive prokinetic and laxative effects, similar to carbachol (CCh). While at higher doses (100, 300, and 500 mg/kg), Mn.Cr offered protection against castor oil‐induced diarrhea. In rabbit jejunum, Mn.Cr and its chloroform fraction inhibited CCh‐induced contractions more potently compared with high K⁺ (80 mm ). Conversely, petroleum fraction was more potent against high‐K⁺‐induced contractions. At 0.01 mg/mL, Mn.Cr caused a parallel shift in acetylcholine concentration–response curves (CRCs) followed by a non‐parallel shift at 0.03 mg/mL, similar to dicyclomine. At further tested concentrations, Mn.Cr (0.1 and 0.3 mg/mL) and petroleum fraction suppressed Ca²⁺ CRCs, similar to verapamil. In guinea‐pig ileum, Mn.Cr, its aqueous and ethyl acetate fractions exhibited atropine‐sensitive gut stimulant activity along with additional uncharacterized excitatory response in the aqueous fraction only. These results suggest that black mulberry possesses prokinetic, laxative, and antidiarrheal effects, putatively mediated through cholinomimetic, antimuscarinic, and Ca²⁺ antagonist mechanisms, respectively. Copyright © 2016 John Wiley & Sons, Ltd.     

Prokinetic and laxative activities of Lepidium sativum seed extract with species and tissue selective gut stimulatory actions

Aim of the study

To provide ethnopharmacological basis for the medicinal use of Lepidium sativum seeds in indigestion and constipation.

Materials and methods

The in vivo studies were conducted in mice, while isolated tissues of mouse, guinea-pig and rabbit were suspended in tissue bath to measure isotonic contractions.

Results

The aqueous-methanolic extract of Lepidium sativum seeds (Ls.Cr) at 30 and 100 mg/kg showed atropine-sensitive prokinetic and laxative activities in mice, which were partially sensitive to atropine. In isolated gut preparations of mouse and guinea-pig, Ls.Cr (0.1-1 mg/mL) caused a concentration-dependent stimulatory effects both in jejunum and ileum, which was blocked in the presence of atropine. In rabbit jejunum, the stimulant effect of Ls.Cr remained unchanged in the presence of atropine, pyrilamine or SB203186, while in rabbit ileum, the stimulatory effect was partially blocked by atropine. The Ls.Cr was more efficacious in gut preparations of rabbit than in guinea-pig or mouse. The phytochemical analysis of the plant extract detected alkaloids, saponins and anthraquinones as plant constituents.

Conclusion

This study showed the prokinetic and laxative effects of Lepidium sativum in mice, which were partially mediated through a cholinergic pathway. The in vitro spasmodic effect of the plant extract mediated through a similar mechanism with species and tissue-selectivity, provides a rationale for the medicinal use of the seeds of Lepidium sativum in indigestion and constipation, and suggests studying the plant extracts on more than one species to get the wider picture.     

Pharmacological Evaluation of Gut Modulatory and Bronchodilator Activities of Achyranthes aspera Linn.

Achyranthes aspera L. is traditionally used to relieve constipation, diarrhea, and asthma. Its crude extract (Aa.Cr) was evaluated through in vivo and ex vivo experiments to rationalize these medicinal uses of A. aspera and to provide their scientific basis. Aa.Cr, at 3 and 10 mg/kg, increased fecal output, similar to castor oil, whereas at 30, 100, 300, and 700 mg/kg, it protected against castor oil‐induced diarrhea in mice when administered orally. Aa.Cr caused spasmogenic effect on rabbit jejunum and guinea pig ileum preparations, which was partially inhibited by atropine while completely blocked by cyproheptadine preincubation. Aa.Cr also relaxed high K⁺ (80 mM)‐induced contraction in rabbit jejunum. Aa.Cr inhibited CCh (100 μg/kg)‐induced bronchospasm in rats, similar to aminophylline. Like dicyclomine, Aa.Cr relaxed high K⁺ and CCh (1 μM)‐induced contractions in guinea pig trachea and caused rightwards parallel shift of CCh concentration–response curves at the lower concentrations followed by non‐parallel shift at the higher concentrations. On activity‐directed fractionation, spasmogenic and spasmolytic activities of Aa.Cr were concentrated in aqueous and organic fraction, respectively. This study suggests the presence of dose‐specific laxative and antidiarrheal effects in A. aspera, possibly mediated through cyproheptadine‐sensitive receptors and dual cholinergic and calcium channel blockade, respectively. The latter combination is also a suggested mechanism underlying its bronchodilator effect. Copyright © 2017 John Wiley & Sons, Ltd.     

The antidiarrheal and spasmolytic activities of Phyllanthus emblica are mediated through dual blockade of muscarinic receptors and Ca2+ channels

Aim of the study

This study was aimed at providing the possible mechanisms for the medicinal use of Phyllanthus emblica in diarrhea.

Materials and methods

The in vivo studies were conducted in mice, while isolated rabbit jejunum and guinea-pig ileum were used for the in vitro experiments.

Results

The crude extract of Phyllanthus emblica (Pe.Cr), which tested positive for alkaloids, tannins, terpenes, flavonoids, sterols and coumarins, caused inhibition of castor oil-induced diarrhea and intestinal fluid accumulation in mice at 500-700 mg/kg. In isolated rabbit jejunum, Pe.Cr relaxed carbachol (CCh) and K⁺ (80 mM)-induced contractions, in a pattern similar to that of dicyclomine. The preincubation of guinea pig-ileum with Pe.Cr (0.3 mg/mL), caused a rightward parallel shift in the concentration-response curves (CRCs) of acetylcholine without suppression of the maximum response. While at the next higher concentration (1 mg/mL), it produced a non-parallel rightward shift with suppression of the maximum response, similar to that of dicyclomine, suggesting anticholinergic and Ca²⁺ channel blocking (CCB)-like antispasmodic effect. The CCB-like activity was further confirmed when pretreatment of the tissue with Pe.Cr, shifted the CRCs of Ca²⁺ to the right with suppression of the maximum response, similar to nifedipine or dicyclomine. The activity-directed fractions of Pe.Cr showed a combination of Ca²⁺ antagonist and anticholinergic like components in all fractions but with varying potency.

Conclusion

These results indicate that the Phyllanthus emblica fruit extract possesses antidiarrheal and spasmolytic activities, mediated possibly through dual blockade of muscarinic receptors and Ca²⁺ channels, thus explaining its medicinal use in diarrhea.     

Calcium Channel Blocking Activity in Desmostachya bipinnata (L.) Explains its use in Gut and Airways Disorders

Desmostachya bipinnata, despite of its popular medicinal uses, has not been widely studied for its effect in diarrhea, indigestion, and asthma. The aim of the present investigation was to provide scientific rationale for these applications. The crude aqueous‐methanolic extract of D. bipinnata (Db.Cr) was evaluated through in vivo and in vitro experiments. Db.Cr (100–500 mg/kg) protected mice against castor oil–induced diarrhea, similar to loperamide. When tested on gut preparations, Db.Cr produced an atropine‐sensitive spasmogenic effect in rabbit jejunum up to 5 mg/mL, followed by a partial relaxation at 10 mg/mL. With atropine preincubation, a verapamil‐like inhibitory effect was evident against spontaneous and high K⁺ (80 mM)–induced contractions. The maximum stimulant effect was comparable with the acetylcholine‐induced maximum contraction and was similarly reproducible in guinea pig ileum. Db.Cr inhibited carbachol (1 μM)‐induced contraction in rabbit trachea but caused an atropine‐sensitive accentuation of high K⁺–induced contraction at 0.003–0.3 mg/mL followed by inhibition at 1–5 mg/mL. On activity‐directed fractionation, inhibitory effect was concentrated on organic and stimulant effect in aqueous fraction. This study, suggesting the presence of calcium antagonist activity, possibly underlying its medicinal effect in hyperactive gut and respiratory disorders, and cholinergic activity, possibly underlying its digestive effect, provides rationale for these therapeutic uses of D. bipinnata. Copyright © 2012 John Wiley & Sons, Ltd.     

Gastrointestinal stimulant effect of Urginea indica Kunth. and involvement of muscarinic receptors

Urginea indica Kunth. (Family; Liliaceae) was studied for its gastrointestinal stimulant effect to rationalize the traditional medicinal uses as a digestive aid, stomachic and laxative. The crude aqueous-methanol extract of Urginea indica bulb (Ui.Cr) was tested on mice and isolated gut preparations. Ui.Cr, which was tested positive for alkaloids, tannins and coumarins, increased faecal output and accelerated charcoal meal transit in mice (6-12 mg/kg, p.o.), similar to that caused by carbachol (10 mg/kg). Ui.Cr (0.01-1 mg/mL) caused a spasmogenic effect in guinea-pig ileum that was reproduced in rabbit jejunum (0.01-0.3 mg/mL) followed by relaxation at a higher concentration. Like carbachol, the stimulant effect of Ui.Cr was blocked by atropine, suggesting the activation of muscarinic receptors mediating the prokinetic effect. Ui.Cr (0.01-5.0 mg/mL) also inhibited K(+) (80 mm)-induced contraction in rabbit jejunum and shifted the Ca(2+) concentration-response curves to the right, similar to verapamil, a standard calcium channel blocker. These data, indicating the presence of a gastrointestinal stimulant effect in Urginea indica possibly mediated through a cholinergic mechanism, provide a rationale for the use of Urginea indica in indigestion and constipation. The presence of a calcium antagonist effect in the plant may help to alleviate untoward effects of the plant that may result from an excessive increase in gut motility.     

Species Differences in the Antidiarrheal and Antispasmodic Activities of Lepidium sativum and Insight into Underlying Mechanisms

The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in‐vivo and in‐vitro experiments. Ls.Cr inhibited castor oil‐induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K⁺ (25 mM) and high K⁺ (80 mM)‐induced contractions, while in guinea‐pig tissues, Ls.Cr caused complete inhibition of only CCh‐induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K⁺‐induced contractions sensitive to K⁺ channel antagonists. Pretreatment of guinea‐pig and rat tissues with Ls.Cr caused a rightward shift in CCh‐induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K⁺ channels, and inhibition of muscarinic receptors, Ca⁺⁺ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.     

Pharmacological Basis for Medicinal Use of Lens culinaris in Gastrointestinal and Respiratory Disorders

Crude extract of Lens culinaris (Lc.Cr), which tested positive for presence of anthraquinones, flavonoids, saponins, sterol, tannins, and terpenes exhibited protective effect against castor oil‐induced diarrhea in mice at 100–1000 mg/kg. In rabbit jejunum preparations, Lc.Cr caused relaxation of spontaneous contractions at 0.03–5.0 mg/mL. Lc.Cr inhibited carbachol (CCh, 1 μM) and K⁺ (80 mM)‐induced contractions in a pattern similar to dicyclomine, but different from verapamil and atropine. Lc.Cr shifted the Ca⁺⁺ concentration‐response curves to the right, like dicyclomine and verapamil. Pretreatment of tissues with Lc.Cr (0.03–0.1 mg/mL) caused leftward shift of isoprenaline‐induced inhibitory CRCs, similar to papaverine. In guinea‐pig ileum, Lc.Cr produced rightward parallel shift of CCh curves, followed by non‐parallel shift at higher concentration with suppression of maximum response, similar to dicyclomine, but different from verapamil and atropine. Lc.Cr (3.0–30 mg/kg) caused suppression of carbachol (CCh, 100 µg/kg)‐induced increase in inspiratory pressure of anesthetized rats. In guinea‐pig trachea, Lc.Cr relaxed CCh and high K⁺‐induced contractions, shifted CCh curves to right and potentiated isoprenaline response. These results suggest that L. culinaris possesses antidiarrheal, antispasmodic, and bronchodilator activities mediated possibly through a combination of Ca⁺⁺ antagonist, anticholinergic, and phosphodiesterase inhibitory effects, and this study provides sound mechanistic background to its medicinal use in disorders of gut and airways hyperactivity, like diarrhea and asthma. Copyright © 2014 John Wiley & Sons, Ltd.     

Isoliquiritigenin,a flavonoid from licorice,plays a dual role in regulating gastrointestinal motility in vitro and in vivo

Licorice root has been used for years to regulate gastrointestinal function in traditional Chinese medicine. This study reveals the gastrointestinal effects of isoliquiritigenin, a flavonoid isolated from the roots of Glycyrrhiza glabra (a kind of Licorice). In vivo, isoliquiritigenin produced a dual dose‐related effect on the charcoal meal travel, inhibitory at the low doses, while prokinetic at the high doses. In vitro, isoliquiritigenin showed an atropine‐sensitive concentration‐dependent spasmogenic effect in isolated rat stomach fundus. However, a spasmolytic effect was observed in isolated rabbit jejunums, guinea pig ileums and atropinized rat stomach fundus, either as noncompetitive inhibition of agonist concentration‐response curves, inhibition of high K⁺ (80 mM)‐induced contractions, or displacement of Ca²⁺ concentration‐response curves to the right, indicating a calcium antagonist effect. Pretreatment with N^ω‐nitro‐L‐arginine methyl ester (L‐NAME; 30 µM), indomethacin (10 µM), methylene blue (10 µM), tetraethylammonium chloride (0.5 mM), glibenclamide (1 µM), 4‐aminopyridine (0.1 mM), or clotrimazole (1 µM) did not inhibit the spasmolytic effect. These results indicate that isoliquiritigenin plays a dual role in regulating gastrointestinal motility, both spasmogenic and spasmolytic. The spasmogenic effect may involve the activating of muscarinic receptors, while the spasmolytic effect is predominantly due to blockade of the calcium channels. Copyright © 2008 John Wiley & Sons, Ltd.     

Gastrointestinal stimulatory and uterotonic activities of dietary radish leaves extract are mediated through multiple pathways

Raphanus sativus, commonly known as radish, is a food plant known worldwide for its culinary and medicinal properties especially as a laxative and abortifacient. This study reports the gastrointestinal and uterine tone modulatory activities of the crude extract (Rl.Cr) of radish leaves. Rl.Cr, showing the presence of saponins and alkaloids, exhibited a spasmogenic effect (0.03-10 mg/mL) in isolated rabbit jejunum, rat stomach fundus and uterus which was partially blocked by atropine. In contrast, Rl.Cr was found to be devoid of any stimulatory effect in rat ileum, instead showed an inhibitory effect (0.1 mg/mL) on the ACh dose-response curves. A mild relaxant effect was also observed in rabbit jejunum at the lower doses (0.1-0.3 mg/mL) but not against K(+)-induced contractions, ruling out a calcium channel blocking effect. In guinea-pig ileum, Rl.Cr exhibited a stimulant effect resistant to atropine while sensitive to pyrilamine pretreatment. The aqueous fraction, showing a strong presence of saponins, was found to be more efficacious than the non-polar fractions in its spasmogenic effect. This study shows the presence of species-dependent gastrointestinal effects of radish mediated partially through cholinergic receptors in rabbit and rat tissues, but through histaminergic activation in the guinea-pig, providing a scientific basis for its use in gut and uterine affections while also giving a wider picture of the activity profile of radish by using different species of animals.     

Pharmacological basis for the medicinal use of muskmelon base (Pedicellus Melo.) for abdominal distention and constipation

Ethnopharmacological relevance

Muskmelon base (Pedicellus Melo.) has a long history (Ming Dynasty) as a Chinese traditional medicine. According to traditional use, it was prepared as rectal suppositories for treating abdominal distention and constipation. The present study was carried out on the pharmacological basis for the medicinal use of muskmelon base.

Aim of the study

The objective of this study was to determine the pharmacological basis for the medicinal use of the ethanol extract from muskmelon base (EMB) for abdominal distention and constipation.

Materials and methods

In this study, we report the gastrointestinal prokinetic action of EMB following single rectal or large intestinal administration. Laxative activity, gastric emptying and small intestinal transit tests were examined in ICR mice. SD rats were used to determine changes in large intestinal transit and contractile effects of the proximal colon in vivo. Guinea pigs were used to evaluate the contractile effects of the proximal colon and the possible mechanism or mechanisms on proximal colon activity ex vivo. Moreover, the acute toxicity of EMB was evaluated.

Results

In the in vivo experiments, the acute toxicity test showed that the maximum tolerated dose (MTD) of EMB was 400 mg/kg. A laxative effect was observed in mice at different dosages (6.5, 13 and 26 mg/kg). EMB showed a dose-dependent acceleration of gastric emptying (13 and 26 mg/kg). It also promoted both small intestinal (6.5, 13 and 26 mg/kg) and large intestinal (4, 8 and 16 mg/kg) transit activity. In the SD rat model, single rectal administration of EMB (8 and 16 mg/kg) showed a significant increase in both the frequency and amplitude of proximal colon smooth muscle contractility. These increases in amplitude and frequency peaked 30–60 min after EMB administration and corresponded with the results of the laxative activity test. The ex vivo experiments showed that varying doses of EMB (11.5, 23 and 46 mg/kg) had a direct prokinetic effect that was sensitive to atropine.

Conclusions

Our results show that EMB is a low dosage, fast acting drug with a large therapeutic window (4–400 mg/kg) and shows significant gastrointestinal prokinetic action after single rectal or large intestinal administration. This gastrointestinal prokinetic effect was stronger in the intestines than in the stomach. This effect was sensitive to atropine, suggesting that EMB acts mainly through cholinergic mechanisms.     

Pharmacological basis for the medicinal use of Carissa carandas in constipation and diarrhea

Ethnopharmacological relevance

Carissa carandas Linn. commonly known as “Karaunda” (Apocynaceae) is a popular medicinal herb widely distributed in different parts of Pakistan. In addition to other medicinal uses, Carissa carandas is popular in indigenous system of medicine for its medicinal use in gut motility disorders like, constipation and diarrhea.

Objective

This study was planned to provide pharmacological basis to the medicinal use of Carissa carandas in constipation and diarrhea.

Materials and methods

The crude extract of the leaves of Carissa carandas (Cc.Cr) was prepared in methanol and its fractionation was carried out with ethylacetate, petroleum ether and n-butanol. In-vivo studies were conducted on mice, while isolated rabbit jejunum and guinea-pig ileum preparations were used for the in-vitro experiments. The spasmogenic and spasmolytic responses of gut tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system.

Results

The HPLC fingerprints of Cc.Cr, its petroleum (Cc.Pef), ethylacetate (Cc.Eaf) and n-butanol (Cc.Baf) fractions showed the presence of oleanolic acid, ursolic acid, stigmasterol and β-sitosterol. Oral administration of Cc.Cr to mice increased fecal output at lower doses (30 and 50 mg/kg), while it showed protection against castor oil-induced diarrhea at higher doses (300 and 600 mg/kg). In isolated guinea-pig ileum and rabbit jejunum, Cc.Cr and Cc.Baf exhibited stimulatory effect at 0.003–3 mg/ml, which was partially sensitive to atropine or pyrillamine or partially/fully sensitive to atropine+pyrillamine, followed by relaxation at higher tested concentrations, being more potent in rabbit tissues. The ethylacetate fraction (0.1–5 mg/ml) exhibited fully atropine-sensitive contractions in both guinea-pig and rabbit tissues, being more potent in guinea-pig while more efficacious in rabbit tissues. However, the petroleum fraction (0.003–1.0 mg/ml) showed only spasmolytic activity in spontaneously contracting rabbit tissues, similar to nifedipine. In guinea-tissue, Cc.Pef did not cause any stimulant effect. When studied against high K⁺ (80 mM)-induced contraction, the crude extract and its fractions caused a dose-dependent inhibition, with the following order of potency: Cc.Pef>Cc.Eaf>Cc.Cr≥Cc.Baf, similar to nifedipine indicating Ca⁺⁺ channel antagonist like activity, which was further confirmed when the plant extract displaced Ca⁺⁺ curves to the right with suppression of maximum effect similar to that of nifedipine.

Conclusion

This study demonstrates that the crude extract of Carissa carandas possesses a gut-stimulatory effect mediated primarily through the activation of muscarinic and histaminergic receptors while its spasmolytic effect was mediated possibly through Ca⁺⁺ antagonist pathway. Thus, this study provides a clear evidence for the dual effectiveness of Carissa carandas in constipation and diarrhea, thus validating its medicinal use.     

Blood pressure lowering,cardiovascular inhibitory and bronchodilatory actions of Achillea millefolium

Achillea millefolium Linn. (Asteraceae) is used in folk medicine for the treatment of overactive cardiovascular and respiratory ailments. This study describes its hypotensive, cardio‐depressant, vasodilatory and bronchodilatory activities. The crude extract of Achillea millefolium (Am.Cr) caused a dose‐dependent (1–100 mg/kg) fall in arterial blood pressure of rats under anaesthesia. In spontaneously beating guinea‐pig atrial tissues, Am.Cr exhibited negative inotropic and chronotropic effects. In isolated rabbit aortic rings, Am.Cr at 0.3–10 mg/mL relaxed phenylephrine (PE, 1 µm ) and high K⁺ (80 mm )‐induced contractions, as well as suppressed the PE (1 µm ) control peaks obtained in Ca⁺⁺‐free medium, like that caused by verapamil. The vasodilator effect of Am.Cr was partially blocked by N_ω‐nitro‐l ‐arginine methyl ester in endothelium intact preparations. In guinea‐pig tracheal strips, Am.Cr inhibited carbachol (CCh, 1 µm ) and K⁺‐induced contractions. These results indicate that Achillea millefolium exhibits hypotensive, cardiovascular inhibitory and bronchodilatory effects, thus explaining its medicinal use in hyperactive cardiovascular and airway disorders, such as hypertension and asthma. Copyright © 2010 John Wiley & Sons, Ltd.     

Antispasmodic,bronchodilator and blood pressure lowering properties of Hypericum oblongifolium – possible mechanism of action

The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration‐dependent (0.1–1.0 mg/mL) relaxation of spontaneous and high K⁺ (80 mM)‐induced contractions in isolated rabbit jejunum preparations, suggesting a Ca⁺⁺ antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca⁺⁺ concentration‐response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 μM) and high K⁺‐induced contractions in guinea pig tracheal preparations. It caused a dose‐dependent (3–100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition of both atrial force and rate of spontaneous contractions. When tested in rabbit aortic rings, Ho.Cr exhibited a vasodilator effect against phenylephrine (1 μM) and high K⁺‐induced contractions. These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca⁺⁺ antagonist mechanism. Copyright © 2009 John Wiley & Sons, Ltd.     

余甘子的本草考证及其现代研究中若干问题的探讨

余甘子Phyllanthus emblica为药食两用的传统药材,在我国中医药及多民族医药中具有广泛且悠久的应用历史。不同医药体系、民族、地域及时期对余甘子的药用方式及功效认识存在差异。通过对历代本草典籍考证,系统梳理和归纳了余甘子的名称、基原、产地、用法及功效,并结合国内外文献报道对余甘子的鲜干差异、炮制工艺、道地品质与质量控制等现代研究相关问题进行探讨,以期为余甘子的临床有效应用、功能产品开发和相关基础研究提供一定的科学参考与理论依据。     

基于化学成分、药理作用和网络药理学的余甘子质量标志物(Q-Marker)预测分析

余甘子为大戟科植物余甘子Phyllanthus emblica的干燥成熟果实.对余甘子化学成分及主要药理作用进行综合分析,基于中药质量标志物(quality marker,Q-Marker)理论,对余甘子从传统药性、药效、药效物质基础和化学成分可测性的角度进行Q-Marker初步预测.基于文献整合及数据分析对余甘子Q-...     

Pharmacological basis for the medicinal use of Zanthoxylum armatum in gut,airways and cardiovascular disorders

This study describes the gut, airways and cardiovascular modulatory activities of Zanthoxylum armatum DC. (Rutaceae) to rationalize some of its medicinal uses. The crude extract of Zanthoxylum armatum (Za.Cr) caused concentration‐dependent relaxation of spontaneous and high K⁺ (80 mM)‐induced contractions in isolated rabbit jejunum, being more effective against K⁺ and suggestive of Ca⁺⁺ antagonist effect, which was confirmed when pretreatment of the tissues with Za.Cr shifted Ca⁺⁺ concentration‐response curves to the right, like that caused by verapamil. Za.Cr inhibited the castor‐oil‐induced diarrhea in mice at 300–1000 mg/kg. In rabbit tracheal preparations, Za.Cr relaxed the carbachol (1 μM) and high K⁺‐induced contractions, in a pattern similar to that of verapamil. In isolated rabbit aortic rings, Za.Cr exhibited vasodilator effect against phenylephrine (1 μM) and K⁺‐induced contractions. When tested in guinea pig atria, Za.Cr caused inhibition of both atrial force and rate of spontaneous contractions, like that caused by verapamil. These results indicate that Zanthoxylum armatum exhibits spasmolytic effects, mediated possibly through Ca⁺⁺ antagonist mechanism, which provides pharmacological base for its medicinal use in the gastrointestinal, respiratory and cardiovascular disorders. Copyright © 2009 John Wiley & Sons, Ltd.     

余甘子及其活性成分肝保护作用及机制的研究进展

余甘子来源于余甘子Phyllanthus emblica的干燥成熟果实,是我国重要的药食同源品种,具有抗炎、抗氧化、抗肿瘤和免疫调节等广泛的生物活性.通过对余甘子提取物及其所含没食子酸、鞣花酸及柯里拉京等活性成分的药理作用进行总结,发现其对肝损伤、病毒性肝炎、非酒精性脂肪肝、肝纤维化及肝癌等具有治疗作用,主要通过抑制脂...     

不同产地藏药余甘子总鞣质含量测定

目的:建立磷钼钨酸/干酪素分光光度法测定不同产地藏药余甘子中总鞣质含量的方法.方法:以没食子酸为对照品,磷钼钨酸为显色剂,检测波长760 nm,测定8个不同产地余甘子中总鞣质含量.结果:没食子酸在0.306～2.448 mg·L-1与吸光度呈良好线性关系(r=0.999 1),平均加样回收率99.27％,RSD 2.30％.不同产地余甘子药材总鞣质含量差别较大(6.72％ ～ 11.95％),印度和尼泊尔产余甘子中总鞣质含量最高.结论:该方法简单、准确、重复性好,可用于测定余甘子中总鞣质含量.     

Effects of an aqueous extract of Ferula ovina on rabbit and guinea pig smooth muscle

The effects of an aqueous extract of Ferula ovina were tested in vitro using isolated segments of rabbit and guinea pig intestine, trachea and aorta. The extract inhibited the spontaneous movements of rabbit jejunum and guinea pig ileum and the contractions induced by acetylcholine. The aqueous extract also inhibited the contractions of rabbit trachealis muscle induced by acetylcholine and the contractions of guinea pig trachealis muscle induced by histamine. These inhibitions were dose-dependent and reversible. However, the aqueous extract did not inhibit the contractions of rabbit and guinea pig aortic rings induced by norepinephrine. These data suggest that this plant has non-specific anticholinergic and antihistaminic antispasmodic effects.