Antidiarrhoeal activity of the ethyl acetate extract of Baphia nitida (Papilionaceae)

In our search for plants useful in the treatment of diarrhoea, we investigated the ethyl acetate extract of Baphia nitida (BN) using intestinal transit, enteropooling and gastric emptying tests in mice and rats. In the castor oil intestinal transit test, BN produced a significant (P<0.05) dose dependent decrease in propulsion with peristaltic index (PI) values of 56.85+/-6.76, 36.84+/-3.04 and 31.98+/-2.60%, respectively at doses of 100, 200 and 400mg/kg vs. 89.33+/-6.28% for control. The effect at 400mg/kg was significantly lower than that of morphine, 10mg/kg, s.c. (20.29+/-3.78%), and was antagonized by isosorbide dinitrate, IDN (150mg/kg, p.o.) but not by yohimbine (1mg/kg, s.c.). This effect was not potentiated by atropine (1mg/kg, s.c.). In the castor oil-induced diarrhoea test, BN produced a significant increase in onset of diarrhoea (103.40+/-8.74, 138.80+/-17.04 and 174.8+/-29.04min, 100 to 400mg/kg, vs. 47.60+/-8.76min for control and 226.10+/-12.57min for morphine). The severity of diarrhoea (diarrhoea score) was dose dependently reduced (19.00+/-2.26, 17.04+/-1.89, 15.00+/-2.05, 100 to 400mg/kg, vs. 31.40+/-2.11 for control and 7.7+/-2.2 for morphine). This effect was not antagonized by IDN or yohimbine. The effect on severity was, however, potentiated by atropine. BN also reduced the number and weight of wet stools but did not have any significant effect on intestinal fluid accumulation and gastric emptying. Results obtained suggest that the ethyl acetate extract of Baphia nitida is endowed with antidiarrhoeal activity possibly mediated by interference with the l-arginine nitric oxide pathway and synergistic with antagonistic action on muscarinic receptors.     

Antidiarrhoeal and spasmolytic activities of the methanolic crude extract of Alstonia scholaris L. are mediated through calcium channel blockade

This study was aimed to provide a pharmacological basis to the medicinal use of Alstonia scholaris as an antidiarrhoeal and antispasmodic by using in vivo and in vitro techniques. In the in vivo study the crude extract of Alstonia scholaris (As.Cr), which tested positive for the presence of alkaloids, provided 31–84% protection against castor oil‐induced diarrhoea in mice at 100–1000 mg/kg doses, similar to loperamide. In isolated rabbit jejunum preparation, the As.Cr caused inhibition of spontaneous and high K⁺ (80 mm )‐induced contractions, with respective EC₅₀ values of 1.04 (0.73–1.48) and 1.02 mg/mL (0.56–1.84; 95% CI), thus showing spasmolytic activity mediated possibly through calcium channel blockade (CCB). The CCB activity was further confirmed when pretreatment of the tissue with the As.Cr (0.3–1 mg/mL) caused a rightward shift in the Ca⁺⁺ concentration‐response curves similar to verapamil, a standard calcium channel blocker. Loperamide also inhibited spontaneous and high K⁺ precontractions as well as shifted the Ca⁺⁺ CRCs to the right. These results indicate that the crude extract of Alstonia scholaris possesses antidiarrhoeal and spasmolytic effects, mediated possibly through the presence of CCB‐like constituent(s) and this study provides a mechanistic base for its medicinal use in diarrhoea and colic. Copyright © 2009 John Wiley & Sons, Ltd.     

Pharmacological analysis of paregoric elixir and its constituents: in vitro and in vivo studies

Paregoric elixir is a phytomedicinal product which is used widely as an analgesic, antispasmodic and antidiarrheal agent. Here, we investigated the pharmacological actions and some of the mechanisms of action of paregoric elixir and compared its action with some of its components, the alkaloids morphine and papaverine. The paregoric elixir given orally to mice did not present relevant toxic effects, even when administered in doses up to 2000-fold higher than those used clinically. However, it showed an antinociceptive action that was more potent, but less efficacious, than morphine. In contrast to morphine, its effect was not dose-dependent and not reversed by the non-selective opioid antagonist naloxone. Moreover, paregoric elixir produced tolerance, but did not cause cross-tolerance, with the antinociceptive actions of morphine. When assessed in the gastrointestinal motility in vivo, paregoric elixir elicited graduated reduction of gastrointestinal transit. Finally, like morphine and papaverine, paregoric elixir concentration-dependently inhibited electrically-induced contraction of the guinea pig isolated ileum. In vivo and in vitro gastrointestinal actions of paregoric elixir were not reversed by naloxone. Collectively, the present findings lead us to suggest that the pharmacological actions produced by paregoric elixir are probably due to a synergic action of its constituents.     

Bidirectional effects of methanol extract of Wei-Chang-An pill on gastrointestinal transit and the spasmolytic activity on isolated rat jejunum

Ethnopharmacological relevance

Wei-Chang-An pill (WCA pill), a traditional Chinese medicine, has been used for treating various gastrointestinal diseases for several decades. Despite the popular medicinal use of WCA pill, less data was available to its activity and mechanism in gastrointestinal disorders. To examine the effects of the methanol extract of WCA pill (ME) on gastrointestinal tract so as to assess some of the possible mechanisms involved in the clinical treatment.

Materials and methods

ME was studied on gastrointestinal transit in vivo including gastric emptying and small intestinal motility in normal and neostigmine-induced mice, as well as on the isolated tissue preparations of rat jejunum in vitro.

Results

In vivo, the gastric emptying decreased and intestinal transit increased after administration of ME in normal mice. However, administration of ME accelerated the intestinal transit ranging from 0.01 to 0.8 mg/mL and reduced it at the concentration of 1.6 and 3.2 mg/mL, while the gastric emptying was inhibited throughout the concentrations in neostigmine-induced mice. in vitro, ME caused inhibitory effect on the spontaneous contraction of rat-isolated jejunum in dose-dependent manner ranging from 0.01 to 6 mg/mL and also relaxed the acetylcholine chloride (Ach, 10⁻⁶ M)-induced and K⁺ (60 mM)-induced contractions. ME shifted the Ca²⁺ concentration–response curves to right, similar to that caused by verapamil (0.025 mM).

Conclusions

These results indicated that ME might play a bidirectional role in gastrointestinal transit modulation and the effects on isolated tissue are probably mediated through calcium influx and muscarinic receptors, which provides pharmacological basis for the clinical use of WCA pill in gastrointestinal tract disorders.     

Gut modulatory, blood pressure lowering, diuretic and sedative activities of cardamom

ETHNOPHARMACOLOGICAL RELEVANCE: Cardamom (Elettaria cardamomum) is traditionally used in various gastrointestinal, cardiovascular and neuronal disorders. AIM OF THE STUDY: To rationalize cardamom use in constipation, colic, diarrhea, hypertension and as diuretic. MATERIALS AND METHODS: Cardamom crude extract (Ec.Cr) was studied using in vitro and in vivo techniques. RESULTS: Ec.Cr caused atropine-sensitive stimulatory effect in isolated guinea-pig ileum at 3-10mg/ml. In rabbit jejunum preparations, Ec.Cr relaxed spontaneous and K+ (80 mM)-induced contractions as well as shifted Ca++ curves to right, like verapamil. Ec.Cr (3-100mg/kg) induced fall in the arterial blood pressure (BP) of anaesthetized rats, partially blocked in atropinized animals. In endothelium-intact rat aorta, Ec.Cr relaxed phenylephrine (1 microM)-induced contractions, partially antagonized by atropine and also inhibited K+ (80 mM) contractions. In guinea-pig atria, Ec.Cr exhibited a cardio-depressant effect. Ec.Cr (1-10mg/kg) produced diuresis in rats, accompanied by a saluretic effect. It enhanced pentobarbital-induced sleeping time in mice. Bio-assay directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively. CONCLUSION: These results indicate that cardamom exhibits gut excitatory and inhibitory effects mediated through cholinergic and Ca++ antagonist mechanisms respectively and lowers BP via combination of both pathways. The diuretic and sedative effects may offer added value in its use in hypertension and epilepsy.     

Antidiarrhoeal activity of seed extract of Albizzia lebbeck Benth

The antidiarrhoeal activity of the seed extract of Albizzia lebbeck (Benth.) was investigated employing conventional rodent models of diarrhoea, i.e. castor oil-induced diarrhoea, upper gastrointestinal transit (u.g.t.) and fluid secretion. It was found that the aqueous methanol extract of Albizzia lebbeck seeds (2.5-5 mg/kg i.p.) possessed antidiarrhoeal activity which strengthens the earlier use of the seeds in the treatment of diarrhoea and dysentery. The antidiarrhoeal dose of the extract was at least 10-30 times less than the LD(50) dose. The extract (2.5-5 mg/kg i.p.) potentiated the antidiarrhoeal activity of loperamide (1 mg/kg i.p.). Nalaxone (0.5 mg/kg i.p.) significantly inhibited the antidiarrhoeal activity of the extract as well as loperamide, thus indicating a role of the opioid system in the antidiarrhoeal activity of the extract.     

Antidiarrhoeal activity of the aqueous extract of Terminalia avicennoides roots

The antidiarrhoeal effects of the aqueous root extract of Terminalia avicennoides were evaluated in rodents. Studies were carried out on the isolated rabbit jejunum, gastrointestinal motility in vivo and on castor oil-induced diarrhoea in mice. The results revealed that the extract exhibited a concentration-dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum and attenuated acetylcholine induced contractions. The extract (100, 200 and 400 mg/kg) also caused a dose-dependent decrease of gastrointestinal transit and markedly protected mice against castor oil-induced diarrhoea. The intraperitoneal LD(50) of the extract was found to be 871.4-917.4 mg/kg in mice (95% confidence). A preliminary phytochemical screening of the aqueous extract of T. avicennoides roots revealed the presence of tannins, saponins and flavonoids. The results obtained showed that the water extract of T. avicennoides roots may contain some biologically active principles that may be active against diarrhoea and this may be the basis for its use traditionally for gastrointestinal disorders.     

Antidiarrhoeal and antiulcerogenic effects of methanolic extract of Asparagus pubescens root in rats

The effect of methanolic extract of Asparagus pubescens root on experimentally-induced diarrhoea and ulceration was investigated in rats. The extract (500-1500 mg/kg) dose-dependently, reduced significantly the intestinal propulsive movement, castor oil-induced diarrhoea and intestinal fluid accumulation. Yohimbine an alpha(2)-adrenoceptor blocker attenuated the antidiarrhoeal effect of the extract. The extract also reduced the ulcer indices induced by indomethacin and ethanol in a dose-related manner. The results indicate that its antidiarrhoeal and antiulcerogenic effects might in part be due to its alpha(2)-adrenoceptor stimulation and its active constituents respectively.     

Antidiarrhoeal evaluation of Aegle Marmelos (Correa) Linn. root extract

A study was undertaken to evaluate the in vitro and in vivo antidiarrhoeal potential of chloroform extract of the root of Aegle marmelos (Correa) Linn. The in vitro activity was determined by agar dilution and disc diffusion techniques. The extract was studied in vivo in rats. Of the 35 tested pathogenic diarrhoea causing strains, the extract was found to be mostly active against the strains of Vibrio cholerae, followed by Escherichia coli and Shigella spp. The in vitro activity was found to be comparable to that of ciprofloxacin. Further, Aegle marmelos root extract (AMRE) treated animals showed significant inhibitory activity against castor oil-induced diarrhoea. The results so obtained thus established the efficacy of AMRE as an effective antidiarrhoeal agent.     

Evaluation of the antidiarrhoeal effect of Sanseviera liberica Gerome & Labroy (Agavaceae) root extract

Ethnopharmacological relevance

The aqueous root extract of Sansevieraliberica (Agavaceae), SL, is used in Traditional African Medicine (TAM) for the treatment of diarrhoea. However, the scientific basis for this usage has not been established.

Aim of the study

To evaluate the antidiarrhoeal activity of SL using various pharmacological models.

Materials and methods

The intestinal transit, castor oil induced diarrhoea, enteropooling, and gastric emptying methods were used in this study.

Results

SL (25–400 mg/kg, p.o.) produced significant (P < 0.05) dose dependent reduction in propulsive movement in both the normal and castor oil induced intestinal transit tests in mice. Peak effect was elicited at 200 mg/kg but this effect was lower than that produced by morphine (10 mg/kg, s.c.). The effect of SL on castor oil induced intestinal transit was antagonized by isosorbide dinitrate, IDN (150 mg/kg, p.o.) but not by yohimbine (1 mg/kg, s.c.). In the castor oil induced diarrhoea test, SL significantly delayed the onset and decreased the frequency and severity of diarrhoea. The effect at 200 mg/kg was comparable to that of morphine and was reversed by IDN. SL at the dose of 200 mg/kg significantly reduced the volume of intestinal secretion induced by castor oil but produced no effect on gastric emptying.The extract was practically nontoxic administered p.o. The LD₅₀ was 631 mg/kg given i.p. Phytochemical analysis revealed the presence of oils, reducing sugars, alkaloids, saponins, anthraquinones, and tannins in the extract.

Conclusion

The results obtained in this study suggest that the aqueous root extract of Sanseviera liberica possesses antidiarrhoeal property due to inhibition of gastrointestinal propulsion and fluid secretion, possibly mediated through inhibition of the nitric oxide pathway. This justifies the use of the plant extract in TAM for the treatment of diarrhoea.     

Antidiarrhoeal activity of hot water extract of black tea (Camellia sinensis)

The effect of a hot water extract of black tea (Camellia sinensis (L.) O. Kuntze, Theaceae) on upper gastrointestinal transit and on diarrhoea was investigated employing conventional rodent models of diarrhoea. Black tea extract was found to possess antidiarrhoeal activity in all the models of diarrhoea used. Naloxone (0.5 mg/kg i.p.) significantly inhibited the antidiarrhoeal activity of the extract as well as loperamide, thus indicating a role of the opioid system in the antidiarrhoeal activity of the extract.     

针灸对血管活性肠肽影响的研究进展

血管活性肠肽是近年来被广泛研究的神经内分泌免疫调节肽,存在于多个系统中,具有多样的生物学作用,和许多疾病有密切关系。近年来关于针灸调节血管活性肠肽的研究较多,我们就近10年来国内外针灸与血管活性肠肽相关的文献进行回顾,发现有关针灸对血管活性肠肽的影响及其机制的研究涉及多个方面。本文从血管活性肠肽的生物学特性和功能,针灸对血管活性肠肽的生物学作用的影响,包括:(1)针灸对血管活性肠肽胃肠道激素功能的影响,(2)针灸对血管活性肠肽舒张血管作用的影响,(3)针灸对血管活性肠肽神经肽功能的影响,(4)针灸对血管活性肠肽免疫功能的影响等方面进行了综述。我们认为针灸可以通过神经体液调节方式对血管活性肠肽的产生和表达水平产生影响,但是针灸具体通过什么方式影响其产生的机制尚不明确,需要更进一步的研究。     

Antidiarrhoeal and antimicrobial activities of Emilia coccinea (Sims) G. Don extracts

Emilia coccinea (Sims) G. Don is reported to possess a number of medicinal properties including antidiarrhoeal and antimicrobial activities. The antidiarrhoeal effects of both methanol and aqueous extracts of the leaves of Emilia coccinea were studied in rats against castor oil-induced diarrhoea at the doses of 200, 400 and 600 mg/kg body weight. The methanol extract, and to a lesser extent the aqueous extract, significantly prolonged the time for diarrhoeal induction; it reduced the frequency of diarrhoea episodes and decreased the propulsion of charcoal meal through the gastrointestinal tract in a dose dependent manner. The aqueous extract did not have any antimicrobial activity at the tested concentration (5 mg/ml), but the methanol extract was most active on Escherichia coli. These results may support the fact that this plant is used traditionally to cure diarrhoea.     

Anti-diarrhoeal activity of aqueous extract of Ocimum kilimandscharicum

Ethnopharmacological relevance

Ocimum kilimandscharicum Baker ex Güerke, commonly referred to as Kapur Tulsi, is a medicinal herb that belongs to the family of Lamiaceae. It is traditionally popular for its gastroprotective effects, including its use as a digestive and anti-diarrhoeal.

Aim of the study

The present study aims to prove the anti-diarrhoeal activity of aqueous extract of leaves of Ocimum kilimandscharicum in animal models.

Materials and methods

The aqueous extract was tested at three different dose levels (100, 200 and 400 mg/kg, p.o. in rats and the corresponding doses in mice) against castor-oil induced diarrhoea model and castor oil induced enteropooling assay in rats; and charcoal meal test/intestinal motility test in mice. The parameters observed were the onset of defecation, cumulative faecal weight and consistency of faeces in the castor oil induced diarrhoea model; the weight of intestinal content in castor oil induced enteropooling assay; and the distance travelled by charcoal in the intestinal motility test.

Results

A significant delay in the onset of defecation (p<0.05), reduction in the cumulative faecal weight (p<0.001), along with a change in the faecal consistency from watery to solid form was observed at the dose of 200 mg/kg in the castor oil-induced diarrhoea model. Similarly, the extract at the doses of 100 mg/kg (p<0.01) and 200 mg/kg (p<0.001) significantly decreased the weight of intestinal content in castor oil induced enteropooling assay. In the charcoal meal test the extract at the dose of 280 mg/kg (corresponding to 200 mg/kg in rats) significantly (p<0.01) reduced the distance travelled by charcoal.

Conclusion

The aqueous extract of leaves of Ocimum kilimandscharicum showed anti-diarrhoeal activity, which may be due to its anti-motility and anti-secretory effects, which thus proved the traditional claims.     

Antidiarrhoeal activity of the methanolic fraction of the extract of unripe fruits of Psidium guajava Linn.

The methanolic fraction of the extract of unripe fruits of Psidium guajava was found to possess significant antidiarrhoeal activity. The fraction decreased gastric motility in an experimental animal model and inhibited acetylcholine release from isolated guinea-pig ileum. On microbial screening the fraction was found to inhibit significantly the growth of different strains of Shigella spp. and Vibrio cholerae.     

Coriander fruit exhibits gut modulatory,blood pressure lowering and diuretic activities

Aim of the study

Coriander (Coriandrum sativum) is traditionally used for various gastrointestinal and cardiovascular disorders and this study was designed to rationalize its use in dyspepsia, abdominal colic, diarrhea, hypertension and as diuretic.

Materials and methods

Coriander crude extract (Cs.Cr) was evaluated through in vitro and in vivo techniques.

Results

Cs.Cr caused atropine sensitive stimulatory effect in isolated guinea-pig ileum (0.1–10 mg/ml). In rabbit jejunum preparations, Cs.Cr evoked a similar contractile response but in the presence of atropine, it exhibited relaxation against both spontaneous and high K⁺ (80 mM)-induced contractions as well as shifted the Ca²⁺ concentration–response curves to right, similar to that caused by verapamil. Cs.Cr (1–30 mg/ml) caused fall in arterial blood pressure of anesthetized animals, partially blocked by atropine. Cs.Cr produced vasodilatation against phenylephrine and K⁺ (80 mM)-induced contractions in rabbit aorta and cardio-depressant effect in guinea-pig atria. Cs.Cr produced diuresis in rats at 1–10 mg/kg. Bio-assay-directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively.

Conclusions

These results indicate that coriander fruit exhibits gut stimulatory, inhibitory and hypotensive effects mediating possibly through cholinergic, Ca²⁺ antagonist and the combination of these mechanisms respectively. Diuretic activity adds value to its use in hypertension.     

Pharmacological study of antispasmodic activity of Mirabilis jalapa Linn flowers

INTRODUCTION: Mirabilis jalapa Linn is a well-studied plant. The indigenous people of Mexico use Mirabilis jalapa to cure many infirmities including dysentery, diarrhea, muscular pain and abdominal colic. In the present investigation, we have further characterized some pharmacological properties of an extract of Mirabilis jalapa flowers; therefore, we intend to contribute to understand the pharmacological effects and clarify the complex use of this medicinal plant. RESULTS: The extract of Mirabilis jalapa (1-1000 mug/mL) exhibits an inhibitory effect (IC(50)=18+/-0.7 micorg/mL) on gut smooth muscle contractility whereas it stimulates the contraction of rabbit aortic muscle (EC(50)=11.60+/-0.26 micorg/mL) in a concentration-dependent manner. CONCLUSIONS: These effects were not due to either ACh or HIS receptors blockage, IP(3), cAMP, cGMP, Ca(2+) release from intracellular storage, or protein kinase mediated contraction-relaxation mechanisms. The effects inducted by the Mirabilis jalapa extract may involve a serotoninergic mechanism, which, in turn, interacts with other adrenergic systems. Further studies are necessary to identify the active compounds within the extract and to elucidate the mechanism of action.     

藤茶提取物的免疫调节作用研究

目的：实验考察AGE的免疫调节作用。方法：正常的及免疫低下小鼠的碳粒廓清实验；DNCB诱导的小鼠迟发性超敏反应实验；小鼠血清溶血素抗体生成实验。结果：AGE（0．3、0．6、1．2、2．5、5g／kg）连续灌胃15天均能显著抑制正常小鼠单核-目篮细胞的吞噬功能；相反的AGE（5、10g／kg）连续灌胃7天能明显增强环磷酰胺（cyc）致免疫低下小鼠的免疫细胞吞噬功能。AGE（5、10g／kg）连续灌胃5天能明显增强DNCB诱导的小鼠迟发性超敏反应及SRBC诱导的小鼠血清溶血素抗体的生成。结论：AGE具有免疫调节作用。     

Ca++ channel blocking activity of Artemisia scoparia extract

Intravenous administration of a hydro-methanolic extract of Artemisia scoparia (3–30 mg/kg) produced hypotensive and bradycardiac effects. These effects remained unaltered in atropine treated animals and the presence of the extract did not modify the vasoconstrictor response of norepinephrine, indicating that cardiovascular effects of the plant extract are not mediated through activation of muscarinic receptors or adrenoceptor blockade. In the in vitro studies, it suppressed the spontaneous movements of rabbit jejunum in a concentration-dependent (0.1-1 mg/mL) manner. The plant extract inhibited K⁺-induced tonic contraction in a manner similar to that of verapamil. Exposure of tissue to Ca⁺⁺-free Kreb's solution abolished the spontaneous movements which were restored on addition of Ca⁺⁺. In tissue pretreated with plant extract or verapamil, addition of Ca⁺⁺ (50 μM) failed to restore spontaneous contractions. These data indicate that Artemisia scoparia cntains Ca⁺⁺ channel blocker-like constituent(s) which may explain the hypotensive effect observed in vivo and the traditional use of the plant as a spasmolytic.