Influence of rhein anthrone and rhein on small intestine transit rate in rats: evidence of prostaglandin mediation

Nijs, Greg; Witte, Peter de; Geboes, Karel; Lemli, J

doi:10.1016/0014-2999(92)90169-5

Cited by 20 publications

(12 citation statements)

References 27 publications

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“…15,16) The mechanism involves the sennosides and their active derivatives acting on the intestinal mucosal epithelium and submucosal nerve bundles, thereby stimulating prostaglandin (PG) synthesis and endogenous acetylcholine release, and consequently enhancing the colonic smooth muscle contraction. [17][18][19] Unfortunately, the purgative activities of anthraquinoids (including senna) are too powerful for them to be regularly used, and even periodic use of these laxatives can induce pseudomelanosis coli, a risk factor for colorectal neoplasma. 3) Indeed, in the present study, the senna extract at 300 and 1000 mg/kg, p.o., had a strong laxative effect, and it induced severe diarrhea at the same doses as those Segments of the rabbit ileum were suspended at 1 g tension in an organ bath containing Tyrode's solution.…”

Section: Discussionmentioning

confidence: 99%

“…In the 1 H-NMR spectrum, the presence of a para-substituted benzene ring was shown by proton signals 6.81 (1H, d, J ¼ 8:6 Hz) and 7.61 (1H, d, J ¼ 8:6 Hz), in addition to a meta-substituted benzene ring due to two doublets at 6.07 (1H, d, J ¼ 2:0 Hz) and 6.30 (1H, d, J ¼ 2:0 Hz). The HMBC and COSY spectra allowed complete assignment and identification of the aglycone as 4, 2 0 , 4 0 , 6 0 -tetrahydroxybenzophenone (iriflophenone) (18,19). The usual acidhydrolysis of compound 2 gave iriflophenone.…”

Section: Laxative Effect Of Sennamentioning

confidence: 99%

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Laxative Effect of Agarwood Leaves and Its Mechanism

Hara

Ise

Morimoto

et al. 2008

Bioscience, Biotechnology, and Biochemistry

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We investigated the laxative activity of an extract of agarwood leaves from Aquilaria sinensis. The laxative activity was measured in mice by counting the stool frequency and stool weight, and the drugs were orally administered. An acetone extract of agarwood leaves and senna (a representative laxative drug) both increased the stool frequency and weight, but a methanol extract did not. The laxative effect of the acetone extract was milder than that of the anthraquinoid laxative, senna, and the former did not induce diarrhea as a severe side effect. We identified the main constituent contributing to the laxative effect of the acetone extract as genkwanin 5-O--primeveroside (compound 4). Compound 4 strengthened the spontaneous motility and induced contraction in the ileum. This ileal contraction induced by compound 4 was inhibited by atropine, but not by azasetron, suggesting that the effect of compound 4 was mediated by acetylcholine receptors, and not by serotonin. The laxative mechanism for compound 4 may in part involve stimulation of intestinal motility via acetylcholine receptors.

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Section: Discussionmentioning

confidence: 99%

Section: Laxative Effect Of Sennamentioning

confidence: 99%

Laxative Effect of Agarwood Leaves and Its Mechanism

Hara

Ise

Morimoto

et al. 2008

Bioscience, Biotechnology, and Biochemistry

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“…50 Therefore, diarrhea score test was carried out to investigate the effect of the prepared formulae in minimizing diarrhea.…”

Section: Diarrhea Score Testmentioning

confidence: 99%

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Allam¹,

Hamdallah²,

Abdallah³

2017

IJN

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Nanodrug delivery systems have been widely reviewed for their use in several drug formulations to improve bioavailability, sustain effect, and decrease side effects of many candidate drugs. The objective of this study was to evaluate the potential of chitosan (CS)-coated nanosuspensions to enhance bioavailability and reduce the diarrheal side effect of diacerein (DCN) after oral administration. DCN nanosuspensions (DNS) were prepared by sonoprecipitation technique using different stabilizers at three different concentrations. The selected DNS with optimum particle size (PS), polydispersity index (PDI), and Zeta potential (ZP) was coated with three different concentrations of CS-coated DNS (CS-DNS) and screened. In vitro dissolution was performed for the selected lyophilized formulae and compared with DCN powder in addition to the assessment of drug crystallinity via scanning electron microscopy, X-ray powder diffraction, and differential scanning calorimetry. Ex vivo drug permeability using noneverted rat intestine, intraluminal content, and mucoadhesion evaluation was studied for nominated formulae in comparison to DCN suspension. Moreover, in vivo study, pharmacokinetic parameters, and evaluation of diarrheal potential were conducted after oral administration of selected formulae. Polyvinyl pyrrolidone (PVP)-stabilized DNS showed a significant increase ( P ≤0.05) in PS and PDI as the stabilizer concentration increased. PVP-stabilized DNS with the lowest CS concentration was protected from aggregation by lyophilization with mannitol. A remarked enhancement in dissolution parameters was observed in the nanocrystals’ formulae. Morphological examination and X-ray diffraction confirmed drug crystallinity. The intermediate permeation parameters of CS-DNS-F10, lowest rhein-to-DCN ratio in intraluminal content along with the highest percentage of mucoadhesive, could serve as a sustaining profile of coated formula. CS-DNS-F10 showed a significantly higher C max of 0.74±0.15 µg/mL at a delayed T max of 3.60±0.55 hours with a relative bioavailability of 172.1% compared to DCN suspension. CS-coated nanosuspensions could serve as promising revenue to enhance bioavailability and reduce the diarrheal side effect of DCN after oral administration.

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“…Prostaglandins could act as mediators of this increase in proliferative activity, as they are released by monocytes and macrophages in response to epithelial damage. Anthranoid laxatives have indeed been described to increase the production of prostaglandin E 2 [26]. Prostaglandin E 2 has a trophic effect on the mucosa of the stomach as well as the small bowel [27]and has been implied to promote development and proliferation of carcinoma in methyl-nitro-nitroso-guanidine(MNNG)-induced large bowel carcinogenesis in rats [28].…”

Section: Discussionmentioning

confidence: 99%

Influence of a Highly Purified Senna Extract on Colonic Epithelium

Gorkom¹,

Karrenbeld

Sluis³

et al. 2000

Digestion

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Background: Chronic use of sennoside laxatives often causes pseudomelanosis coli. A recent study suggested that pseudomelanosis coli is associated with an increased colorectal cancer risk. A single high dose of highly purified senna extract increased proliferation rate and reduced crypt length in the sigmoid colon compared to historical controls. Aims: To evaluate in a controlled study the effects of highly purified senna extract on cell proliferation and crypt length in the entire colon and on p53 and bcl-2 expression. Methods: Addition of a senna extract to colonic lavage was studied in 184 consecutive outpatients. From 32 randomised patients, 15 with sennosides (Sen), 17 without (NSen), biopsies were taken. Proliferative activity was studied in 4 areas of the colon, using 5-bromo-2′-deoxyuridine labelling and immunohistochemistry (labelling index, LI). Expression of p53 and bcl-2 in the sigmoid colon was determined immunohistochemically. Results: Crypts were shorter in Sen than in NSen in the transverse and sigmoid colon. LI was higher in Sen than in NSen in the entire colon. No difference in p53 expression was seen. Bcl-2 expression was higher in both groups when crypts were shorter and/or proliferation was increased. Conclusion: Sennosides induce acute massive cell loss probably by apoptosis, causing shorter crypts, and increased cell proliferation and inhibition of apoptosis to restore cellularity. These effects may reflect the mechanism for the suggested cancer-promoting effect of chronic sennoside use.

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Influence of rhein anthrone and rhein on small intestine transit rate in rats: evidence of prostaglandin mediation

Cited by 20 publications

References 27 publications

Laxative Effect of Agarwood Leaves and Its Mechanism

Laxative Effect of Agarwood Leaves and Its Mechanism

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Influence of a Highly Purified Senna Extract on Colonic Epithelium

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