Effect of an aqueous extract of dried immature fruit of Poncirus trifoliata (L.) Raf. on intestinal transit in rodents with experimental gastrointestinal motility dysfunctions

Lee, Hyun Tai; Seo, Eun Kyoung; Chung, Suk Jae; Shim, Chang-Su

doi:10.1016/j.jep.2005.08.015

Cited by 40 publications

(30 citation statements)

References 13 publications

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“…The prokinetic effect of PF-W has already been known in both humans and rodents and even in GMD rats [1,2]. Although the prokinetic activity was evident, the underlying molecular mechanism of this activity was uncertain until the involvement of serotonin receptor subtype 4 (5-HT4R) was reported [19].…”

Section: Discussionmentioning

confidence: 99%

“…Indeed, many studies have proved that PF-W enhances gastrointestinal motor function by accelerating the transit of intestinal contents without leading to gastric emptying in human subjects and rodents [1]. It also improved the intestinal transit rate (ITR) in rodents with experimental digestive dysfunctions [2]. Recently, it was revealed that naringin, a chemical component in PF-W, can cause the activation of ghrelin receptor in vitro [3].…”

Section: Introductionmentioning

confidence: 99%

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Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

2013

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Background and Purpose: Poncirus fructus (PF), also known as the dried immature fruit of Poncirus trifoliata (L.) Raf., has long been used as a cure for the treatment of various gastrointestinal disorders in eastern Asia. Recently, it was reported that naringin, a flavonoid constituent of the PF extract, causes the activation of ghrelin receptor in vitro. Although the ghrelin receptor is involved in the enhancement of intestinal motility, there are no studies as yet involving in vivo action of naringin. Therefore, the purpose of the present study is to investigate whether naringin exhibits a prokinetic effect in vivo. Methods: We measured the intestinal transit rate in rats with gastrointestinal motility dysfunction (GMD) and performed a pharmacokinetic analysis of naringin to investigate the effect of naringin on prokinetic activity in vivo. Results: The results of this study show that the aqueous extract of PF and its constituent naringin have a strong prokinetic activity in GMD rats via activation of the ghrelin receptor. Surprisingly, pharmacokinetic analysis revealed that naringin has low bioavailability (11%), implying that the prokinetic effect of naringin was largely due to the local activation of ghrelin receptor in the intestine rather than a systemic effect after absorption. Indeed, it turned out that intravenous administration of naringin led to a lower prokinetic effect than when administrated orally to rats, indicating that naringin prefers to act on the intestinal wall rather than getting absorbed into the systemic circuit. This local mode of action might be advantageous for preventing possible systemic side effects since naringin is not well absorbed into the system circuit. Conclusions: Naringin exhibits an in vivo prokinetic activity by a preferable local activation of ghrelin receptor. Moreover, we propose that naringin could play a role as a leading compound for the development of ghrelin receptor-based prokinetic agents.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

2013

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“…fruits (ZF), both of which have been used in Asian traditional medicine for the treatment of gastrointestinal disorders. PF has been used as a traditional medicine for the treatment of abnormal gastrointestinal motility and gastric (18)(19)(20). ZF, which belongs to the Rutaceae family, has been used as a traditional medicine to alleviate stomach pain, diarrhea, and jaundice (21,22).…”

Section: Introductionmentioning

confidence: 99%

Prokinetic effects of LD02GIFRO on functional gastrointestinal disorder in rats

Choi

Zheng

Park³

et al. 2017

Experimental and Therapeutic Medicine

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Abstract. LD02GIFRO is a novel prokinetic agent formulated with Poncirus fructus and Zanthoxylum sp. fruits. The aim of the present study was to evaluate the effect of LD02GIFRO on delayed gastrointestinal transit (GIT) and colorectal hypersensitivity. To investigate the effect of LD02GIFRO, a rat model of delayed GIT was induced via three mechanisms; postoperative ileus (POI), morphine, and POI plus morphine. Visceromotor responses (VMR) to colorectal distension (CRD) were also evaluated. POI was induced by laparotomy surgery and manipulation of the small intestine under anesthesia, and GIT was calculated by measuring the length that Evans Blue travelled through the gastrointestinal tract in a given time. Oral administration of 260 mg/kg LD02GIFRO caused Evans Blue to migrate significantly further in the delayed GIT models induced by POI, morphine and POI plus morphine compared with the control (P<0.05). This effect was inhibited by atropine, a muscarinic receptor antagonist, and completely abolished by GR125487, a 5-HT 4 -receptor antagonist. Furthermore, intraperitoneal administration of 600 and 900 mg/kg LD02GIFRO significantly reduced VMR to CRD in acute and chronic colorectal hypersensitive rat models, induced by acetic acid and trinitrobenzenesulfonic acid, to almost normal levels (P<0.01). In the present study, LD02GIFRO successfully ameliorated delayed GIT models and colorectal hypersensitivity models, suggesting that LD02GIFRO may be an effective therapeutic treatment for patients with functional gastrointestinal disorders and abnormalities in GIT.

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“…The main active components of trifoliate orange are flavonoids, hesperidin, neohesperidin, naringin, and cumalin (Park and Chun, 1969;Oh et al, 1989;Chung et al, 2004). The main biological functions of trifoliate orange are involvement in immune function and lipid lowering (Patkar et al, 1979;Fewtrell et al, 1982;Sagi-Eisenberg et al, 1985;Kanemoto et al, 1993;Lee et al, 1996;Lee et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Effects of Trifoliate Orange (Poncirus trifoliata) Extract on Inflammatory Responses in LPS-induced Shock Rats and RAW 264.7 Cells

Lee¹

2016

Korean Journal of Plant Resources

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-This study examined the effects of trifoliate orange extract (TOE) on inflammatory reactions at the time of an LPS shock by performing experiments on rats injected with trifoliate orange extract and in Raw 264.7 cell cultures, with the aim of developing a new anti-inflammatory medicine. The IL-1β, IL-6, and TNF-α concentrations were lower in all of the groups treated with TOE than in the control group after 5 h of LPS treatment. The IL-10 concentration was higher in the 300-㎎/㎏ TOE group than in the control group after 2 h and 5 h of LPS treatment. The liver concentrations of cytokines IL-1β and IL-6 decreased more in the groups treated with TOE than in the control group and the IL-6 concentration did not differ significantly between the 100-㎎/㎏ TOE group than in the control group. The TNF-α and IL-10 concentrations did not differ significantly between the TOE groups and the control group. In the experiments involving Raw 264.7 macrophage cultures subjected to LPS shock, the productions of IL-1β, IL-6, and TNF-α decreased in all of the groups treated with TOE compared to the control group. The IL-10 concentration did not differ significantly between the groups treated with TOE and the control group. Together the findings of this study suggest that TOE contains functional substances that can influence inflammatory reactions.

show abstract

Effect of an aqueous extract of dried immature fruit of Poncirus trifoliata (L.) Raf. on intestinal transit in rodents with experimental gastrointestinal motility dysfunctions

Cited by 40 publications

References 13 publications

Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

Prokinetic effects of LD02GIFRO on functional gastrointestinal disorder in rats

Effects of Trifoliate Orange (Poncirus trifoliata) Extract on Inflammatory Responses in LPS-induced Shock Rats and RAW 264.7 Cells

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