Intestinal spasmolytic effects of STW 5 (Iberogast®) and its components

Heinle, H.; Hagelauer, D.; Pascht, U.; Kelber, O; Weiser, D

doi:10.1016/j.phymed.2006.03.013

Cited by 43 publications

(28 citation statements)

References 23 publications

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“…Generally, these results are in agreement with other studies, suggesting a relaxant effect of isolated furanocoumarins and plant extracts rich in these compounds on smooth muscle (He et al, 2007;Heinle et al, 2006;Zhang et al, 2010). However, previous studies typically focused on the myorelaxant effect of furanocoumarins on vascular smooth muscle (Chiu et al, 2001;He et al, 2007;Thastrup et al, 1983), and only very few analyzed their impact on gastrointestinal (GI) smooth muscle (Abbaskhan et al, 2012;Heinle et al, 2006;Schemann et al, 2006).…”

Section: Discussionsupporting

confidence: 90%

“…The effect of bergapten on the amplitude of spontaneous motor activity is, however, not very surprising. A similar impact was observed in case of the extract of celandine, Iberis amara L. (Brassicaceae) (Heinle et al, 2006;Schemann et al, 2006). Increasing the force of the spontaneous contraction is a desirable effect for a phytoconstituent regarding the paralytic behavior of the intestine found in irritable bowel syndrome and for antral hypomotility in functional dyspepsia (Tack et al, 1998).…”

Section: Discussionmentioning

confidence: 53%

“…However, previous studies typically focused on the myorelaxant effect of furanocoumarins on vascular smooth muscle (Chiu et al, 2001;He et al, 2007;Thastrup et al, 1983), and only very few analyzed their impact on gastrointestinal (GI) smooth muscle (Abbaskhan et al, 2012;Heinle et al, 2006;Schemann et al, 2006). According to these data, it can be postulated that bergapten contributes to the spasmolytic effect of A. archangelica extract and the phytomedicine STW 5 mentioned previously (Heinle et al, 2006;Schemann et al, 2006). However, it is surprising that in contrast to furanocoumarins of the psoralen type (e.g., imperatorin, xanthotoxin) bergapten caused a contractile response of the rat isolated jejunum strips when administered at high concentrations (10 and 50 mM).…”

Section: Discussionmentioning

confidence: 99%

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Isolation and evaluation of the myorelaxant effect of bergapten on isolated rat jejunum

Skalicka-Woźniak

Mendel

Chłopecka

et al. 2015

Pharmaceutical Biology

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Context: Plants of the genus Heracleum L. (Apiaceae) have a long history of being used in traditional medicines for the treatment of alimentary tract disorders, and these biological effects have been ascribed to the presence of furanocoumarins (including bergapten). Objectives: This study aimed to develop an efficient, preparative, counter-current chromatographic separation of bergapten in order to characterize its spasmolytic activity in isolated rat jejunum strips. Materials and methods: Successful separation of the dichloromethane extract of the fruits of Heracleum leskovii Grossh. was achieved by high-performance countercurrent chromatography (HPCCC) using a two-phase solvent system composed of n-heptane/EtOAc/MeOH/H 2 O (6:5:6:5, v/v/v/v). The pharmacological assessment of bergapten (0.0001-50 mM) on jejunum smooth muscle strips isolated from rats was conducted under isotonic conditions, following up to three hours of incubation. Results: The separation method was scaled up six-fold from analytical to semi-preparative conditions, affording bergapten of 499% purity in less than 30 min. This permitted bergapten to be available in quantity for spasmolytic tests on isolated jejunum strips from rats. Bergapten caused myorelaxation of the intestine preparations in the concentration range of 0.0001-1 mM. At higher doses, bergapten caused either relaxation or contraction of the smooth muscle. Discussion and conclusion: Bergapten was successfully isolated by rapid HPCCC and its spasmolytic activity was confirmed, thereby providing a preliminary evidence base for the traditional medicine application. The data suggest that bergapten causes no irreversible changes to intestinal tissue.

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Section: Discussionsupporting

confidence: 90%

Section: Discussionmentioning

confidence: 53%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Isolation and evaluation of the myorelaxant effect of bergapten on isolated rat jejunum

Skalicka-Woźniak

Mendel

Chłopecka

et al. 2015

Pharmaceutical Biology

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“…16,[20][21][22][23][24] The current study has demonstrated that Iberogast ® improved histological parameters including a reduced jejunal ODS score and improved villus and crypt structure in the jejunum during 5-FU induced mucositis; however, Iberogast ® did not improve sucrase activity as indicated by the SBT and the sucrase assay.…”

Section: Discussionmentioning

confidence: 50%

“…[16][17][18][19] Iberogast ® is a herbal formula comprised of nine different extracts including Iberus amara (bitter candy tuft) (15%), Angelica archangelica (angelica root) (10%), Matricaria recutita (chamomile) (20%), Carum carvi (caraway) (10%), Silybum marianum (St. Mary's thistle) (10%), Melissa officinalis (lemon balm leaf ) (10%), Mentha piperita (peppermint leaf ) (5%), Chelidonium majus (celadine herb) (10%) and Glycyrrhiza glabra (liquorice root) (10%). 16 Iberogast ® has been clinically prescribed to treat gastrointestinal disorders such as functional dyspepsia (FD) for more than 40 years 16,[20][21][22][23][24] and has indicated promise in alleviating the symptoms of irritable bowel syndrome (IBS), markedly modulating gastrointestinal motor and sensory function. 21 Therefore, the aim of the current study was to investigate whether Iberogast ® could reduce small intestinal damage in a 5-FU model of mucositis in Dark Agouti rats.…”

Section: Introductionmentioning

confidence: 99%

The herbal extract Iberogast® improves jejunal integrity in rats with 5-Fluorouracil (5-FU)-induced mucositis

Wright¹,

Yazbeck²,

Lymn³

et al. 2009

Cancer Biology & Therapy

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There is an acute need for the development of effective therapies for mucositis, a debilitating side effect of cancer chemotherapy. Iberogast ® is a herbal extract reported to possess anti-inflammatory properties. We investigated Iberogast ® for its potential to reduce the severity of 5-Fluorouracil (FU)-induced mucositis in rats. Rats were allocated to three treatment groups (n = 8) and gavaged daily with a 10% solution of Iberogast ® or water from day 0 to day 8. Rats were injected intraperitoneally with 5-FU (150 mg/kg) or saline on day 6, and killed after 72 h. In vivo and in vitro sucrase activity was assessed by 13 C-sucrose breath test (SBT) and sucrase assay respectively. Intestinal disease severity was determined by histological assessment of villus height and crypt depth. Significant increases in villus height (277 ± 9 μm) and crypt depth (67 ± 3 μm) were observed in 5-FU + Iberogast ® -treated rats compared with 5-FU + Water (224 ± 13 μm and 48 ± 2 μm respectively; p < 0.05). Sucrase activity was significantly reduced in all 5-FU groups compared to control. Significant reductions in SBT and sucrase activity were observed in all 5-FU groups compared with Saline + Water controls (p < 0.05). We conclude that although Iberogast ® partially improved the histopathological features of 5-FU induced mucositis, it conferred no significant protection as indicated by the assessed endpoints.

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Mechanism‐based inactivation of cytochrome P450 2D6 by chelidonine

Liu

Cui

Peng

et al. 2018

J Biochem & Molecular Tox

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Chelidonine (CHE) is a major bioactive constituent of greater celandine, a plant used in traditional herbal medicines. CHE has widely been used as an analgesic in clinical settings. We evaluated the inhibitory effects of CHE on human cytochrome P450 enzymes. CHE produced time-, concentration-, and NADPH-dependent inhibition of CYP2D6, with K I and k inact values of 20.49 μM and 11.05 min −1 , respectively.Approximately 76% of CYP2D6 activity was suppressed after 9 minute incubation with CHE (50 μM). The loss of enzyme activity was not restored following dialysis.The estimated partition ratio of the inactivation was about 156. Quinidine, a competitive inhibitor of CYP2D6, attenuated the CHE-mediated enzyme inactivation, while glutathione and catalase/superoxide dismutase did not markedly ameliorate the inhibitory effect. Upon oxidation using potassium ferricyanide, the 15.1% activity of CYP2D6 was restored. These findings indicate that CHE acted as a mechanism-based inactivator of CYP2D6 and the observed effects may induce potential drug-drug interactions. K E Y W O R D Scytochrome P450 enzymes (CYP), mechanism-based inactivation, metabolic activation

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Intestinal spasmolytic effects of STW 5 (Iberogast®) and its components

Cited by 43 publications

References 23 publications

Isolation and evaluation of the myorelaxant effect of bergapten on isolated rat jejunum

Isolation and evaluation of the myorelaxant effect of bergapten on isolated rat jejunum

The herbal extract Iberogast® improves jejunal integrity in rats with 5-Fluorouracil (5-FU)-induced mucositis

Mechanism‐based inactivation of cytochrome P450 2D6 by chelidonine

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