Inhibitors of gastric acid secretion

Bays, D. E.; Finch, Harry

doi:10.1039/np9900700409

Cited by 12 publications

(8 citation statements)

References 174 publications

(73 reference statements)

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“…The current medical treatment for peptic ulcers is generally based on proton pump inhibitors and histamine H 2 -receptor blockers (Jain et al, 2007). However, the long-term use of these therapeutic agents can produce adverse effects, such as hypergastrinemia and hyperplasia in the enterochromaffinlike (ECL) cells, the risk of pneumonia, diarrhea and the disturbance of human gastrointestinal microflora (Orlando, Lenard, Orlando, 2007;Bays, Finch, 1990;Devault, Talley, 2009;Ksiadzyna, Szelag, Paradowski, 2015). Therefore, the search for safer and more effective alternatives to treat F. Sobreira, L. S. Hernandes, A. Vetore-Neto, I. E. C. Díaz, F. C. Santana, J. Mancini-Filho, E. M. Bacchi Braz.…”

Section: Introductionmentioning

confidence: 99%

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Sobreira

Hernandes

Vetore-Neto

et al. 2017

Braz. J. Pharm. Sci.

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Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE 50 =41.91 µg/mL) by DPPH in comparison with Trolox ® and 11.33 mmol Trolox ® equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.Uniterms: Gastric ulcer/study/rats. Gastric ulcer/treatment. Kalanchoe pinnata/chromatographic profile. Kalanchoe pinnata/gastroprotective activity. Quercetrin. Quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside. INTRODUCTIONFor the past two centuries, peptic ulcers have caused high morbidity and mortality (Malfertheiner, Chan, Mccoll, 2009). This disease is a serious and prevalent pathology (Calam, Baron, 2001). A peptic ulcer is a chronic lesion, usually single, that can be located in the gastric or duodenal mucosae (Kumar, Abbas, Fausto, 2005). In the UK, the incidence of this disease was 12% higher in men than in women (Araujo, Borini, Guimarães, 2014). A review article (January 1980 to February 2009 showed that the incidence rate of uncomplicated peptic ulcers was approximately one case per 1000 people per year in the general population; the incidence rate for complicated peptic ulcers that included bleeding and perforation was approximately 0.7 cases per 1000 people per year (Lin, Rodrígues, Hernándes-Diaz, 2011).The pathophysiology of peptic ulcers suggests that this disease is caused by an imbalance between defensive factors (mucus and bicarbonate secretion, mucosal barrier, blood flow, and prostaglandins) and destructive factors (reactive oxygen species and acid and pepsin secretion), resulting in the acute inflammation of the gastrointestinal mucosae (Laine, Takeuchi, Tarnawski, 2008). Several stimuli serve as offensive factors, including Helicobacter pylori, the use of nonsteroidal anti-inflammatory drugs (NSAIDs), stress, alcohol and cigarette smoking (Malfertheiner, Chan, Mccoll, 2009;Malnick et al., 2014). The current medical treatment for peptic ulcers is generally based on proton pump inhibitors and histamine H 2 -receptor blockers (Jain et al., 2007). However, the long-term use of these therapeutic agents can produce adverse effects, such as hypergastrinemia and hyperplasia in the enterochromaffinlike (ECL) cells, the risk of pneumonia, diarrhea and the disturbance of ...

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Section: Introductionmentioning

confidence: 99%

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Sobreira

Hernandes

Vetore-Neto

et al. 2017

Braz. J. Pharm. Sci.

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“…Our results clearly indicate that a single dosage of 2 mg/ Kg IV omeprazole inhibits gastric acid secretion for 24 hours. After absorption, omeprazole is transferred from the plasma to the acid secretory canaliculi of parietal cells (Holt and Howden, 1991) and covalently binds to H+, K+ ATPase (Bays and Finch, 1990), so the anti-secretory effect of omeprazole on parietal cells persist long after plasma concentrations have decreased (Holt and Howden, 1991).…”

Section: Discussionmentioning

confidence: 99%

Effects of two intravenous dose levels of omeprazole on the gastric juice pH of healthy horses

Ruiz

Ramírez²,

Lezcano³

2016

Rev Colomb Cienc Pecu

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Efecto de dos niveles de dosis intravenosas de omeprazol sobre el pH del jugo gástrico de caballos sanos Efeito de dois níveis de doses intravenosas de omeprazol no suco gástrico pH cavalos saudáveisJhon D Ruiz * , MV, MSc, PhD; Juan E Ramírez, MVZ; Ángel Lezcano MVZ. Zootecnia, Universidad CES. Medellin, Colombia. (Received: March 29, 2015; accepted: June 8, 2016) doi: 10.17533/udea.rccp.v29n4a05 Summary Background: omeprazole suppresses gastric acid secretion and increases gastric juice pH by blocking the H+, K+ ATPase in the secretory membrane of parietal cells. Gastric juice pH below 4, long periods of no feed intake and stress are factors predisposing to gastric ulcers in horses. Objective: to determine the effect of 1 and 2 mg/Kg intravenous (IV) omeprazole on the gastric juice pH of Colombian Creole horses. Methods: seven horses were treated with two IV levels of omeprazole (1, and 2 mg/Kg body weight (BW)) in a crossover design. The omeprazole dose for each animal was reconstituted with 100 ml 0.9% NaCl. Gastric pH was measured using a portable pH-meter in stomach samples collected at time 0 (just before treatment), and 1, 2, 3, 5, 7, 9, 11, and 24 hours post-treatment. Results: the gastric pH at time 0 fluctuated from 1.6 to 3.2 in all horses. Both omeprazole doses (1 and 2 mg/Kg) significantly increased the gastric pH (pH>4.6) from 1 to 11 hours after the treatment. At 24 hours post-treatment, pH of the group treated with 1.0 mg/Kg significantly decreased to 2.8 ± 0.3, but remained elevated at 5.7 ± 0.87 for the group treated with 2 mg/Kg. Conclusion: the study demonstrated that a single IV omeprazole dose of 2 mg/Kg, but not 1 mg/Kg, maintained gastric pH above 4 during 24 hours. Grupo de Investigación en Ciencias (INCA-CES). Facultad de Medicina Veterinaria y

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“…OH ~ H o CHa (11): R=H (12): R=CON~ In addition to these last two compounds (90,92) other streptothricinlike antibiotics isolated from Streptomyces are: glycinothricin (15), which is the deformimino derivative of LL-AB664 (93), N-methylstreptothricin F (16) (94), albothricin (17), which is the 4-desoxy analog of streptothricin (95), two inseparable isomers, A-269A (18) and A-269A' (19), which differ from streptothricin in the amino acid substituent on cx-D-gulose and from each other in the position of carbamate function (96), and finally, a series of Nil-ace tyla ted derivatives of streptothricins E, D and F, named AN-201 1(20), and , from Streptomyces nojiriensis (97). All these compounds were isolated from Streptomycetes and have a trans junction between the 2-aminoimidazolyl and the o-lactam rings.…”

Section: ~)mentioning

confidence: 99%

“…More recently, MORI (8,9) has discussed many aspects of natural guanidine derivatives, CHEVOLOT (10) has focused on guanidine secondary metabolites isolated from marine organisms, and MARESCAU (11) and also ROBIN and MARESCAU (12) have discussed the biological role of both primary and secondary guanidine metabolites. Guanidines of synthetic origin have presented much interest as drugs (13, 13a), mainly as antihistamines (14,15), as antihypertensives (16) and as potent sweeteners (17). Apart from their academic interest, some of these compounds have direct implications in public health (for example the well-known tetrodotoxin and saxitoxin), in agriculture (blasticidin Sand peramine), and in medicinal chemistry (the bleomycins and the argiopin-like spider toxins are some examples).…”

Section: Introductionmentioning

confidence: 99%

Some Aspects of Guanidine Secondary Metabolites

Berlinck

1995

Fortschritte Der Chemie Organischer Naturstoffe / Progress in the Chemistry of Organic Natural Products

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Inhibitors of gastric acid secretion

Cited by 12 publications

References 174 publications

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

Effects of two intravenous dose levels of omeprazole on the gastric juice pH of healthy horses

Some Aspects of Guanidine Secondary Metabolites

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