Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2012 Aug 3;17(8):9306-20.
doi: 10.3390/molecules17089306.

Cytoprotective effect of benzyl N'-(5-chloro-indol-3-yl-methylidene)-hydrazinecarbodithioate against ethanol-induced gastric mucosal injury in rats

Affiliations

Cytoprotective effect of benzyl N'-(5-chloro-indol-3-yl-methylidene)-hydrazinecarbodithioate against ethanol-induced gastric mucosal injury in rats

Harita Hashim et al. Molecules. .

Retraction in

Abstract

Indolic compounds have attracted a lot of attention due to their interesting biological properties. The present study was performed to evaluate the subacute toxicity and anti-ulcer activity of BClHC against ethanol-induced gastric ulcers. Experimental animal groups were orally pre-treated with different doses of BClHC (50, 100, 200 and 400 mg/kg) in 10% Tween 20 solution (vehicle). Blank and ulcer control groups were pre-treated with vehicle. The positive group was orally pretreated with 20 mg/kg omeprazole. After one hour, all groups received absolute ethanol (5 mL/kg) to generate gastric mucosal injury except the blank control group which was administered the vehicle solution. After an additional hour, all rats were sacrificed, and the ulcer areas of the gastric walls determined. Grossly, the ulcer control group exhibited severe mucosal injury, whereas pre-treatment with either derivative or omeprazole resulted in significant protection of gastric mucosal injury. Flattening of gastric mucosal folds was also observed in rats pretreated with BClHC. Histological studies of the gastric wall of ulcer control group revealed severe damage of gastric mucosa, along with edema and leucocytes infiltration of the submucosal layer compared to rats pre-treated with either BClHC or omeprazole where there were marked gastric protection along with reduction or absence of edema and leucocytes infiltration of the submucosal layer. Subacute toxicity study with a higher dose of derivative (5 g/kg) did not manifest any toxicological signs in rats. In conclusions, the present finding suggests that benzyl N'-(5-chloroindol-3-ylmethylidene)hydrazinecarbodithioate promotes ulcer protection as ascertained by the comparative decreases in ulcer areas, reduction of edema and leucocytes infiltration of the submucosal layer.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Histological sections of liver and kidney in subacute toxicity test (A) liver of rats treated with vehicle (10% Tween 20, 5 mL/kg) showing normal structural appearance; (B) kidney of rats treated with vehicle (10% Tween 20, 5 mL/kg) showing normal structural appearance; (C) Liver of rats treated with 2 g/kg of BClHC showing normal structural appearance; (D) Kidney of rats treated with 2 g/kg of BClHC showing normal structural appearance; (E) Liver of rats treated with 5 g/kg of BClHC showing normal structural appearance; (F) kidney of rats treated with 5 g/kg of BClHC showing normal structural appearance.
Figure 2
Figure 2
Gross appearance of the gastric mucosa in rat, (A) pre-treated with vehicle 0.2 mL of 10% Tween 20 (ulcer control). Severe injuries are seen in the gastric mucosa (arrow).Absolute ethanol produced extensive visible hemorrhagic necrosis of gastric mucosa; (B) Rats pre-treated with omeprazole (20 mg/Kg). Injuries to the gastric mucosa are milder (arrow) compared to the injuries seen in the ulcer control rats; (C) Rats pre-treated with BClHC (100 mg/Kg). Mild injuries to the gastric mucosa can be seen showing the beginning of gastric mucosa flattening; (D) Rats pre-treated with BClHC (200 mg/Kg). Very mild injuries to the gastric mucosa can be seen, showing the flattening of gastric mucosa, (E) Rats pre-treated with BClHC alone (400 mg/Kg). No injuries to the gastric mucosa are seen, but the flattening of gastric mucosa can been seen.
Figure 3
Figure 3
Histological sections of the ethanol-induced gastric mucosal damage in rats (H&E stain 10×). (A) Rats pre-treated with 5 mL/Kg of 10% Tween 20 solution (ulcer control). There is severe disruption to the surface epithelium, and edema of the submucosal layer with leucocytes infiltration. (B) Rats pre-treated with 20 mg/kg of omeprazole. There is mild disruption to the surface epithelium with no edema and no leucocytes infiltration of the submucosal layer. (C) Rats pre-treated with 200 mg/kg of BClHC. There is very mild disruption to the surface epithelium with no edema and no leucocytes infiltration of the submucosal layer. (D) Rats pre-treated with 400 mg/kg of BClHC. There is no disruption to the surface epithelium with the absence of edema and leucocytes infiltration of the submucosal layer.
Figure 4
Figure 4
The effect of BClHC on gastric tissue glycoprotein-PAS staining in ethanol-induced gastric ulcer in rats(PAS stain 20×). (A) Normal control group; (B) Ulcer control group; (C) BClHC-treated group with 50 mg/kg; (D) BClHC-treated group with 400 mg/kg.
Figure 5
Figure 5
Benzyl N'-(5-chloroindol-3-ylmethylidene)hydrazinecarbodithioate.

References

    1. Gurkok G., Coban T., Suzen S. Melatonin analogue new indole hydrazide/hydrazone derivatives with antioxidant behavior: Synthesis and structure-activity relationships. J. Enz. Inhib. Med. Chem. 2009;24:506–515. doi: 10.1080/14756360802218516. - DOI - PubMed
    1. Ates-Alagoz Z., Kus C., Coban T. Synthesis and antioxidant properties of novel benzimidazoles containing substituted indole or 1,1,4,4-tetramethyl-1,2,3,4-tetrahydro-naphthalene fragments. J. Enz. Inhib. Med. Chem. 2005;20:325–331. doi: 10.1080/14756360500131706. - DOI - PubMed
    1. Singh P., Kaur M., Verma P. Design, synthesis and anticancer activities of hybrids of indole and barbituric acids-Identification of highly promising leads. Bioorg. Med. Chem. Lett. 2009;19:3054–3058. doi: 10.1016/j.bmcl.2009.04.014. - DOI - PubMed
    1. Wang J.J., Shen Y.K., Hu W.P., Hsieh M.C., Lin F.L., Hsu M.K., Hsu M.H. Design, synthesis, and biological evaluation of pyrrolo[2,1-c[1,4]benzodiazepine and indole conjugates as anticancer agents. J. Med. Chem. 2006;49:1442–1449. doi: 10.1021/jm050956q. - DOI - PubMed
    1. Chen J.J., Wei Y., Drach J.C., Townsend L.B. Synthesis and antiviral evaluation of trisubstituted indole N-nucleosides as analogues of 2,5,6-trichloro-1-(beta-D ribofuranosyl)benzimidazole (TCRB) J. Med. Chem. 2000;43:2449–2456. doi: 10.1021/jm990320x. - DOI - PubMed

Publication types

MeSH terms

LinkOut - more resources