Anti-ulcerogenic and anti-ulcerative colitis (UC) activities of seven amines derivatives

The Novel target compounds (CP-1-7) were synthesized and tested at doses up to 1000mg/kg for their entitled activities. They exerted promising results without any behavioral changes and mortality in mice. Therefore, according to the results obtained in our study, it could be categorized as highly safe agents for treating UC since substances possessing LD50 higher than 50mg/kg are considered nontoxic. They also possessed a potent anti-ulcerogenic activity with different potentials. The most effective compound was CP-4, it produced 97.7% ulcer protection of control followed by CP-3, which produced 90.3% protection, while the standard drug ranitidine (100mg/kg) produced 49.2% protection. Compound CP-1 showed lowest activity among the current series, it produced 55.5% protection. The target compounds were significantly more effective than the standard in reducing ulcer index. The anti-ulcerative colitis activity was tested using acetic acid induced colitis model. The curative effect of the tested compounds at a dose of 50mg/kg oral administration on rats showed a potent anti-ulcerative colitis activity with different potentials. They induced a significant decrease in ulcer score, ulcer area, ulcer index and weight/length of the colon specimens.The percent protection of control colitis ranged from 66.8% for CP-7 to 22.3% for CP-5; however the percent protection for dexamesathone (0.1. mg/kg) was 59.3%. The effect of the tested compounds CP-7 and CP-3 at dose 50. mg/kg were significantly more effective than dexamesathone (0.1. mg/kg) in reducing all parameters.Liver functions were not affected as there is no effect on the activity of both AST and ALT in animals that received the compounds, so the compounds didn't reveal hepatotoxic manifestation. Although, the results on kidney functions showed that, CP-1 slightly elevated blood urea concentration and CP-3 & CP-4 slightly elevated serum creatinine; no apparent nephrotoxic manifestations were recorded

Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4- aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & AntiUlcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50 mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds

Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity

A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 μg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging

Morphohistological and surgical anatomy of the sinus interdigitalis in Egyptian native breeds of sheep

The current study aimed to characterize the gross and microscopic structures of the interdigital sinus in Egyptian native breeds of sheep and goats (Baladi sheep and goats) to aid in conducting farther studies on such sinus and its surgical importance. The study was carried out on the distal fore and hind limb specimens (below the fetlock joint) obtained from healthy mature ten Baladi sheep and ten Baladi goats of both sexes. For sheep, thirty specimens were subjected to gross anatomical investigation and the other ten specimens were used for histological examination. While, the forty goats fore and hind feet specimens were examined grossly. The results obtained revealed the presence of a well-developed interdigital sinus in Baladi sheep, but there was no evidence for the existence of this unique structure in all examined specimens of Baladi goats. Such sinus appeared grossly as a pipe-like, composed of two parts; body (corpus) and neck (column) which opened in the skin of the interdigital area with an external orifice. The body consisted of three distinct parts in the forefeet and a single part in the hind feet. Histologically, the wall in body and neck regions of the interdigital sinus composed of three distinct layers; epidermis, dermis and a fibrous capsule. Many sebaceous glands, hair follicles and sweat glands in addition to the glandular apocrine gland were distributed within the dermis. The secretory adenomers of the interdigital sinus arranged in different lobules and lined with cuboidal cells with bleb-like projections. It reacted positively with Periodic Acid Schiff (PAS), Sudan black and Sudan III stains, on the other hand it negatively reacted with Alcian blue stain (AB)

Anatomical and radiographical studies on the venous drainage of the udder in goat with special reference to the cranial superficial epigastric vein

The present study was achieved to clarify the venous drainage of the udder in twelve healthy Egyptian Baladi goats. Gum-milk latex injection (nine specimens) and radiographic imaging technique (three specimens) were used to demonstrate the course and tributaries of the main veins draining the udder. The obtained results revealed that the udder of goat was drained through three venous circles, one at its base, while the other two were present in the form of one circle at the base of each teat. The basal venous circle was formed by the external pudendal and cranial superficial epigastric veins, as well as the dorsal labial and mammary branch of the ventral perineal vein. While the papillary venous circle was formed mainly by the cranial and caudal lateral sinus branches of the cranial mammary vein of the external pudendal vein. Also, the origin, course, distribution and termination of the cranial superficial epigastric vein were described. The venous architecture reported in this study could serve as a guide for the further surgical interference within the udder of goat

Anatomical and radiographical studies on the arterial supply of the udder in goat and their surgical importance

The present study aimed to show the arterial blood supply of the udder of the Egyptian native breed of goat (Baladi goat) to be used as a guide during mastectomy and other surgical interferences. The study was carried out on the udder of twelve apparently healthy adult female Egyptian Baladi goats. Four goats were used for mastectomy, one specimen was used for radiography and the other specimens were subjected to gum-milk latex injection to clarify the origin, course and distribution of the main arteries supplying the udder. The results revealed that the udder of goat was supplied by the external pudendal artery and dorsal labial and mammary branch of the ventral perineal artery. The course of the external pudendal artery through the inguinal canal before reaching the base of the udder, as well as that of the dorsal labial and mammary branch of the ventral perineal artery in the perineal region, were briefly described to determine the appropriate site for ligation of these vessels before mastectomy. Moreover, the arterial interconnection between the two halves of the udder was emphasized to be highlighted during unilateral mastectomy. Vascular ligation of the main blood vessels supplying the udder on the basis of the anatomical description provided less traumatic surgery and reduced the severity of the blood loss

Antitumor activity of extract and isolated compounds from Drechslera rostrata and Eurotium tonophilum

Total extracts of Drechslera rostrata and Eurotium tonophilum in addition of two isolated compounds from their cultures [di-2-ethylhexyl phthalate (H1) and 1,8-Dihydroxy-3-methoxy-6-methyl-anthraquinone (H2)] were tested for their antitumor activity using four human carcinoma cell lines. Antitumor activity was assessed by performing MTT assay to check the % cell viability. The % viability of HCT-116 (colon carcinoma), HeLa (cervical carcinoma), HEp-2 (larynx carcinoma) and HepG-2 (hepatocellular carcinoma) cells decreased after treatment with Drechslera rostrata and Eurotium tonophilum extracts, these effects were ranged from 059.0 ±  0.1 to 217.0  ±  0.3 µg/ml on all types of cancer cells. The best activity was recorded for Eurotium tonpholium extract (054.5 ± 0.3, 059.0 ± 0.5 and 059.0 ± 0.1 for HEp-2, Hela, and HepG-2 respectively). The isolated compounds (H1&H2) were found to be responsible about the activities because they recorded the lowest IC50 on tested cell lines with range of 9.5–20.3 μg/ml. Vinblastine sulphate was used as a reference standard and showed in vitro anticancer activity. This study demonstrated that all extracts and isolated compounds have antitumor activity against HCT-116, HeLa, HEp-2 and HepG-2 cells