Anti-ulcer activity

S)-a-substituted P-bromo-a-hydroxy acids (S)-4 are very important chiral synthon for medicinally important compounds, such as potential new hypoglycemia active alkylglycidic acids (ref. 1) and anti-ulcer active misoprost (ref. 2). 

Stimulation of macrophage phagoc3dosis Anti-ulcer activity... 

The most potent activities (gastric antisecretory activity in the pylorus-ligated rat or anti-ulcer activity on stress-induced gastric lesion in rat) have been observed with compounds (30), (31) [106], (32) [107], (33) and (34) [108], which were shown neither to be histamine H2 receptor inhibitors nor to act as anticholinergic agents. Thus, the activity of compound (32), for example, has been reported to be superior to that of cimetidine [107],... 

Cannahinoids are usually well tolerated, and do not produce the generalized toxic effects of conventional chemotherapies . Anti-ulcer activity. Petroleum ether extract of the dried aerial parts, administered intra-peritoneally to male rats, was active k Antiviral activity. Hot water extract of the dried fruit, in veto cell culture at a concentration of 0.5 mg/mL, was inactive on herpes simplex 1 virus, measles virus, and poliovirus... 

Anti-ulcer activity. Water extract of the dried leaf, administered intragastrically to mice, was active against aspirin-induced gastric ulcers . 

Anti-thyroid activity. Boiled rice taken orally by adults at a dose of 350 g/person was inactive on iodine uptake by the thyroid Anti-tumor activity. Bran, administered intraperitoneally to mice at a dose of 100 mg/kg, was active on Sarcoma 180 (solid). The biological activity has been patented . Fermented grains, in the ration of rats, were active. Miso, a paste made from the seeds of Oryza sativa and G lycine max (soybean), was fed ad libitum. The incidence of cancers in the miso treated rats was 20% less than controls vs 7,12-dimethylbenz-[a]anthracene -induced carcinogenesis ". Water extract of dried seed hull, administered intraperitoneally to mice, was active on Sarcoma 180 (ASC). A glycoprotein fraction has been tested. The biological activity reported has been patented . Anti-ulcer activity. A cerebroside fraction of rice bran, administered intraperitoneally to mice at a dose of 100 mg/kg, was inac-... 

Kyogoku, K. et al.. Anti-ulcer effect of isoprenyl flavonoids. II. Synthesis and anti-ulcer activity of new chalcones related to sophoradin, Chem. Pharm. Bull, 27, 2943, 1979. 

The duodenal ulcerogenic action of propionitrile and cysteamine was confirmed and extended by several authors (J, 8, 25-32). The model, especially the rapidly developing cysteamine-induced duodenal ulcer, was actually introduced in several laboratories to routinely test drugs for anti-ulcer activity (7.8,27.33). The cysteamine model, a simple, fast, and inexpensive procedure, became especially useful after a chronic form of duodenal ulcer was developed ( ) and similarities between the model and human duodenal ulceration were noted (7-10). 

Pumiacidins A, B, C, D, E, F and G (Fig. 5) were isolated by Naruse et al. in 1990 from Bacillus pumilus. Pumilacidins show no inhibitory activity against bacteria and fungi at l,000ng/ml by paper-disk assay. These compormds inhibit herpes virus typel and K -ATPase, and demonstrate anti-ulcer activity in rats ... 

For example, the 1 ",2"-(dimethylheptyl)-homologue of (-h)-(3S,4S)-A6-THC(Va) shows no activity in the monkey test up to 5 mg/kg. When tested on glaucomatic rabbits this compound is active in dilutions lower than 0.001% when administered directly into the eye in suspension. It has also a pronounced anti-ulcer activity. It is effective in the prevention and reduction of desoxycorticosterone and salt induced hypertension. 

I4°) Lippmann, W., Seethaler, K. Oral anti-ulcer activity of a synthetic prostaglandin analogue (9-Oxoprostanoic acid AY-22, 469). Experientia 29, 993 (1973). 

Yanagisawa, T., Wakabayashi, S., Tomiyama, T., Yasunami, M., and Takase, K. (1988). Synthesis and anti-ulcer activities of sodium al-... 

Plaunotol, (2, E, El-2-(4,8-Dimerhyl-3,7-nonadte-nyl)-6-methyi-2,6-octadiene-l,8-diol (E.Z.EJ-7-hydroxymethyl-3, 11,15-trimethyl-2,6,10.14-hexadecatetraen-l -ol CS-684 Kelnac. Cj H O,. mol wt 306 49. C 78.38%, H 11.18%, O 10.44%. Acyclic diterpene alcohol isolated from a Thai medicinal plant identified as Croton sublyratus Kurz, Euphorbiaceae. Isoln, synthesis and anti-ulcer activity H. Mishima et at., Japan. Kokai 77 62,213 eidem, U.S, pat. 4,059,641 (both 1977 to Senkyo) A. Ogiso et aL, Chent... 

Moreover, as compounds with oleanic structure, contained in O. europaea leaf, exert anti-ulcer activities, so they were studied for their effect on the rat gastric mucosae. 

S. Mitsui, S. Kobayashi, H. Nagohori and A. Ogiso, "Constituents from Seeds of Alpinia galanga Wild, and Their Anti-Ulcer Activities", Chem. Pharm. Bull., 1976, 24, 2377 - 2382. 

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