Ulcerogenic activity

OS 122 Okuyama, E., and M. Yamazaki. The principles of Tetragonia tetragonoid.es having anti-ulcerogenic activity. LI. Isolation and structure of cerebro-sides. Chem Pharm Bull 1983 31(7) 2209-2219. 

A new class of compounds is reported to have dual inhibitory properties. They have a y-sultam skeleton and show potent inhibitory effects towards both COX-2 and 5-lipoxygenase as well as production of IL-1 in in vitro assays. These compounds have also proved to be effective in several animal arthritic models without any ulcerogenic activity. Among these compounds S-2474 ((E)-(5)-(3,5-di-fe/t.-butyl-4-hydroxy-benzylidene)-2-ethyl-1,2-isothiazolidine-1,1-dioxide) was selected as an anti-arthritic drug candidate and is now under clinical investigations (Inagaki et al., 2000). 

Wallace et al. (1989) studied the ulcerogenic activity of endothelin in indomethacin pre-treated rats using an ex vivo gastric chamber. 

Rainsford (1987) published an assay for gastro-ulcerogenic activity of non-steroidal anti-inflammatory drugs in cholinomimetic-treated mice using visual image analysis. 

H)-Oxazolone derivatives, (V), prepared by Duran (5) were selective as COX-II inhibitors and used in treating inflammation, pain, fever, and asthma without ulcerogenic activity. 

Carrageenan Oedema PBQ -mduced algesia Yeast-induced pyrexia Acute toxicity in mice (LD,q) Ulcerogenic activity in rats (UDjo... 

The specific risks of salt and water retention in cardiac and renal disease have already been mentioned. The potential for ulcerogenic activity should be kept in mind if phenylbutazone is given to a patient with a history of peptic ulceration. Patients who are hypersensitive to other drugs (especially aspirin) should be carefully monitored when taking phenylbutazone. 

Carbonic anhydrase inhibitors decreased the incidence of phenylbutazone induced ulcers in rats with acetazolamide giving complete protection. There was good correlation between diuretic activity of the carbonic anhydrase inhibitors and the degree of antagonism of the ulcers. This was cited as support for the contention that the ulcerogenic activity of phenylbutazone is partly due to stimulation of carbonic anhydrase in... 

Potent antiulcer activity without ulcerogenic activity [270] coupled with potent anti-inflammatory and an llgesic activities distinguishes copper complexes as a unique class of antiulcer agents, since all other antiulcer drugs do not have anti-inflammatory and analgesic activities. Known copper-dependent biochemical processes can be cited to possibly account for antiulcer activities of copper complexes. 

In this context, P-sitosterol has been reported [220] to possess potent anti-inflammatory and antipyretic activities and its effect was similar to hydrocortisone and oxyphenbutazone on carrageenin induced oedema and it was independent of the pituitary adrenal system moreover, P-sitosterol had a wide margin of safety with minimal ulcerogenic activity and may be of therapeutic value. 

The use of NAA has invariably been accompanied by gastrointestinal irritation. In the rat the operation of the enterohepatlc cycle has been shown to be an important factor in ulcer formation due to indomethacln39 40 and flufenamlc acid. Correlations between the antiinflammatory potency of NAA and gastric irritation in the rat have been claimed g d denied, 3 Leads to a solution of the irritation problem may have been provided by the observations that spironolactone and - -chlorocarbobenzoxy-L-lysin-OMe HCl prevented the ulcerogenic activity of NAA in rats, with the former causing only a limited depression of antiinflammatory activity. 

Indazoles - Tetrydamine (16) was found to be similar to phenylbutazone in acute and chronic AI screens, superior to aspirin as an analgetic, and devoid of ulcerogenic activity. 2 Extensive animal studies-with benzydamine HCl demonstrated AI but not antiarthritic activity. A series of Indazoles for which AI activity was claimed in acute screens is represented by 17a.7 17b. 5 l7c.7o and 17d. ... 

Documented effects Fruits are used as raw material for the preparation Kholosas, which has choleretic activity and is used to treat cholecystitis and hepatitis (Khalmatov et al. 1984). Extracts of the fresh fruits exhibit high anti-ulcerogenic activity in rats (Gurbuz et al. 2003). A galactolipid, which is found in this species, has been shown to possess antitumor-promoting properties, as well as anti-inflammatory effects (Larsen et al. 2003). In a clinical trial, treadnent with a standardized rose-hip powder showed significant reduction of symptoms associated with osteoarthritis (Warholm et al. 2003). 

Gupta SPK (2002) Rustom Jtil Valdl (1911-1974) father of modem cardiology - a profile. J Indian Acad Qin Med 3(1) 100-104 Gutbuz I, Ustun O, Yesilada E, Sezik E, Kutsal O (2003) Anti-ulcerogenic activity of some plants used as folk remedy in Turkey. J Ethnopharmacol 88(l) 93-97... 

I.C.I. 54,450), The agent appears to have potency similar to phenylbutazone in acute screens and is more potent in chronic tests. The related compound (ll) (Wy 21,743) is active in the anti-carrageenin and granuloma pouch screens and la claimed to be non ulcerogenic. Activity in the U.V. erythema test has been reported for the acids (ill), (iv), and (v). ... 

The modification of plasma lipid profiles by rice bran oil has been extensively studied and is the major health benefit highlighted in this section. Other health benefits associated with components of rice bran oil include suppression of B16 melanoma cell proliferation by y- and P-tocotrienols (He et al., 1997 Qureshi et al, 1997, 2000 Lane et al, 1999) and inhibition of tumor-promoting activity by oryzanols (Yasukawa et al, 1998 Akihisa et al, 2000). Cicero and Gaddi (2001) have reviewed other health benefits, including modulation of pituitary secretion and anti-ulcerogenic activity. 

Rosmarinic acid has been found to have anti-inflammatory activity (Sahu et al., 1999). Some anti-inflammatory activity may also be attributed to camosol, which was found to inhibit cyclooxygenase in rat peritoneal leukocytes (Laughton et al., 1991). Anti-ulcerogenic activity also was found in rats given 70% alcohol extracts of rosemary (Dias et al, 2000). The anti-ulcerogenic activity was not due to an inhibition of prostaglandin production, but was related to an increase in the content of mucosal non-protein sulfhydryl groups. 

Best, R., Lewis, D.A. and Nasser, N. The anti-ulcerogenic activity of the unripe plantain banana Musa species). Brit. J. Pharmacol. 82, 107-116 (1984). 

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