Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties, diuretic, and anticonvulsant action.

Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.

Anti-inflammatory properties from isolated compounds of Cyclolepis genistoides.

CONTEXT: Cyclolepis genistoides D. Don (Asteraceae) is an Argentinean endemic shrub, known by the vernacular name "palo azul" or "matorro negro". It is widely used in folk medicine as a diuretic, an antirheumatic, and an antispasmodic agent. OBJECTIVE: The aim of this work was to describe the activity of two isolated compounds of C. genistoides, oleanolic acid (1) and deacylcynaropicrin (2), using the carrageenan-induced paw edema method in mice. MATERIALS AND METHODS: Aerial parts of C. genistoides were dried, powdered, and extracted with petroleum ether, ethyl acetate, dichloromethane, and methanol for 48 h. The fractions obtained from the ethyl acetate extract yielded oleanolic acid, while deacylcynaropicrin was obtained according to Abdei-Mogib et al. Structures were elucidated by ¹H-NMR and ¹³C-NMR. The products were administered intraperitoneally at doses of 40, 75, and 100 mg/kg. RESULTS AND DISCUSSION: Compound 1 exhibited significant activity during the first 7 h of the inflammatory phase (at 1, 3, 5, and 7 h), exercising its inhibitory action on inflammation mediated by histamine, prostaglandins, serotonin, and kinins, while compound 2 showed a significant inhibition at 3 and 5 h contributing to this effect, acting in the intermediate phase. CONCLUSIONS: According to the results of this work, the intraperitoneal administration of oleanolic acid and deacylcynaropicrin isolated from the aerial parts of C. genistoides produced a significant inhibition of carrageenan-induced inflammation at doses of 75 and 100 mg/kg. These results give support to the use of this plant as an anti-inflammatory in traditional medicine.

In vitro-in vivo antifungal evaluation and structure-activity relationships of 3H-1,2-dithiole-3-thione derivatives.

As part of our project devoted to the search of new antifungal agents, we report here the in vitro-in vivo antifungal evaluations and a structure-activity relationship (SAR) study of 17 thione derivatives. Some compounds of this series exhibited remarkable antifungal activity against a broad spectrum of pathogenic opportunistic fungi. SAR studies provide a useful information for the determination of the minimum structural requirements for producing the biological response.

Lethal effect of dehydroleucodine (DhL) on amphibian Bufo arenarum embryos.

The dehydroleucodine is a sesquiterpene lactone isolated from Artemisia douglasiana Besser which is used in popular medicine. Toxicity tests using embryos of amphibian have been widely used in order to predict toxic effects of different compounds. However, to our knowledge, there are not studies focussed on the toxic effects of dehydroleucodine on Bufo arenarum, which is an anuran widely distributed in South America. The effect of dehydroleucodine on the survival of embryos was evaluated in an acute test during the early life stage of B. arenarum embryos. Lethality and the degree of adverse effects were dehydroleucodine dose-dependent. Overall, amphibian early life stages appeared to be more susceptible to the embryotoxicity associated with exposure to dehydroleucodine, especially at concentration greater that 3mM. This increased susceptibility may result from the relatively high rate of cellular differentiation and morphogenesis that occurs at this early stage of development.

Comparative study of flavonoids in experimental models of inflammation.

The anti-inflammatory activities of flavonols (quercetin, rutin and morin) and flavanones (hesperetin and hesperidin) were investigated in animal models of acute and chronic inflammation. Rutin was only effective in the chronic process, principally in adjuvant arthritis. On neurogenic inflammation induced by xylene, only the flavanones were effective; besides, these compounds were the most effective on subchronic process. The most important compound in reducing paw oedema induced by carrageenan was quercetin.