In vitro and in vivo immune stimulating effects of a new standardized Echinacea angustifolia root extract (Polinacea).

Polinacea is a new standardized hydroethanolic extract obtained from Echinacea angustifolia roots containing echinacoside (>4%), the high molecular weight polysaccharide IDN 5405 (>5%) and a isobutylamide fraction (<0.1%). For in vitro tests, a bacterial lipopolysaccharide-free (LPS-free) Polinacea has been prepared in order to avoid non-specific responses of immunocompetent cells. LPS-free Polinacea enhanced the immune functions as highlighted by the proliferation rate and gamma-interferon production in murine T-lymphocyte cell cultures stimulated by anti-CD3. LPS-free Polinacea did not have a direct role on macrophage response as measured in the nitric oxide production test using the J774 macrophage cells line. In vivo, Polinacea showed an immune stimulating activity by reducing the Candida albicans induced mortality both in normal and in cyclosporin A-treated mice.

Botanical derivatives for the prostate.

The prostate, after the age of 45 years, may undergo benign hyperplasia (BPH). Its etiology has not yet been completely explained, but different factors play a major role in its occurrence, among them, the sexual hormones (with a fundamental role of 5 alpha reductase). The 5-alpha reductase activity and inflammatory aspects in the prostate tissue can be effectively controlled with the use of highly standardized plant extracts (Pygeum africanum, Serenoa repens, etc.), which yield excellent results in the prophylaxis and treatment of the symptoms linked to prostate hypertrophy. The prostate tissue is not affected only by benign diseases but may also be subject to neoplastic transformation. From an epidemiological point of view, a vegetable derivative, lycopene, was linked with a lower occurrence of prostate carcinoma. A recent clinical study demonstrated that lycopene might not only prevent prostate cancer but also have therapeutic effects.

Contractile effect of (+)-glaucine in the isolated guinea-pig ileum.

The intestinal effects of (+)-glaucine [(S)-1,2,9,10-tetramethoxyaporphine] were studied using the guinea-pig ileum. (+)-Glaucine (10-300 microM) induced ileal contractions. The contraction was not affected by tetrodotoxin, atropine, hexamethonium, propranolol, naloxone, methysergide, N(G)-nitro-L-arginine methyl ester, SR141716A (a cannabinoid CB1 receptor antagonist) or SR140333 (a tackykinin NK1 receptor antagonist) plus SR48968 (a tackykinin NK2 antagonist). (+)-Glaucine-induced contraction was reduced by indomethacin, nordihydroguaiaretic acid or bisindolylmaleimide I and abolished by verapamil and nifedipine. These results suggest that (+)-glaucine-induced contraction involves activation of voltage-dependent Ca2+ channels and protein kinase C and could be mediated by the release of arachidonic acid metabolites.

Synthesis and muscle relaxant activity of cyclic baclofen analogues.

Some new cyclic analogues of baclofen have been prepared and characterized, starting from 4-(4-chlorophenyl)-pyrrolidone. When tested in comparison with the parent compound, they exhibited only a moderate muscle relaxant activity.

Synthesis and antiulcer activity of uvaol hemiphthalate derivatives.

Disodium salts of the dihemiphthalates of urs-12-ene-3 beta, 28-diol 3b and of ursa-9(11), 12-diene-3 beta,28-diol 4b were synthesized from uvaol and examined for their gastroprotective activity in rats. The effects showed by 3b and 4b, given p.o. in two antiulcer tests (ethanol induced gastric lesions and diclofenac induced gastric ulcers), were 5-25 times better than those of carbenoxolone. When given p.o. in the rat once a day for 5 days at a gastroprotective dose, 3b and 4b did not induce any change in urine excretion, whereas carbenoxolone significantly reduced urine volume, Na+ excretion and Na+/K+ ratio. In conclusion, 3b and 4b are effective antiulcer agents, devoid of mineral-corticoid activity and therefore provided with a good therapeutic index.

Synthesis and antihypertensive activity of imidazo[2,1-b]-thiazoles bearing a 2,6-dichlorophenyl group.

A number of imidazo[2,1-b]thiazoles bearing a 2,6-dichlorophenyl group as hydrazone or as amide were prepared and tested in rats as antihypertensive agents. Only compounds bearing a chlorine at position 6 were active.

Effect of a natural flavonoid on gastric mucosal barrier.

The effects of 3,5,7-trihydroxy-2-(3,4-dihydroxyphenyl)-1-benzopyrylium chloride (IdB 1027) on the rat gastric mucosa were evaluated. IdB 1027 administered intragastrically at doses ranging from 100 to 400 mg/kg inhibited the fall in transmucosal potential difference and the increase in H+ back-diffusion induced by acetylsalicylic acid. Moreover, IdB 1027 at doses of 50 and 200 mg/kg by intragastric route increased the gastric bicarbonate secretion. These results suggest that the gastroprotective activity of IdB 1027 is mediated by an increase in the efficiency of gastric mucosal barrier.

Antiulcer activity of an anthocyanidin from Vaccinium myrtillus.

The antiulcer effects of 3,5,7-trihydroxy-2-(3,4-dihydroxyphenyl)-1-benzopyrylium chloride (IdB 1027) were assessed in various experimental models. Given orally, IdB 1027 antagonized gastric ulcerations induced by pylorus ligation, stress, nonsteroidal antiinflammatory drugs, ethanol, reserpine, histamine and duodenal ulceration induced by mercaptamine (cysteamine). Moreover it antagonized chronic gastric ulcers induced by acetic acid. Given intraperitoneally, it was more potent than after oral administration. IdB 1027 did not affect gastric secretion in pylorus-ligated rats and increased gastric mucus in normal animals both in the absence and in the presence of indometacin treatment. Tolerability was very good. These results indicate that IdB 1027 possesses a promising antiulcer activity, probably by potentiating the defensive barriers of the gastrointestinal mucosa.

Studies on Vaccinium myrtillus anthocyanosides. I. Vasoprotective and antiinflammatory activity.

A Vaccinium myrtillus anthocyanosides preparation (equivalent to 25% of anthocyanidins) demonstrated significant vasoprotective and antioedema properties in exerimental animals. In rabbits, the skin capillary permeability increase, due to chloroform, was reduced both after i.p. (25--100 mg/kg) and oral administration (200--400 mg/kg) of anthocyanosides. Their activity was more lasting in comparison to rutin or mepyramine and this did not seem to be due to a specific antagonism towards inflammatory process mediators such as histamine or bradykinin. Experiments carried out in rats demonstrated that Vacinium myrtillus anthocyanosides were effective both in skin capillary permeability test as well as on vascular resistance of rats fed a P factor deficient diet. In the former test effective doses were in the range of 25--100 mg/kg (by oral route). In both the animal species investigated, anthocyanosides were two-fold more active when compared to the flavonoid rutin. Vaccinium myrtillus anthocyanosides by oral route inhibited carrageein paw oedema in rats showing a dose-response relationship. An antioedema activity was detected also after i.v. or topical application.