Antitumor activity and chemical modification of polysaccharides from niohshimeji mushroom, Tricholma giganteum.

Two chemical modification procedures, Smith degradation and formolysis processes, were used in an attempt to improve the antitumor activity of water-soluble and water-insoluble polysaccharides prepared from the fruiting body of niohshimeji, Tricholoma giganteum. The chemically modified products were examined for their antitumor effects on Sarcoma 180 solid tumor implanted in mice. The following results were as follows: Some Smith degradation products, i.e., O-R-Flo-c-beta and O-R-FA-2 prepared from water-soluble polysaccharides, and O-R-FII-1 and O-R-FIII-2-c from water-insoluble polysaccharides, had higher antitumor activities than the original polysaccharides. None of the formolysis products, F-Flo-a, F-W-Flo-a, F-FA-3, F-W-FA-3 from water-soluble polysaccharides, and F-FII-2, F-W-FII-2, F-FIII-2-b, and F-W-FIII-2-b prepared from water-insoluble polysaccharides had improved antitumor activities.

Antitumor-active heteroglycans from niohshimeji mushroom, Tricholoma giganteum.

Water-soluble polysaccharide FI and water-insoluble polysaccharides FII, FIII-1, and FIII-2 were obtained from fruiting bodies of Tricholoma giganteum. Polysaccharides were further fractionated by ion-exchange chromatography, gel filtration, and affinity chromatography. The 24 polysaccharide fractions obtained were examined for their antitumor effect on Sarcoma 180 implanted in mice. The following antitumor-active polysaccharides were identified: FIo-a, a mixture of alpha-D-glucan and xyloglucomannan with an average molecular weight of 1.6 x 10(6); FA-1, a beta-D-glucan containing 1% protein and with a molecular weight of 4.0 x 10(4); FII-1, a (1-->3)-beta-D-glucan containing 7.8% protein, with a molecular weight of 5.2 x 10(4); FIII-1-b, a protein-polysaccharide complex (ratio, 37.5:62.5, w/w), with a molecular weight of 6.8 x 10(4) and with xylose, galactose, mannose, and glucose in the polysaccharide moiety (proportions of 8.9:14.9:29.3:46.9 by weight), and FIII-2-a, b, and c, three (1-->6)-beta-D-glucosyl-branched (1-->3)-beta-D-glucans with a molecular weight from 2.6 x 10(5) to 4.1 x 10(5) and containing small amounts of xylose and galactose and 3.5-8.3% protein.

Antitumor protein-containing polysaccharides from a Chinese mushroom Fengweigu or Houbitake, Pleurotus sajor-caju (Fr.) Sings.

Protein-containing polysaccharides extracted from fruiting bodies of a Chinese fungus named Feng Wei Gu, were fractionated and purified, and their antitumor activities were tested, out of which the following active fractions were obtained. FIo-a: A protein-containing xyloglucan, MW 280,000, polysaccharide: protein = 76:24 (w/w), polysaccharide consisting of Man:Gal:Xyl:Glc = 2:12:42:42 (molar ratio). [alpha]D23 + 25.3 degrees. FA-2: A protein-containing mannogalactan, MW 120,000, polysaccharide: protein = 76:16 (w/w), consisting of Xyl:Man:Gal = 9:35:56 (molar ratio), [alpha]D23 + 98.5 degrees. FII-1: A Protein-containing xylan (62:21 w/w). MW 200,000, [alpha]D23 + 8.7 degrees. FIII-1a: A protein-containing glucoxylan (15:71 w/w), [alpha]D23 + 30.7 degrees, MW 90,000, consisting of Glc:Xyl = 40:44 (molar ratio). FIII-2a: A protein-containing xyloglucan, MW 70,000, polysaccharide:protein = 69:3 (w/w), polysaccharide consisting of Xyl:Glc = 36:62 (molar ratio). [alpha]D23 + 38.6 degrees.

[Pharmacological action of bromazepam suppository].

Differences between the pharmacological effects of bromazepam given by oral and rectal administration were investigated in mice and rats. 1) Bromazepam dose-dependently prolonged the sleeping time induced by thiopental-Na, ethanol and ether by both administration routes. 2) The analgesic action of bromazepam was recognized by the hot-plate method and the algolytic test. In the hot-plate test, analgesic actions of morphine and pentazocine were potentiated by bromazepam in a dose of 0.5 mg/kg by both routes. 3) The muscle relaxant effect of bromazepam administered rectally was more potent than that administered orally in the inclined screen test and the rotarod test. This effect of bromazepam by rectal administration was approximately 2 times as potent as that by oral administration. 4) Bromazepam inhibited the convulsion induced by maximum electric shock, pentylenetetrazol and picrotoxin. In pentylenetetrazol-induced convulsion, the inhibitory effect of bromazepam administered rectally was 2 times as potent as that administered orally. In the other convulsion test, no significant differences between oral and rectal administration could be recognized. 5) Hyperemotionality and muricide (mouse-killing behaviour) of rats with bilateral olfactory bulb ablations (OB rat) were reduced by oral and rectal administrations of bromazepam in a dose-dependent manner. The effects by rectal administration were more potent than that by oral administration. Bromazepam was approximately 20 times as potent as diazepam administered by the same route. Fighting behaviour in mice subjected to footshock was suppressed by rectal administration of bromazepam, and this effect was as same as that by oral administration. 6) The rate of lever pressing response in the lateral hypothalamic self-stimulation test in the Skinner box was markedly increased by rectal administration of 0.2 mg/kg bromazepam. 7) Methamphetamine-induced hyperactivity of mice was significantly suppressed only by bromazepam administered rectally in a dose of 5 mg/kg. 8) The falling effect of bromazepam on body temperature in normal rats was the same in both administration routes and was dose-dependent. From these data, significant differences of the pharmacological effects between oral and rectal administration of bromazepam were recognized in the duration of action and, in part, potencies; and therefore, rectal administration of bromazepam may be a useful dosage form for clinical use.