€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****AMERICAN JOURNAL OF VETERINARY RESEARCH***** Hatch RC Jain AV Weiss R Clark JD Toxicologic study of carboxyatractyloside (active principle in cocklebur--Xanthium strumarium) in rats treated with enzyme inducers and inhibitors and glutathione precursor and depletor. In: Am J Vet Res (1982 Jan) 43(1):111-6 ISSN: 0002-9645 Male rats (10 rats/group) were treated with phenobarbital (PB), phenylbutazone (PBZ), stanozolol (3 inducers of cytochrome P450- dependent enzymes), piperonyl butoxide (PBO; a P450 inhibitor), cobaltous chloride (CoCl2; an inhibitor of hemoprotein synthesis), 5,6-benzoflavone (BNF; an inducer of cytochrome P448 dependent enzymes), cysteine [CYS; a glutathione (GSH) precursor], or ethyl maleate (EM; a GSH depletor). The rats were then given a calculated LD50 dosage (13.5 mg/kg of body weight) of carboxyatractyloside (CAT) intraperitoneally. Clinical signs of toxicosis, duration of illness, lethality, gross lesions, and hepatic and renal histopathologic lesions were recorded. Seemingly, (i) CAT toxicosis has independent lethal and cytotoxic components (PBZ decreased lethality and cytotoxicity; CoCl2 decreased cytotoxicity but not lethality; BNF decreased duration of illness, and perhaps lethality, but not cytotoxicity); (ii) CAT cytotoxicity could be partly due to an active metabolite formed by de novo-synthesized, P450-/P448-independent hemoprotein (PBZ and CoCl2 had anticytotoxic effects, but PB, stanozolol, PBO, and BNF did not); (iii) CAT detoxification may occur partly through a hemoprotein-independent, PBZ-inducible enzyme, and partly through a P448-dependent (BNF-inducible) enzyme; and (iv) CAT detoxification apparently is not P450 or GSH-dependent because PB, stanozolol, and CYS had no beneficial effects, and PBO, CoCl2, and EM did not enhance toxicosis. Metabolism of CAT may have a role in its cytotoxic and lethal effects. Registry Numbers: 10418-03-8 (Stanozolol) 141-05-9 (diethyl maleate) 17754-44-8 (Atractyloside) 35988-42-2 (carboxyatractyloside) 4371-52-2 (Cysteine) 50-06-6 (Phenobarbital) 50-33-9 (Phenylbutazone) 51-03-6 (Piperonyl Butoxide) 6051-87-2 (beta-Naphthoflavone) 7440-48-4 (Cobalt) 7646-79-9 (cobaltous chloride) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ASIAN PACIFIC JOURNAL OF ALLERGY AND IMMUNOLOGY***** Kanthawatana S Tontayapiwat A Tonsuwannont W Manorot M A single-dose comparison of three slow-release theophylline oral preparations in healthy Thai volunteers. In: Asian Pac J Allergy Immunol (1996 Jun) 14(1):13-8 ISSN: 0125-877X The study was done to compare the pharmacokinetic characteristics of three slow-release theophylline (SRT) preparations. Twelve healthy nonsmokers were randomly assigned a single dose of the following treatments at weekly intervals: Theo-Dur, Theo-24 or Xanthium orally, or aminophylline intravenously. Serially collected serum samples were analyzed for theophylline with use of fluorescence polarization immunoassay (FPIA). All three SRT preparations showed reliable absorption characteristics, but Theo-Dur had a shorter Tmax and MRT and a higher Ka. The pharmacokinetic characteristics of Theo-24 and Xanthium were similar except that Xanthium had lower bioavailability. Using single dose data for simulation of steady state pharmacokinetics, we found that a once-a-day dosage regimen with either Theo-24 or Xanthium would maintain serum levels within the therapeutic range for average non-smoking young adults whereas more frequent dosing intervals with Theo-Dur would be more appropriate. Our results argue against open substitution of SRT preparations without, close monitoring of the serum theophylline concentrations when a change is made. Registry Numbers: 58-55-9 (Theophylline) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****EXPERIENTIA***** Kawazu K Nakajima S Ariwa M Xanthumin and 8-epi-xanthatin as insect development inhibitors from Xanthium canadense Mill. In: Experientia (1979 Oct 15) 35(10):1294-5 ISSN: 0014-4754 Two insect development inhibitors against Drosophila melanogaster have been isolated from the leaves of X. canadense and identified as xanthumin and 8-epi-xanthatin. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF ETHNOPHARMACOLOGY***** Talakal TS Dwivedi SK Sharma SR In vitro and in vivo antitrypanosomal activity of Xanthium strumarium leaves. In: J Ethnopharmacol (1995 Dec 15) 49(3):141-5 ISSN: 0378-8741 Antitrypanosomal activity of crude 50% ethanolic extract of Xanthium strumarium leaves was studied in vitro and in vivo. The extract exhibited trypanocidal activity at all four concentrations tested i.e. 5, 50, 500 and 1000 micrograms/ml, in vitro. In vivo trial revealed that the extract exerted antitrypanosomal effect at dosage of 100, 300 and 1000 mg/kg, intraperitoneally. At 100 and 300 mg/kg doses the survival period of the Trypanosoma evansi infected mice was significantly prolonged. However, the extract was found to be toxic to the animals at 1000 mg/kg dose. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF NATURAL PRODUCTS***** MacLeod JK Moeller PD Franke FP Two toxic kaurene glycosides from the burrs of Xanthium pungens. In: J Nat Prod (1990 Mar-Apr) 53(2):451-5 ISSN: 0163-3864 Two H2O-soluble toxic kaurene glycosides 3 and 4 responsible in part for the poisonous properties of the burr of Xanthium pungens have been isolated and identified. The structures of the compounds were elucidated using high resolution 2D nmr and mass spectral techniques. Registry Numbers: 17754-44-8 (Atractyloside) 34424-57-2 (kaurene) 35988-42-2 (carboxyatractyloside) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ZEITSCHRIFT FUR NATURFORSCHUNG. SECTION C. JOURNAL OF BIOSCIENCES***** Tsankova ET Trendafilova AB Kujumgiev AI Galabov AS Robeva PR Xanthanolides of Xanthium italicum Moretti and their biological activity. In: Z Naturforsch [C] (1994 Jan-Feb) 49(1-2):154-5 ISSN: 0341-0382 Seven xanthanolides were identified in the extract of X. italicum leaves. Antibacterial and cytotoxic activities were found for the total extract and its major constituents xanthinin and xanthatin. Registry Numbers: 26791-73-1 (xanthatin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€