Pharmacologically Active Ingredients V

Pharmacokinetic-Metabolic Studies With 14C-Aloe Emodin After Oral Administration To Male & Female Rats Lang W Department Of Radiobiochemistry, Madaus AG Pharmacology 47 Suppl 1():110-9 1993 Oct After oral administration of 4.5 mg/kg 14C-Aloe emodin (AE) to rats 20-30% of the dose was excreted in urine and the rest in feces. AE was quickly metabolized to rhein, to an unknown metabolite and to conjugates of all three. In the plasma about 10% of 14C-activity was identified as free AE. Maximum plasma values were reached 1.5-3 h p.a. with 248 (male) and 441 (female) ng equivalents AE/ml. Maximum concentrations in plasma were about 3 times higher than those in ovaries and 10 times higher than those in testes. Only liver, kidney and intestinal tract showed higher concentrations than plasma. Terminal half-life (for radioactivity) in blood was about 50 h. Genotoxicity Of Naturally Occurring Hydroxyanthraquinones Westendorf J; Marquardt H; Poginsky B; Dominiak M; Schmidt J; Marquardt H Department Of Toxicology, University Of Hamburg Medical School Mutat Res Vol 240, ISS 1, 1990, P1-12 A variety of structurally related hydroxyanthraquinones (HA) were investigated in a test battery for the evaluation of mutagenicity and cell-transforming activity. The tests were: (1) the Salmonella typhimurium mutagenicity assay, (2) the V79-HGPRT mutagenicity assay, (3) the DNA-repair induction assay in primary rat hepatocytes and (4) the in vitro transformation of C3H/M2 mouse fibroblasts. In Salmonella, most of the tested compounds were mutagenic in strain TA1537, but only a few were active in other strains. Among these were HA with a hydroxymethyl group, such as lucidin and Aloe-emodin. In V79 cells, only HA with 2 hydroxy groups in the 1,3 positions (1,3-DHA, purpurin, emodin) or with a hydroxymethyl sidechain (lucidin and Aloe-emodin) were mutagenic. The compounds found to be active in V79 cells were also active in the DNA-repair assay and in the C3H/M2 transformation assay. Thus, it appears that the genotoxicity of HA is dependent on certain structural requirements. Mechanochemical Solid State Reactions Of Natural Products For Medicinal Use Containing Hydroxyanthraquinone Derivatives Kuzuya M; Sakata H; Kondo S; Noguchi A Gifu Pharmaceutical University Yakugaku Zasshi 111(11):665-71 1991 Nov In commercial powdered natural products for medicinal use containing various combined forms of hydroxyanthraquinone derivatives such as Sennae Folium, Cassiae Semen, Rhei Rhizoma and Aloe a considerable amount of stable free radicals (ca. 10(17)-10(18) spin/g) was found to be contained by use of electron spin resonance (ESR) spectral measurements. It was also found that the vibratory milling of such powders in a metallic vessel enhanced the ESR spectral intensities, demonstrating the occurrence of mechanoradical formation. Separate experiments also demonstrated that the vibratory milling of various kinds of powdered hydroxyanthraquinone derivatives mixed with calcium oxalate has produced the mechanoradicals effectively, but they decayed gradually on standing at room temperature. It was suggested, therefore, that the mechanoradicals formed in the above natural products are metal complexes of the corresponding semiquinone anion radicals induced by solid state one electron transfer mechanism from the active metal surface, part of which is further immobilized in polymeric fibers or the like in the plant tissues. Aloe Vera Klein AD; Penneys NS Department Of Dermatology, University Of Miami School Of Medicine J Am Acad Dermatol, 18(4 Pt 1):714-20 1988 Apr We reviewed the scientific literature regarding the Aloe vera plant and its products. Aloe vera is known to contain several pharmacologically active ingredients, including a carboxypeptidase that inactivates bradykinin in vitro, salicylates, and a substance(s) that inhibits thromboxane formation in vivo. Scientific studies exist that support an antibacterial and antifungal effect for substance(s) in Aloe vera. Studies and case reports provide support for the use of Aloe vera in the treatment of radiation ulcers and stasis ulcers in man and burn and frostbite injuries in animals. The evidence for a potential beneficial effect associated with the use of Aloe vera is sufficient to warrant the design and implementation of well-controlled clinical trials.