The antitumor activity of the culture filtrate of the fungus Hohenbuehelia geogenius (basidiomycete) was investigated on two rapidly growing grafted tumors: Ehrlich's ascites carcinoma and L1210 lymphoid leukemia and also on a slow growing spontaneous mammary tumor in PS strain mice. The mycelial culture filtrate inhibited the growth of these three tumors. An active substance was isolated from the mycelial culture filtrate by solid-liquid extraction and column chromatography. Its chemical structure was elucidated with ultraviolet and infrared spectra, mass spectrum, nuclear magnetic resonance, and X-ray diffraction.

AbstractAus der Säure (I) wird über das Säurechlorid (II) das Titelamid (III) dargestellt.

The effects of 2-(p-chloro-alpha-hydroxybenzyl) benzimidazole HCl (HBBPC) have been studied on the femoral peripheral resistance (i.v. route) and only femoral blood flow (local i.a. injection), in comparison with other vasodilators, i.e., sodium nitroprusside, dihydralazine and piribedil. The vasomotor activity of HBBPC, namely, decreased peripheral resistance and increased femoral blood flow, seems interesting because it begins after pressure has returned to normal. This substance is likely to induce a vasoconstriction in other areas (increased femoral blood flow with decreased peripheral resistance without a fall of blood pressure).

The effects of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride (HBBPC) have been studied in the rabbit and rat. Most of these studies were performed comparatively with reference vasodilators and papaverine. HBBPC vasodilator activity is nearly the same as that of papaverine in the isolated rabbit ear. The characteristic of the vasoactive action of HBBPC seems to reside in its duration. The mechanism of action of HBBPC seems of peripheral type, that is to say it acts on the vascular smooth muscle.

The activity of a number of vasodilatory drugs was studied, with the help of impedance rheoplethysmography, on the vascular bed of the hind limb of anaesthetized rabbits. The vasodilators under study induce changes in rheoplethysmogram to a more or less important degree. The results were compared with those obtained with electromagnetic flowmetry. This method seems to be useful in the study of vasodilators because it allows to measure their effects and the duration thereof in a non-aggressive way. This method using flowmetry, allows to study in an analytical way those substances' effects on artery, vein and also capillary.

The investigation of methyl (2,2-diphenyl)-vinyl sulfone (14C-MDVS) administered i.p. in mice shows that this product appears rapidly in the general circularoty system. The blood concentration of MDVS reaches a maximum 1 h after injection. Part of the MDVS is bound to the plasma proteins. Infrared spectrometry analysis of radioactive products eliminated by the urine confirms that the product is not split, but also reveals the presence of hydroxyl and carbonyl groups in the metabolic conversion products.