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cf. C.A. 52, 4929d. In the course of a systematic investigation of Central European plants for antibacterial components, substances in hemp were found to have high activity. Ascending paper chromatography was used to sep. the components of the extract, and strips of the chromatogram were laid on plate cultures of Staphylococcus aureus (in prelim. expts.) to demonstrate activity through inhibitory effects. Under conditions of low conch., chlorophyll so tested with the chromatogram was without antibiotic action (perhaps because of low concentration). The active principle was an amorphous resinous substance, soluble in EtOH, pert. ether, and C6H6, of acid nature, with phenolic and COOH groups, and could be acetylated. The Ac derivs., crystalline substances, showed slight reductions in antibacterial activity over the amorphous material, and were not studied as antibiotics. Purified exts. of Cannabis representing antibiotic-active materials were prepared as follows (cf. Krejci and Santav.acte.y, C.A. 50, 12080d): the comminuted drug was extracted with petr. ether, light benzene, or C6H6; the extract was shaken with N NaOH to form a water-soluble salt; HCl added to precipitate the resin, and this extracted with Et2O, the latter evaporated to leave the antibacterial substance. This could be crystallized by acetylation. This extract was antibacterial to Mycobacterium tuberculosis, even when diluted to 1:150,000. Gram-neg. organisms of the coli-typhus group, Pseudomonas aerogenes, and Proteus vulgaris were not affected. Blood, blood plasma, and Blood serum partially inactivated this substance, reducing the antibiotic effect. Thus, a diln. of 1:100,000, which inhibited S. aureus, was inactivated by adding 10% blood or blood plasma; there was lesser inactivation at 1:10,000 dilns. Antibiotic activity was compared at different pH values (cf. Stoll, et al., Schweiz. Z. allgem. Pathol. Bakteriol. 14, 591(1952)) with penicillin and streptomycin. Na salts of the isolated amorphous substance in aqueous alkaline solution showed increasing activity with increase of pH from 5 to 7.5, whereas crystallized Ac derivs. (acids) showed increasing activity when the pH was decreased from 8 to 5. The rapidity of antibacterial action varied with differing dilns., using S. aureus cultures for testing. Thus, 1: 100 dilns. produced immediate sterilization, 1:10,000 were sterile after 3 hrs., and 1:100,000 dilns. were sterile after 8 hrs. Clinical usage in stomatology, otorhinolaryngology, dermatology, and treatment of tuberculosis is reviewed. 44 references.
Source: CAS Reference Linking Service
Source: CAS Reference Linking Service