The formation of 2 photochemically from 1 could be thought of in terms of a concerted ["2a + T2a] cycloaddition reaction;11 however, such a mechanism does not account for the formation of 3.15 An alternative pathway, which can account for the production of both 2 and 3, is an electrocyclic ring-opening reaction that breaks the CeC7 bond of 1 to give the open-chain cation 12. Such a process is directly comparable to that observed upon the photoisomerization of the isoelectronic cyclohexa-1,3-dienes to the bicyclo[3.1.0]hexenes.1116 While the direct isomerization of 12 to give 2 is possible, in view of the constant ratio of 2 to 3 observed in these reactions, it is attractive to consider that a cation resembling 11 might be formed either photochemically, or thermally, from 12 and that this gives the observed products, 2 and 3.(15) A trans ring juncture would result from the alternative [

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A crystalline germination stimulant (trivial name strigol) for the rootparasite, witchweed (Striga lutea Lour.), has been isolated from cotton rootexudates and characterized as a C(19)H(22)O(6) compound. Although apparently different from known plant hormones, the stimulant is active at hormonal levels, causing germination at concentrations less than 1O(-5) part per million.

Drug development is needed to improve chemotherapy of patients with locally advanced or metastatic colon carcinoma, who otherwise have an unfavorable prognosis. DNA topoisomerase I, a nuclear enzyme important for solving topological problems arising during DNA replication and for other cellular functions, has been identified as a principal target of a plant alkaloid 20(S)-camptothecin. Significantly increased concentrations of this enzyme, compared to that in normal colonic mucosa, were found in advanced stages of human colon adenocarcinoma and in xenografts of colon cancer carried by immunodeficient mice. Several synthetic analogs of camptothecin, selected by tests with the purified enzyme and tissue-culture screens, were evaluated in the xenograft model. Unlike other anticancer drugs tested, 20(RS)-9-amino-camptothecin (9-AC) induced disease-free remissions. The overall drug toxicity was low and allowed for repeated courses of treatment.

A comparative study was done in women and men of the effects of delta 9-tetrahydrocannabinol (delta 9-THC), intravenously or orally, on dynamic activity, metabolism, excretion, and kinetics. In general no differences between the two sexes were observed. delta 9-THC is converted by microsomal hydroxylation to 11-hydroxy-delta 9-THC (11-OH-delta 9-THC), which is both a key intermediate for further metabolism to 11-nor-delta 9-THC-9-carboxylic acid (11-nor-acid) by liver alcohol-dehydrogenase enzymes and a potent psychoactive metabolite. Major differences in the ratio of the concentration of 11-OH-delta 9-THC to that of delta 9-THC in plasma were found after intravenous dosing (ratio 1:10 to 20) compared with oral administration (ratio 0.5 to 1:1). The final metabolic products are the 11-nor-acids and the related, more polar acids. Urinary excretion of delta 9-THC is restricted to acidic nonconjugated and conjugated metabolites. After 72 hr mean cumulative urinary excretion, noted for both routes and for both sexes, ranged from 13% to 17% of the total dose. After 72 hr the cumulative fecal excretion for both sexes after intravenous administration ranged from 25% to 30%; after oral administration the range was 48% to 53%. Metabolites were found in the feces in large concentration in the nonconjugated form; concentrations of 11-OH-delta 9-THC were particularly noteworthy. Kinetics of delta 9-THC and metabolites were much the same for female and male subjects. For delta 9-THC, terminal-phase t1/2s for both sexes, irrespective of the route, ranged from 25 to 36 hr. A comparison of the results for AUC/dose (delta 9-THC) after oral dosing with comparable data from intravenous administration indicated bioavailability of the order of 10% to 20% for both sexes. After intravenous delta 9-THC, large apparent volumes of distribution were noted (about 10 l/kg for both sexes).