A new diterpenoid with antispasmodic activity from Salvia cinnabarina.

From the leaf surface exudate of the aerial parts of Salvia cinnabarina a new secoisopimarane diterpenoid with a non-specific spasmolytic activity on histamine-, acetylcholine-, and barium chloride-induced contractions in the isolated guinea-pig ileum was obtained. The IC50 value obtained was comparable with that obtained for papaverine. The structure of 3,4-secoisopimara-4(18),7,15-triene-3-oic acid was established by 1D and 2D NMR spectroscopic techniques.

Methyleugenol in Ocimum basilicum L. Cv. genovese gigante.

Ocimum basilicum cv. Genovese Gigante is the basil cultivar used the most in the production of a typical Italian sauce called pesto. The aromatic composition of plants at different growth stages was determined. Plants from different areas of northwestern Italy were analyzed at 4 and 6 weeks after sowing and showed methyleugenol and eugenol as the main components. The content of these compounds was correlated with plant height rather than plant age. Particularly, methyleugenol was predominant in plants up to 10 cm in height, whereas eugenol was prevalent in taller plants. These results are important in the evaluation of risk to human health posed by dietary ingestion of methyleugenol contained in pesto.

Isolation and characterization of cell lines derived from hamster kidney cells transformed by BK virus, and transforming activity of their DNA.

Eight cell lines obtained from BK virus-transformed hamster kidney cells were characterized by some biological parameters as presence of BKV T antigen, growth properties and tumourigenicity. The transforming ability of their DNA on primary foetal rat fibroblasts was then studied, and transformed rat cells were characterized by the same biological parameters as above. Transformed hamster cells showed no correlation among presence of virus, growth properties and tumourigenicity; DNA from normal hamster kidney cells and from two BKV-transformed cell lines induced transformation on rat fibroblasts, but presence of BKV T antigen was detected only in one DNA-transformed rat cell line. The role of cellular and viral genes on neoplastic transformation is discussed.

Cycloaddition of dichloroketene to N,N-disubstituted 3-aminomethylene-5-hydroxy-2,2-dimethyl-7-pentyl-4-chromanone: synthesis of 2H,5H-pyrano[3,2-c][1]benzopyran derivatives.

The synthesis of N,N-disubstituted 3-aminomethylene-5-hydroxy-2,2-dimethyl-7-pentyl-4-chromanones (III) and their reaction with dichloroketene are described. The resulting cycloadducts (IV) gave, by dehydrochlorination, the N,N-disubstituted 4-amino-3-chloro-10-hydroxy-5,5-dimethyl-8-pentyl-2H,5H-pyrano[3,2-c] [1]benzopyran-2-ones (V), which are structurally related to tetrahydrocannabinols. Only the compound (V a) displayed a very weak stimulant activity on the CNS.

Derivatives of 5,7,7-trimethyl-6-oxa-3-azatricyclo[3.2.2.0(2.4)]nonane with antiarrhythmic, local anesthetic and hypotensive activities.

The synthesis of ureas (IV) and amides (V) derived from the tricyclic terpenoid amine 5,7,7-trimethyl-6-oxa-3-azatricyclo[3.2.2.0(2.4)]nonane (III) is described. A number of these compounds showed hypotensive and bradycardic activity in rats, as well as infiltration anesthesia and antiarrhythmic activity in mice. In particular, the n-butylurea (IV b) was superior to lidocaine concerning the anesthetic effect, and the benzamide (V f) showed the same degree of local anesthetic and antiarrhythmic activity as lidocaine. Antiacetylcholine activity in vitro and antitumor activity against P388 lymphocytic leukemia in mice are also reported.

N-Monosubstituted urethanes of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo [2.2.2] octan-5-trans-ols with hypotensive and other activities.

The synthesis of three series of N-monosubstituted urethanes of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo [2.2.2] octan-5-transols (IV), (V) and (VI) (dialkylamino = pyrrolidino, piperidino, morpholino) by reaction of the corresponding aminoalcohols with alkyl or aryl isocyanates, is described. A number of compounds (IV) and (V) showed remarkable hypotensive and bradycardic activity in rats, whereas (IV c) showed infiltration anesthesia and (IV n) antiarrhythmic activity in mice comparable to those of lidocaine. Antiacetylcholine activity in vitro is also reported.

Correlation of in vitro properties and tumourigenicity of hamster kidney cells transformed by BK virus.

Hamster kidney cells transformed by BK virus (HKBK cells) were studied at low passage (about 30 subcultures) after transformation and at high passage (about 130 subcultures) after transforming. Several in vitro properties (rescue of virus, presence of T antigen, colony formation on plastic, in soft agar, on monolayers of normal cells, and serum dependency of growth) and tumourigenicity of these cells for newborn and adult hamsters were compared. HKBK cells at low passage showed high levels of T antigen, the growth properties of normal cells and low tumour-producing ability, while HKBK cells at high passage showed low levels of T antigen, the growth properties of transformed cells and high tumour-producing ability. These results may indicate that cellular transformation by BK virus is initiated, but not maintained, by the expression of genes regulating T antigen, and that the maintenance of the transformed state is due to complicated cellular and viral gene interactions occurring during the course of cell life.