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[The semisynthetic production of pharmacologically active flavone derivatives. I. The pharmaco-toxicological properties of theophylline-rutozide (TR 1722)].

The pharmaco-toxicological properties of the compound theophylline-rutozide, termed conventionally TR-1722, are presented. Studied comparatively with aminophylline, it presents important advantages: soluble in water, the aqueous solutions have a pH close to the physiological one and are stable. It induces a weaker excitation on the central nervous system as compared to aminophylline, but its antihistaminic and anti-inflammatory properties are slightly increased. The physicochemical and pharmacological properties of TR 1722 recommend it for the patients with asthma and associated arterial hypertension or obstructive bronchopneumopathy associated with pulmonary hypertension.

Aminophylline↗

Response of primary tumour, spontaneous metastases and recurrence of Lewis lung carcinoma (3LL) to flavone acetic acid (FAA, LM975).

B6D2F1 mice bearing 3LL were more sensitive to FAA than control mice, the LD50 being 180 x 2 and 336 x 2 mg/kg respectively. At a dosage of 140 mg/kg, injected i.p. at day 4 and 11, FAA significantly decreased the primary tumour growth, the occurrence and the growth of spontaneous pulmonary metastases. The effect of two injections was dose-dependent on the primary tumour and metastases; the survival time was also dose-related. Combined with primary tumour ablation, FAA administered before any dissemination (at day 3) was more efficient against metastases than when it was injected after the end of the dissemination (i.e. after primary tumour ablation). When all treatment schedules were pooled, the number of mice without metastasis was significantly higher in treated than in control groups. The effect of FAA on recurrences was also notable.

Animals↗

Flavones and isoflavones as inducing substances of legume nodulation.

Rhizobia are soil bacteria that can form symbiotic associations with leguminous plants leading to the fixation of atmospheric nitrogen to ammonia which the plant can use. This is an interaction which involves the exchange of many signals between the plant and the bacterium. To start this interaction, rhizobia have adapted to use flavonoid compounds, released by the plant root, as part of a regulatory system to initiate the transcription of their infection (nodulation, nod) genes. The development of an assay system for the detection of plant-derived stimulatory biofactors has now led to the isolation and identification of the compounds which are responsible for the activation of the nod genes. Stimulatory compounds now have been isolated from plants: from clovers, 7,4'-dihydroxyflavone; from alfalfa, luteolin; from peas, apigenin; and from soybeans, the isoflavones daidzein and genistein. These hydroxylated flavonoid compounds are derived from the phenylpropanoid pathways which are responsible for the synthesis of many important plant phenolic compounds, including the phytoalexin molecules which are thought to be involved in plant defence systems. The current hypothesis on the regulation of the nodulation genes in Rhizobium strains is that the gene product of the regulatory nod gene, nodD, requires the presence of the plant signals to convert it to an active form. This altered NodD protein then induces the expression of the other nodulation genes. This bacterium, induced by plant biofactors, now is able to infect legume root hairs.

Fabaceae↗