€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CLINICA TERAPEUTICA***** Sopranzi N De Feo G Mazzanti G Braghiroli L [The biological and electrophysiological parameters in the rat chronically treated with Lobelia inflata L.] Parametri biologici ed elettrofisiologici nel ratto trattato cronicamente con Lobelia inflata L. In: Clin Ter (1991 May 31) 137(4):265-8 ISSN: 0009-9074 (Published in Italian) In this paper we have studied the rat under chronic treatment with Lobeline sulphate ip. For a three week period we have recorded, once a week, weight, rectal temperature, tail-flick, motor coordination and general activity in a one-arm radial maze and in a Boissier-Simon table. At the end of the third week surface (SEEG) and deep (DEEG) EEG were recorded both from treated and control animals. The findings are: 1) no changes was observed in weight, rectal temperature, tail- flick and motor coordination; 2) the treated rats showed an increased general activity both in a one-arm radial maze and in the Boissier- Simon table; 3) the EEG effects were analyzed and quantified, by means of Fast Fourier transform, as total power and as power in preselected bands of frequency. The lobeline sulphate seems to produce both in SEEG and hippocampus a shift toward low frequencies and in amygdala a drift toward high frequencies. Registry Numbers: 90-69-7 (Lobeline) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF THE CHEMICAL SOCIETY. PERKIN TRANSACTIONS 1***** O'Donovan DG Long DJ Forde E Geary P The biosynthesis of lobelia alkaloids. Part III. Intermediates in the biosynthesis of lobeline; biosynthesis of 8, 10-diethyl- lobelidione. In: J Chem Soc [Perkin 1] (1975)(5):415-9 ISSN: 0300-922X [No Abstract Available] €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF PHARMACY AND PHARMACOLOGY***** Subarnas A Tadano T Oshima Y Kisara K Ohizumi Y Pharmacological properties of beta-amyrin palmitate, a novel centrally acting compound, isolated from Lobelia inflata leaves. In: J Pharm Pharmacol (1993 Jun) 45(6):545-50 ISSN: 0022-3573 Effects of beta-amyrin palmitate isolated from the leaves of Lobelia inflata were studied on the central nervous system of mice and were compared with those of antidepressant drugs, mianserin and imipramine. In the forced swimming test, beta-amyrin palmitate, like mianserin and imipramine, reduced the duration of immobility of mice significantly in a dose-dependent manner (5, 10 and 20 mg kg-1). beta- Amyrin palmitate (5, 10 and 20 mg kg-1) or mianserin (5, 10 and 20 mg kg-1) elicited a dose-related reduction in locomotor activity of mice and antagonized locomotor stimulation induced by methamphetamine. In contrast, imipramine (5, 10 and 20 mg kg-1) increased locomotor activity and potentiated methamphetamine-induced hyperactivity. beta- Amyrin palmitate showed no effect on reserpine-induced hypothermia, whilst mianserin (10 mg kg-1) and imipramine (10 and 20 mg kg-1) antagonized the reserpine-induced effect. Unlike imipramine, beta- amyrin palmitate and mianserin did not affect haloperidol-induced catalepsy, tetrabenazine-induced ptosis and apomorphine-induced stereotypy. beta-Amyrin palmitate and imipramine had no effects on the head-twitch response induced by 5-hydroxytryptophan, whereas mianserin (5, 10 and 20 mg kg-1) decreased it in a dose-dependent manner. A potentiating effect of beta-amyrin palmitate (5, 10 and 20 mg kg-1) on narcosis induced by sodium pentobarbitone was stronger than that of imipramine (10, 20 and 40 mg kg-1) but weaker than that of mianserin (2.5, 5 and 10 mg kg-1). These results suggest that beta- amyrin palmitate has similar properties in some respects to mianserin and might possess a sedative action.(ABSTRACT TRUNCATED AT 250 WORDS) Registry Numbers: 24219-97-4 (Mianserin) 50-06-6 (Phenobarbital) 50-49-7 (Imipramine) 50-55-5 (Reserpine) 52-86-8 (Haloperidol) 537-46-2 (Methamphetamine) 58-00-4 (Apomorphine) 58-46-8 (Tetrabenazine) 5973-06-8 (amyrin palmitate) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF PHARMACEUTICAL SCIENCES***** Subarnas A Oshima Y Sidik Ohizumi Y An antidepressant principle of Lobelia inflata L. (Campanulaceae). In: J Pharm Sci (1992 Jul) 81(7):620-1 ISSN: 0022-3549 A crude methanolic extract of the leaves of Lobelia inflata exhibited antidepressant activity in mice. The extract was fractionated, monitored by the activity, to give beta-amyrin palmitate as an active component. Registry Numbers: 50-49-7 (Imipramine) 559-70-6 (amyrin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****LIFE SCIENCES***** Subarnas A Tadano T Nakahata N Arai Y Kinemuchi H Oshima Y Kisara K Ohizumi Y A possible mechanism of antidepressant activity of beta-amyrin palmitate isolated from Lobelia inflata leaves in the forced swimming test. In: Life Sci (1993) 52(3):289-96 ISSN: 0024-3205 A mechanism of antidepressant activity of beta-amyrin palmitate was studied using the forced swimming method in mice. Beta-amyrin palmitate (10 mg/kg) reduced the increase in the duration of immobility induced by tetrabenazine (100 and 200 mg/kg), but showed no effect on that in mice treated with alpha-methyl-para-tyrosine (500 mg/kg). Beta-amyrin palmitate (5 and 10 mg/kg) decreased the duration of immobility in mice treated with desipramine plus 6- hydroxy-dopamine (50 micrograms/mouse), but did not affect that induced by nomifensine plus 6-hydroxydopamine. The decreased immobility produced by desipramine (15 mg/kg) was not affected by beta-amyrin palmitate. A study of norepinephrine release in mouse brain synaptosomes indicated that beta-amyrin palmitate caused a release of [3H]norepinephrine. The results of the present study suggest that beta-amyrin palmitate might release norepinephrine from newly synthesized pools, and thus, it might activate noradrenergic activity. Registry Numbers: 10028-17-8 (Tritium) 1199-18-4 (Oxidopamine) 24526-64-5 (Nomifensine) 50-47-5 (Desipramine) 51-41-2 (Norepinephrine) 58-46-8 (Tetrabenazine) 5973-06-8 (amyrin palmitate) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****SCIENCE IN CHINA. SERIES C, LIFE SCIENCES***** Tian Q Zhao D Zhang J Gao L Liu S Yang J Su J Zhang Z Tang J Tang C Investigation on inhibition of biological effects of endothelin. In: Sci China C Life Sci (1996 Apr) 39(2):207-16 ISSN: 1006-9305 The effects of a series of substances on the biological function of endothelin (ET) are reported. The substances used are: synthetic inhibitors of endothelium derived relaxing factors (EDRFs), inhibitor of big-endothelin converting enzyme phosphoramidon, antiserum of endothelin, antagonists of endothelin A receptor BQ123 and JKC301, and two Chinese anti-snake venom herb medicines Lobelia radicans Thumb and Taris polyphylla Smith var. chinensis (Franch) Hara. The results showed that inhibiting the production of nitric oxide (NO) could stimulate ET release from vascular endothelium, elevate plasma ET and increase blood pressure. These changes could be reversed by L- arginine (L-Arg), the substrate of nitric oxide synthase (NOS). The amount of ET released by arterial endothelium could be increased or inhibited by inhibiting or stimulating the synthesis of prostacyclin (PGI2). The plasma ET level and blood pressure in both SHR and WKY rats could be decreased by giving phosphoramidon (PhR). The above results indicate that the biological effects of ET could be antagonized by inhibiting the synthesis or release of ET, decreasing the level of plasma ET, blocking the binding of ET with its receptor and using some Chinese anti-snake venom herb medicines. Registry Numbers: 136553-81-6 (BQ 123) 2149-70-4 (nitroarginine) 35121-78-9 (Epoprostenol) 36357-77-4 (phosphoramidon) 7004-12-8 (Arginine) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€