Flavonol glycosides from Calendula officinalis flowers

Seven flavonol 3- O-glycosides were isolated from the flowers of CALENDULA OFFICINALIS L. Their structures were elucidated as isorhamnetin 3- O-glucoside, rutinoside, neohesperidoside, 2 (G)-rhamnosylrutinoside, quercetin glucoside, neohesperidoside, and 2 (G)-rhamnosylrutinoside by paper and thin layer chromatography, UV, (13)C-NMR, and mass spectroscopy. The interglycosidic linkages of isorhamnetin 3- O-neohesperidoside, 2 (G)-rhamnosylrutinoside, quercetin 3- O-neohesperidoside and structural determination of quercetin 2 (G)-rhamnosylrutinoside are described for the first time in CALENDULA OFFICINALIS.     

Revised structures of four saponins from Nauclea diderrichii

The interglycosidic linkages of four quinovic acid glycosides previously described from the bark of Nauclea diderrichii (de Wild) Merr. (Rubiaceae) are revised on the basis of 2D-NMR spectroscopic results. The structures were established as: quinovic acid 3-O-beta-glucopyranosyl(1-->4)-beta-fucopyranosyl-(28-->1)-beta -glucopyranosyl ester, quinovic acid 3-O-beta-glucopyranosyl-(1-->4)-alpha-rhamnopyranosyl-(28-->1)-beta-glucopyranosyl ester, quinovic acid 3-O-beta-glucopyrnaosyl-(1-->4)-beta-fucopyranoside, and quinovic acid 3-O-beta-glucopyranosyl-(1-->4)-alpha-rhamnopyranoside. The first three saponins are new compounds.     

Antimalarial activity of extracts and alkaloids isolated from six plants used in traditional medicine in Mali and Sao Tome

Methanol and chloroform extracts were prepared from various parts of four plants collected in Mali: Guiera senegalensis (Gmel.) Combretaceae, Feretia apodanthera (Del.) Rubiaceae, Combretum micranthum (Don.) Combretaceae, Securidaca longepedunculata (Fres.) Polygalaceae and two plants -collected in Sao Tome: Pycnanthus angolensis (Welw.) Myristicaceae and Morinda citrifolia (Benth.) Rubiaceae were assessed for their in vitro antimalarial activity and their cytotoxic effects on human monocytes (THP1 cells) by flow cytometry. The methanol extract of leaves of Feretia apodanthera and the chloroform extract of roots of Guiera senegalensis exhibited a pronounced antimalarial activity. Two alkaloids isolated from the active extract of Guiera senegalensis, harman and tetrahydroharman, showed antimalarial activity (IC(50) lower than 4 microg/mL) and displayed low toxicity against THP1. Moreover, the decrease of THP1 cells in S phase of the cell cycle, after treatment with harman and tetrahydroharman, was probably due to an inhibition of total protein synthesis.     

Antimalarial activity of alkaloids isolated from Stephania rotunda

Stephania rotunda (Menispermaceae) is used in traditional medicine for the treatment of fever. Four major alkaloids: dehydroroemerine, tetrahydropalmatine, xylopinine, cepharanthine as well as aqueous extract (SA), dichloromethane extracts (SD1 and SD2) from this plant were tested against Plasmodium falciparum W2 in vitro. Dehydroroemerine, cepharanthine and SD1 were the most active against W2 with IC(50) of 0.36, 0.61microM and 0.7microg/mL, respectively. Their IC(50) on human monocytic THP1 cells were 10.8, 10.3microM and >250microg/mL, respectively. Cepharanthine, SD1 and SA were selected for in vivo antimalarial test against Plasmodium berghei in mice. The results of SD1 and SA at dose of 150mg/kg showed a decrease of 89 and 74% of parasitaemia by intra-peritoneal injection and 62.5 and 46.5% of parasitaemia by oral administration, respectively. The result of cepharanthine at dose of 10mg/kg showed a decrease of 47% of parasitaemia by intra-peritoneal injection and 50% of parasitaemia by oral administration. Drug interaction of chloroquine and major alkaloids indicates that cepharanthine-chloroquine and tetrahydropalmatine-xylopinine associations are synergistic. These results are in agreement with the use of this plant in the treatment of malaria. This is the first report on in vivo antimalarial investigation for Stephania rotunda.     

Antimutagenic activity of some saponins isolated from Calendula officinalis L., C. arvensis L. and Hedera helix L

Thirteen saponins were isolated and identified from Calendula officinalis, C. arvensis and Hedera helix. Mutagenic and antimutagenic activities of these products were investigated using a modified liquid incubation technique of the Salmonella/microsomal assay. The Salmonella tester strain TA98 +/- S9 mix was used. Screening of the antimutagenic activity was performed with a known promutagen: benzo-[a]pyrene (BaP) and a mutagenic urine concentrate from a smoker (SU). Antimutagenic activities were also compared with the activity of chlorophyllin. All the saponins were found to be non-toxic and non-mutagenic for doses of 400 micrograms. Chlorophyllin inhibited the mutagenic activities of BaP (1 microgram) and SU (5 microliters) in a dose-dependent manner. The four saponins from C. arvensis and the three saponins from H. helix showed antimutagenic activity against BaP (1 microgram) and SU (5 microliters) with a dose-response relationship. The possible mechanism of the antimutagenic activity of saponins is discussed.     

Arterial pressure--self measurement. Recommendations. French Society for Arterial Hypertension--the Measurement Group

Self-measurement of blood pressure has become widespread in recent years. It may be defined as the measurement of arterial pressure by a conscious and free-willed subject. Self-measurement must remain a medical procedure, which means that doctors should be able to advise their patients (a) on the type of apparatus they should purchase and get validated at regular intervals; (b) on the method of using the apparatus in practice, and (c) on the circumstances, conditions and numbers of measurements to be performed. Doctors must remain responsible for the interpretation of the results obtained and for the diagnostic, pronostic an therapeutic applications of the method. Self-measurement of blood pressure naturally has advantages and disadvantages, but it must be noted that it may offer an alternative to hospitalization or to ambulatory arterial pressure measurement, avoid excessive or defective therapies and improve the patient's compliance with his treatment.     

Effect of atenolol, a new cardioselective beta-blocker, on plasma renin activity in treatment of hypertension.

Atenolol, a cardioselective beta-blocking drug, was prescribed in doses of 100 mg b.i.d. in 23 patients with essential hypertension. At the end of the first month of treatment with Atenolol we found a significant fall in blood pressure, heart rate and plasma renin activity (P.R.A.). Besides, there existed a relationship between changes in diastolic blood pressure, in mean arterial pressure and initial plasma renin activity, and a relationship between changes in blood pressure and changes in P.R.A. It results from this finding that pretreatment P.R.A. is of predictive value of short-term efficacy of the beta-blocker. This correlation was borderline in 21 patients after a mean of 7 month treatment and could no be found for 12 cases after a mean of 10 month-treatment while the fall in P.R.A. was still significant. It therefore appears that--with reserve of the representativeness of the sample--quantitative relations between the antihypertensive effect of Atenonol and P.R.A. are no longer significant on long-term treatment.