€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****BIOCHEMISTRY***** McManus OB Harris GH Giangiacomo KM Feigenbaum P Reuben JP Addy ME Burka JF Kaczorowski GJ Garcia ML An activator of calcium-dependent potassium channels isolated from a medicinal herb. In: Biochemistry (1993 Jun 22) 32(24):6128-33 ISSN: 0006-2960 Large-conductance calcium-dependent potassium (maxi-K) channels play an important role in regulating the tone of airway smooth muscle and the release of bronchoconstrictive substances from nerves in the lung. Crude extracts of Desmodium adscendens, a medicinal herb used in Ghana as a treatment for asthma, inhibit binding of monoiodotyrosine charybdotoxin (125I-ChTX) to receptor sites in bovine tracheal smooth muscle membranes that have been shown to be associated with maxi-K channels. Using this assay, three active components have been purified and identified by NMR and MS. Comparison with authentic samples revealed the three active components as the known triterpenoid glycosides dehydrosoyasaponin I (DHS-I), soyasaponin I, and soyasaponin III. The most potent of these compounds, DHS-I, is a partial inhibitor of 125I-ChTX binding (Ki = 120 nM, 62% maximum inhibition). Inhibition of 125I-ChTX binding is primarily due to a decrease in the observed maximum number of binding sites, with a smaller decrease in affinity. DHS-I increases the rate of toxin dissociation from its receptor, suggesting that modulation of ChTX binding occurs through an allosteric mechanism. DHS-I reversibly increases the open probability of maxi-K channels from bovine tracheal smooth muscle incorporated into planar lipid bilayers when applied to the intracellular, but not the extracellular, side of the membrane at concentrations as low as 10 nM. In contrast, DHS-I had no effect on several other types of potassium channels or membrane transporters. This natural product is the first example of a high-affinity activator of calcium-dependent potassium channels and is the most potent known potassium channel opener. Registry Numbers: 115422-61-2 (Charybdotoxin) 117210-14-7 (dehydrosoyasaponin I) 51330-27-9 (soyasaponin I) 55304-02-4 (soyasaponin III) 7440-70-2 (Calcium) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****BRITISH JOURNAL OF UROLOGY***** Hirayama H Wang Z Nishi K Ogawa A Ishimatu T Ueda S Kubo T Nohara T Effect of Desmodium styracifolium-triterpenoid on calcium oxalate renal stones. In: Br J Urol (1993 Feb) 71(2):143-7 ISSN: 0007-1331 We have studied the inhibitory effects of Desmodium styracifolium- triterpenoid (Ds-t) (extracted from Desmodium styracifolium (Osbeck) Merr, a herbal medicine) on the formation of calcium oxalate renal stones induced experimentally by ethylene glycol (EG) and 1 alpha(OH)D3 (1 alpha D3) in rats. The incidence of urinary stone formation was 81% in the control group, which received EG and 1 alpha D3, and 29% in the Ds-t group, which received EG and 1 alpha D3 supplemented by Ds-t. The serum calcium (Ca) concentration in the Ds- t group was significantly elevated and urinary Ca excretion was markedly reduced. Urinary excretion of citrate (Cit), a factor that prevents stone formation, was significantly increased in the Ds-t group. Excretion of urinary phosphorus (P), which was elevated to a significantly greater extent in the controls than in the Ds-t group, was increased in both groups. The increase in urine volume in the Ds- t group was significantly greater than in the control group. The 24-h creatinine clearance rate (Ccr) was significantly lower in the controls. These findings suggest that Ds-t inhibits the formation of Ca oxalate stones in rat kidneys by increasing the output of urine, decreasing the excretion of calcium and increasing the urinary excretion of citrate. Ds-t may be useful in preventing the recurrence of urinary Ca oxalate stones in the clinical setting. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****AMERICAN JOURNAL OF CHINESE MEDICINE***** Ho CS Wong YH Chiu KW The hypotensive action of Desmodium styracifolium and Clematis chinensis. In: Am J Chin Med (1989) 17(3-4):189-202 ISSN: 0192-415X The cardiovascular pharmacology of aqueous extracts of Desmodium styracifolium (DSE) and Clematis chinensis (CCE) were studied in rats both in vivo and in vitro. DSE produced two successive hypotensive actions: the first one via cholinergic receptor stimulation, while the second one potentiated by blockades of autonomic ganglion and alpha-adrenoceptor. In contrast to DSE, CCE produced only one hypotensive response which was mediated through histaminergic activity. Furthermore, both extracts relaxed isolated methoxamine preconstricted helical tail artery strips. CCE also produced both negative chronotropic and inotropic effects on isolated atria, while DSE was positive chronotropic without apparent effect on the contractile force. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY***** Addy ME Burka JF Effect of Desmodium adscendens fractions on antigen- and arachidonic acid-induced contractions of guinea pig airways. In: Can J Physiol Pharmacol (1988 Jun) 66(6):820-5 ISSN: 0008-4212 Three fractions (n-butanol, F2, and L5), isolated from an aqueous extract of Desmodium adscendens, a plant used in Ghana for the management of asthma, were evaluated for their pharmacological activity using ovalbumin and arachidonic acid-induced contractions of guinea pig airways. All three fractions inhibited the ovalbumin- induced contractions of indomethacin-pretreated tracheal spirals from sensitized animals dose dependently, but only L5 and n-butanol inhibited such contractions in the absence of indomethacin. The concentrations required to inhibit ovalbumin-induced contractions of lung parenchymal strips were threefold higher than with trachea. The contractile response over a 60-min period was divided into three phases. F2 and n-butanol inhibited all phases, whereas L5 inhibited only the late phase. n-Butanol and L5 inhibited arachidonic acid- induced contractions on indomethacin-pretreated tracheal spirals, a leukotriene-dependent reaction. There was no inhibition of arachidonic acid-induced contractions of lung parenchymal strips, which is largely a thromboxane-dependent reaction. The results suggest that D. adscendens contains several pharmacologically active substances that can inhibit allergic airway smooth muscle contraction at multiple sites, including the synthesis and (or) activity of the bronchoconstrictor leukotrienes. Registry Numbers: 506-32-1 (Arachidonic Acid) 53-86-1 (Indomethacin) 71-36-3 (n-butyl alcohol) 9006-59-1 (Ovalbumin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHEMICAL AND PHARMACEUTICAL BULLETIN***** Kubo T Hamada S Nohara T Wang ZR Hirayama H Ikegami K Yasukawa K Takido M Study on the constituents of Desmodium styracifolium. In: Chem Pharm Bull (Tokyo) (1989 Aug) 37(8):2229-31 ISSN: 0009-2363 Two triterpenoid saponins (1 and 2) were isolated from Desmodii Herba [the dried whole plants of Desmodium styracifolium (Osbeck) Merr. (Leguminosae)] and their chemical structures were characterized as soyasaponin I and a new saponin, 3-O-[alpha-L-rhamnopyranosyl-(1---- 2)-beta-D-galactopyranosyl- (1----2)-beta-D- glucuronopyranosyl]soyasapogenol E, respectively, by chemical and spectroscopic means. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF ETHNOPHARMACOLOGY***** Addy ME Burka JF Effect of Desmodium adscendens fraction 3 on contractions of respiratory smooth muscle. In: J Ethnopharmacol (1990 Jul) 29(3):325-35 ISSN: 0378-8741 The third flash chromatography fraction prepared from an aqueous extract of Desmodium adscendens leaves (DAF3) was evaluated for pharmacological activity using contractions of tracheal spirals and lung parenchymal strips caused by ovalbumin, arachidonic acid, histamine and carbachol. DAF3 inhibited both the early and late phases of antigen-induced contractions of both tissues dose- dependently, but had no effect on arachidonic-induced contractions. With tracheal spirals, the inhibition occurred whether the tissue was pretreated with indomethacin or not. On tracheal spirals, the maximum contraction (Emax) caused by histamine and carbachol were enhanced, but the pD2 value for histamine was not affected while that for carbachol was decreased. DAF3 had no effect on Emax or pD2 values for these agonists on lung parenchymal strips. The results suggest that DAF3 may inhibit the release of free arachidonic acid. Registry Numbers: 506-32-1 (Arachidonic Acid) 51-45-6 (Histamine) 51-83-2 (Carbachol) 64-17-5 (Alcohol, Ethyl) 9006-59-1 (Ovalbumin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Addy ME Awumey EM Effects of the extracts of Desmodium adscendens on anaphylaxis. In: J Ethnopharmacol (1984 Aug) 11(3):283-92 ISSN: 0378-8741 Desmodium adscendens, used by herbalists in Ghana for the treatment of asthma, is anti-anaphylactic in vitro. As the plant material is administered orally, in vivo studies of its anti-anaphylactic property were undertaken using the guinea-pig. The results show that both aqueous and ethanolic extracts of D. adscendens, when taken orally, reduce anaphylactic contractions, interfere with histamine- induced contractions, and reduce the amount of smooth muscle stimulating substances released from lung tissue of guinea pigs. Registry Numbers: 51-45-6 (Histamine) 9006-59-1 (Ovalbumin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ N'gouemo P Baldy-Moulinier M Nguemby-Bina C Effects of an ethanolic extract of Desmodium adscendens on central nervous system in rodents. In: J Ethnopharmacol (1996 Jun) 52(2):77-83 ISSN: 0378-8741 This study investigates some pharmacological effects of the ethanolic extract of the leaves of Desmodium adscendens (Papillionaceae), a medicinal plant in the African traditional medicine, on the central nervous system. The plant extract induced hypothermia and had analgesic effect in mice. D. adscendens suppressed the tonic phase of convulsion and mortality induced by pentylenetetrazole (PTZ) in mice. In addition, the plant extract delayed the onset of PTZ forelimb clonus, and generalized limbic seizures induced by kainic acid. In contrast, the plant extract did not affect either tonic convulsion induced by maximal electroshock in mice or the progression of limbic seizures towards the status epilepticus in rats. Registry Numbers: 487-79-6 (Kainic Acid) 54-95-5 (Pentylenetetrazole) 64-17-5 (Alcohol, Ethyl) 64-19-7 (acetic acid glacial) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Addy ME Dzandu WK Dose-response effects of Desmodium adscendens aqueous extract on histamine response, content and anaphylactic reactions in the guinea pig. In: J Ethnopharmacol (1986 Oct) 18(1):13-20 ISSN: 0378-8741 Different concentrations of a hot water extract of Desmodium adscendens, a plant used in Ghana to control asthmatic attacks, were used in drinking water to evaluate the plant's anti-anaphylactic properties in guinea pigs. The results show that the extract's inhibition of histamine-induced ileal contraction is largely competitive and that its effect of reducing lung histamine content is dose-dependent. The results also show that the extract causes a dose- dependent reduction in the amount of spasmogens released anaphylactically and in anaphylactic-induced contraction of ileal muscle. Registry Numbers: 51-45-6 (Histamine) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****MEMORIAS DO INSTITUTO OSWALDO CRUZ***** Vargas VM Guidobono RR Henriques JA Genotoxicity of plant extracts. In: Mem Inst Oswaldo Cruz (1991) 86 Suppl 2:67-70 ISSN: 0074-0276 Aqueous extracts of seven species used in Brazilian popular medicine (Achyrocline satureoides, Iodina rhombifolia, Desmodium incanum, Baccharis anomala, Tibouchina asperior, Luehea divaricata, Maytenus ilicifolia) were screened to the presence of mutagenic activity in the Ames test (Salmonella/microsome). Positive results were obtained for A. satureoides, B. anomala and L. divaricata with microsomal activation. As shown elsewhere (Vargas et al., 1990) the metabolites of A. satureoides extract also show the capacity to induce prophage and/or SOS response in microscreen phage induction assay and SOS spot chromotest. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PHYTOCHEMISTRY***** Monache GD Botta B Vinciguerra V de Mello JF de Andrade Chiappeta A Antimicrobial isoflavanones from Desmodium canum. In: Phytochemistry (1996 Feb) 41(2):537-44 ISSN: 0031-9422 Bioassay-directed fractionation of Desmodium canum resulted in the isolation and characterization of three antimicrobial isoflavonones. These compounds, namely, desmodianones A, B and C, were assigned the structures 5,7,2'-trihydroxy-6,6"-dimethyl-6"-(4-methylpent-3- enyl)pyrano(2",3";4',5')isoflavanone, 5,2',4'-trihydroxy-7-methoxy-6- methyl-8-(3-methylbut-2-enyl)-is oflavanone, and 5,7,2',4'- tetrahydroxy-6-methyl-5'-(3,7-dimethylocta-2,6-dienyl )-isoflavanone, respectively. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PLANTA MEDICA***** Iwu MM Jackson JE Tally JD Klayman DL Evaluation of plant extracts for antileishmanial activity using a mechanism-based radiorespirometric microtechnique (RAM). In: Planta Med (1992 Oct) 58(5):436-41 ISSN: 0032-0943 Extracts of eleven plants used in Nigerian traditional medicine have been evaluated for possible antileishmanial activity using a radiorespirometric microtest technique based on in vitro inhibition of catabolism of 14CO2 from a battery of 14C-substrates by promastigotes. Of 13 methanol extracts tested, 5 from Gongronema latifolia, Dorstenia multiradiata, Picralima nitida, Cola attiensis, and Desmodium gangeticum, were active at concentrations of 50 micrograms/ml or less against a visceral Leishmania isolate. Registry Numbers: 124-38-9 (Carbon Dioxide) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS***** Addy ME Some secondary plant metabolites in Desmodium adscendens and their effects on arachidonic acid metabolism. In: Prostaglandins Leukot Essent Fatty Acids (1992 Sep) 47(1):85-91 ISSN: 0952-3278 The effects of three chemically different groups of compounds, (triterpenoid saponins, beta-phenylethylamines and tetrahydroisoquinolines), known to be present in Desmodium adscendens, on plasma membrane ion channel, cytochrome P450 NADPH- dependent oxygenation of arachidonic acid, and production of prostaglandins by the cyclooxygenase enzyme system, are described. The very high-conductance calcium-activated potassium ion channel, which is responsible for the maintenance of tone in smooth muscles, was activated by the saponins. The cytochrome P450 NADPH-dependent monooxygenase reaction, which produces epoxy- and hydroxylated eicosanoids from arachidonic acid metabolism, was inhibited by an analogue of the tetrahydroisoquinoline present in the plant. This analogue also acted as a reductant in the prostaglandin synthesizing system using microsomes from ram seminal vesicles. The same system was activated by the beta-phenylethylamines found in the plant material, with the formation of more prostaglandins, the type being dependent on the amount of cyclooxygenase enzyme used and the presence or absence of coenzyme. Registry Numbers: 506-32-1 (Arachidonic Acid) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****YAO HSUEH HSUEH PAO [ACTA PHARMACEUTICA SINICA]***** Yang JS Su YL Wang YL [Studies on the chemical constituents of Desmodium styracifolium (Osbeck) Merr.] In: Yao Hsueh Hsueh Pao (1993) 28(3):197-201 ISSN: 0513-4870 (Published in Chinese) A new alkaloid, named desmodimine, C12H15NO4, gum, and a new natural product, named desmodilactone, C8H13NO3, mp 84-85 degrees C have been isolated from the aerial parts of Desmodium styracifolium (Osbeck) Merr. belonging Leguminosae. On the basis of spectral analysis their structures were deduced as formula I and II. In addition, lupenone (III), lupeol (IV), tritriacontane (V), stearic acid (VI), eicosanoic acid eicosyl ester (VIII) and beta-sitosterol (VII) were isolated for the first time from this plant. Registry Numbers: 150036-83-2 (desmodimine) 60010-74-4 (desmodilactone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€