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Antithrombotic Effect of Chikusetsusaponin IVa Isolated from Ilex paraguariensis (Maté)
Tabitha Dahmer,Markus Berger,Adriana Gregory Barlette,Jose´ Reck Jr.,Je´ferson Segalin,Simone Verza,George Gonza´lez Ortega,Simone Cristina Baggio Gnoatto,Jorge Almeida Guimara˜es,Hugo Verli,Grace Gos 한국식품영양과학회 2012 Journal of medicinal food Vol.15 No.12
The triterpene chikusetsusaponin IVa was isolated from the fruit of Ilex paraguariensis. Using biochemical and pharmacological methods, we demonstrated that chikusetsusaponin IVa (1) prolongs the recalcification time, prothrombin time, activated partial thromboplastin time, and thrombin time of normal human plasma in a dose-dependent manner, (2) inhibits the amidolytic activity of thrombin and factor Xa upon synthetic substrates S2238 and S2222, (3) inhibits thrombin-induced fibrinogen clotting (50% inhibition concentration, 199.4±9.1 μM), and (4) inhibits thrombin- and collagen-induced platelet aggregation. The results also indicate that chikusetsusaponin IVa preferentially inhibits thrombin in a competitive manner (Ki=219.6 μM). Furthermore, when administered intravenously to rats, chikusetsusaponin IVa inhibited thrombus formation in a stasis model of venous thrombosis, although it did not induce a significant bleeding effect. Chikusetsusaponin IVa also prolonged the ex vivo activated partial thromboplastin time. Altogether, these data suggest that chikusetsusaponin IVa exerts antithrombotic effects, including minor hemorrhagic events. This appears to be important for the development of new therapeutic agents
Isoquinoline alkaloids supplementation on performance and carcass traits of feedlot bulls
Michels, Alex,Neumann, Mikael,Leao, Guilherme Fernando Mattos,Reck, Angela Maria,Bertagnon, Heloisa Godoi,Lopes, Leandro Samia,de Souza, Andre Martins,dos Santos, Leslei Caroline,Stadler, Edelmir Silv Asian Australasian Association of Animal Productio 2018 Animal Bioscience Vol.31 No.9
Objective: Isoquinoline Alkaloids, derived from one plant (Macleaya cordata) can be an alternative when it is desired to increase performance in feedlot cattle. However, results on these nutritional additives in high energy diets in ruminants are still incipient in literature. In this context, the objective of this study was to evaluate performance and carcass traits of feedlot bulls supplemented with sanguinarine, the main alkaloid presents in Macleaya cordata in high energy density diets. Methods: Thirty-two crossbred Angus-Nelore bulls with mean initial body weight of $365{\pm}10kg$ and mean initial age of $11{\pm}3$ months were used. The experiment lasted 119 days, with 14 days of adaptation and 105 experimental days. Experimental diet consisted of 85% whole corn grains and 15% protein-vitamin-mineral nucleus and supplied ad libitum. Treatments consisted of a control diet (CON) and a diet with sanguinarine supplementation (SAN) at a dosage of 4 g of product sufficient to provide 6 mg of sanguinarine/d. Experimental design was completely randomized. Results: Dry matter intake, average daily gain and feed conversion were similar (p>0.05) between treatments. However, SAN group animals had higher carcass yield (p = 0.045) and were more efficient in the transformation of dry matter consumed in carcass gain (p = 0.046) than CON. In addition, haptoglobin, increased throughout feedlot duration meaning high challenge for the animals due to the diet, but this behavior was similar (p>0.05) between treatments. Conclusion: Sanguinarine produced positive results in relation to carcass yield and could be used as an additive for bulls fed diets receiving high energy density diet.
김동원,박성록,강용환,이남기,Dong Won Kim,Song Reck Park,Yong Whan Kang,Nam Kee Rhee 대한화학회 1980 대한화학회지 Vol.24 No.5
용리액으로 염산과 숙신산 및 그들의 혼합액을 사용하고, 강산성 양이온 교환수지, Dowex 50W-x8, 100∼200 mesh 를 사용하여 금속, Mg(Ⅱ), Ca(Ⅱ), Sr(Ⅱ), Ba(Ⅱ), Cr(Ⅲ), Mn(Ⅱ), Fe(Ⅲ), Co(Ⅱ), Ni(Ⅱ), Cu(Ⅱ), Cd(Ⅱ), Hg(Ⅱ) 및 Pb(Ⅱ)의 이온들에 대한 분포계수를 측정하였다. 분리도와 양이온의 전하와의 관계를 고찰하였고, 이온반지름에 따른 분포계수를 비교하였다. 특히 0.9M 염산용액에서 Fe(Ⅲ), Co(Ⅱ), Ni(Ⅱ)의 완전분리가 가능하였다. Distribution coefficients of various elements with the strong acidic caion-exchanger, Dowex 50W-x8, 100∼200 mesh were investigated in various concentrations of succinic, hydrochloic acid and it's mixture. Based on these distribution coefficients,the experimental condition for their quantitative separation of those elements is established in 0.9 M hydrochloric acid as eluent, several examples of successful separations are described and the dependence of distribution coefficients on ionic radius is also discussed.
Edelman, Martin J.,Schneider, Claus-Peter,Tsai, Chun-Ming,Kim, Heung-Tae,Quoix, Elisabeth,Luft, Alexander V.,Kaleta, Remigiusz,Mukhopadhyay, Pralay,Trifan, Ovidiu C.,Whitaker, Laura,Reck, Martin American Society for Clinical Oncology 2013 Journal of clinical oncology Vol.31 No.16
<P><B>Purpose</B></P><P>Retrospective studies have reported that tumor expression of the beta-3 tubulin (β3T) isoform is an unfavorable prognostic factor in non–small-cell lung cancer (NSCLC) treated with tubulin-inhibiting chemotherapy. Ixabepilone is a tubulin-inhibiting agent with low susceptibility to multiple resistance mechanisms including β3T isoform expression in several tumor models. This randomized phase II study evaluated ixabepilone-based chemotherapy in stage IIIb/IV NSCLC, compared with paclitaxel-based chemotherapy. Tumor specimens were prospectively evaluated for β3T expression.</P><P><B>Patients and Methods</B></P><P>Patients were stratified by β3T status (positive <I>v</I> negative) and randomly assigned at a ratio of 1:1 to receive ixabepilone (32 mg/m<SUP>2</SUP>) and carboplatin (area under concentration-time curve [AUC], 6) or paclitaxel (200 mg/m<SUP>2</SUP>) and carboplatin (AUC, 6) for up to six cycles. The primary end point was progression-free survival (PFS) in the β3T-positive subgroup.</P><P><B>Results</B></P><P>Ninety-five patients (β3T positive, 52; β3T negative, 43) received ixabepilone plus carboplatin; 96 patients (β3T positive, 49; β3T negative, 47) received paclitaxel plus carboplatin. No significant differences in median PFS were observed between arms for either subgroup (β3T positive, 4.3 months in both arms; β3T negative, 5.8 <I>v</I> 5.3 months). Ixabepilone did not significantly improve overall survival (OS) for the β3T-positive subset or the overall population. Adverse events were similar between the two arms and comparable with those in previous studies.</P><P><B>Conclusion</B></P><P>There was no predictive value of β3T in differentiating clinical activity of ixabepilone- or paclitaxel-containing regimens. Ixabepilone did not improve PFS or OS in patients with β3T-positive tumors. β3T-positive patients had worse PFS relative to β3T-negative patients, regardless of treatment; hence, β3T expression seems to be a negative prognostic factor, but not a predictive factor, in advanced NSCLC treated with either ixabepilone or paclitaxel platinum-based doublets.</P>
Barlesi, F.,Scherpereel, A.,Gorbunova, V.,Gervais, R.,Vikströ,m, A.,Chouaid, C.,Chella, A.,Kim, J. H.,Ahn, M. J.,Reck, M.,Pazzola, A.,Kim, H. T.,Aerts, J. G,Morando, C.,Loundou, A.,Groen, H. J. M. Oxford University Press 2014 Annals of oncology Vol.25 No.5
<P>The randomized, phase III AVAPERL trial evaluated the safety and efficacy of bevacizumab maintenance with or without pemetrexed in nonsquamous non–small cell lung cancer (nsNSCLC). Progression-free survival (PFS) was significantly prolonged with bevacizumab–pemetrexed. At a median follow-up of 14.8 months, OS events occurred in 58% of all patients. OS was numerically longer with bevacizumab–pemetrexed versus bevacizumab when measured from randomization (17.1 versus 13.2 months, HR, 0.87 [0.63–1.21]; P=0.29). Second-line therapy was administered in 77% and 70% of patients in the bevacizumab and bevacizumab–pemetrexed arms, respectively.</P>