Design and efficient synthesis of a new scaffold based on unsymmetrical protoporphyrin IX derivatives for use in SPPS.

Fmoc-protected amine derivatives of Protoporphyrin IX were synthesized by two original methods using solid-phase chemistry. The new compounds represent unsymmetrical scaffolds suitable for the generation of a large range of peptidic porphyrin derivatives through SPPS strategy.

Effects of short- and long-term detraining on the metabolic response to endurance exercise.

Changes in the metabolic response to an endurance exercise were studied (18 rowing km at 75 % of maximal aerobic velocity) during detraining in ten rowers previously highly-trained. Maximal aerobic velocity (VO2 max) and the metabolic response to exercise were determined in the 1 st, 24 th, and 47 th week (training), and in the 52 nd, 76 th, and 99 th week (detraining). Over the decrease of VO2 max, detraining induced a biphasic alteration of the previously observed training adaptations: 1-short-term detraining (5 weeks) resulted in a lower adipose tissue triglyceride (TG) delivery during exercise (p = 0.029), but this one did not represent a direct metabolic limit to exercise since the liver TG delivery increased (p = 0.039), allowing that total fatty acid concentration remained unchanged (12.1 +/- 2.4 vs. 11.8 +/- 2.1 mmol/l; weeks 47 vs. 52); 2-long-term detraining (52 weeks) altered even more the metabolic response to exercise with a decreased total fatty acid concentration during exercise (week 99: 10.6 +/- 2.0 mmol/l; p = 0.022), which induced a higher glycolysis utilization. At this moment, a hemolytic response to endurance exercise was observed through haptoglobin and transferrin concentration changes (weeks 47 vs. 99; p = 0.029 and 0.027, respectively), which resulted probably from higher red blood cell destruction. Endurance-trained athletes should avoid detraining periods over a few weeks since alterations of the metabolic adaptations to training may become rapidly chronic after such delays.

Fourier-transform infrared spectrometry determination of the metabolic changes during a maximal 400-meter swimming test.

We describe the metabolic changes in the blood that appeared during a maximal 400-m swimming test in 7 male swimmers by Fourier-transform infrared spectrometry (FT-IR spectrometry). A 400-m test (255.9 +/- 6.8 s) was performed during which stroke frequency and time to complete each pool distance were recorded. In three other tests, the first 100 m, 200 m, and 300 m were swam at the same stroke frequency and velocity. Capillary blood samples were taken at rest and after tests to analyze change in plasma contents by FT-IR spectrometry. Best swimmers were characterized by higher glycemia increase at the onset of exercise (r = -0.91; p < 0.01). Lactate increase was also higher after 300 m (r = -0.97; p < 0.01). Higher amounts of fatty acids were also available at the end of exercise, as assessed by the relationships found between swimming velocity and concentrations of albumin (r = 0.96; p < 0.01), apolipoprotein C 3 (r = 0.93; p < 0.01), triglycerides (r = -0.81; p < 0.05), and fatty acids (r = 0.97; p < 0.01). This metabolic response allowed the best swimmers to maintain longer their initial swimming velocity. The best swimmers presented also higher amino-acid concentration increase during exercise (r = 0.91; p < 0.01). Therefore, performance competence originated probably from better regulation in carbohydrate, lipid, and amino-acid metabolism.

Vascular endothelial cell growth factor (VEGF), an emerging target for cancer chemotherapy.

Angiogenesis is a process of development and of growth of new capillary blood vessels from pre-existing vessels. When pathological, it contributes to the development of numerous types of tumors, and the formation of metastases. In order to grow, carcinoma need new blood vessels to form so that they can feed themselves. Therefore, nowadays the concept according to which the development of cancer is angiogenesis dependent is generally recognized. This concept makes the control of tumoral angiogenesis one of the promising therapeutic ways in cancerology. The transition from the latent phase to the invasive and metastatic phase of a cancer is linked to what is called the angiogenic switch. It implies complex cellular and molecular interactions between cancerous cells, endothelial cells and the components of the extra-cellular matrix and namely the existence of specific proteins secreted by the tumoral cells able to stimulate the proliferation of capillary endothelial cells. Among them, VEGF, Vascular Endothelial Growth Factor was found in several types of tumors. It has shown a tumoral angiogenic activity in vitro and in vivo, and thus is a privileged target for the control of angiogenesis in an anti-tumoral goal. The role of VEGF in tumoral angiogenesis has been extensively studied. It has been proved to undergo as well autocrine as paracrine stimulation of tumoral angiogenesis. During the last few years, several members of the VEGF family have been described namely the VEGF-A, B, C, D, E and placenta growth factor (PlGF) among which VEGF-A (121 aminoacids) plays a role of prime importance in angiogenesis. VEGF is a 45 kDA glycoprotein, homodimeric, basic, and able to bind heparin. The three-dimensional structure of VEGF has been recently determined, by X-rays diffraction, and NMR spectroscopy. The different forms of the VEGF bind to receptors that exhibit a tyrosine-kinase activity (RTK). The specific action of the VEGF on the endothelial cells is mainly regulated by two types of RTK of the VEGF family, VEGFR1, or Flt-1, and VEGFR2, or KDR/Flk-1. Mutagenesis studies have shown that only a small number of VEGF residues are important and essential for the binding with RTK. Data described to date from the studies of VEGF/RTK interactions agree to the hypothesis that KDR receptor is the main human receptor responsible for the VEGF activity in both physiological and pathological vascular development, and VEGF-KDR signalling pathway has been validated as a priority target for the development of anti- and pro- angiogenic agents. Therefore angiogenesis mediated by VEGF constitutes a new target for anti-cancer therapy which has explored through different ways of intervention aiming at the blocking of the tumoral angiogenesis. The main ones are: -Struggle against the stroma degradation and invasion by the neo-vessels -Inhibition of activated endothelial cells. -Inhibition of angiogenic factors production and of their receptors. -Inhibition of the VEGF signal pathway, by peptides blocking the bond between VEGF and its receptors through the inhibition of intracellular transduction of VEGF signal. In conclusion, this bibliographic study allows to situate works of medicinal chemistry in the context of present knowledge concerning the vascular endothelial growth factor (VEGF) and its role in angiogenesis.

The biological and metabolic adaptations to 12 months training in elite rowers.

We studied the effects of a twelve months endurance-training program on exercise-induced change in blood contents in thirteen rowers. A standardized testing-session (18 km rowing at 80 % of VO2max) was performed 19 times during the training program. Capillary blood samples were taken at rest and immediately post-exercise to analyse a wide range of serum concentrations. During exercise, glucose and lactate concentrations stabilized after only five training weeks and did not evolve from that point. Transport and hepatic protein concentrations increased with exercise up to the 15th week (p = 0.03), and remained stable from that point (p = 0.02). Evolution of exercise-induced change in alpha 1 -acid glycoprotein concentration revealed protein metabolism adaptations to training. Change in alpha 1 -acid glycoprotein concentrations were exactly opposite to that of urea and alpha 1 -antitrypsin (p = 0.01 and 0.002, respectively). Immunoglobulin concentrations exhibited important increases up to the 6th training week (p < 0.05), and a global stabilization was observed from that point. However, analysis of IgG subclasses highlighted significant changes that could not be found with the study of total IgG concentrations. Evolution of the exercise-induced change in Apo-A 1 /Apo-B concentrations ratio was also more informative about lipid metabolism than the Apo-A 1 and Apo-B concentrations taken individually. Indeed, evolution of metabolic changes during exercise should be carefully monitored during training to avoid interpretative errors on the training status of athlete.

Discriminant serum biochemical parameters in top class marathon performances.

Blood chemical parameters were analyzed by Fourier-transform infrared spectrometry (notably for determining the concentrations of glucose, lactate, urea, glycerol, triglycerides, and proteins) in 14 top-class marathon runners (133.7+/-4.1 min at marathon, 10.1% difference between extremes) who performed a 10-km run at their individual marathon velocity. Marathon performance level was correlated to glycemia increase during exercise (9% difference between extremes; r=0.93; p<0.005). The best marathon runners presented longer and/or less unsaturated blood fatty acids during exercise (17% difference between extremes; r=0.89; p<0.01), suggesting an improved fatty acid selectivity for muscular metabolism. The marathon performance level was also found correlated to a decrease of blood triglycerides during exercise (r=20.95; p<0.003) and to a proportional glycerol concentration increase (11% difference between extremes; r=0.94; p<0.005). The best marathon runners presented higher amino acid blood delivery (r=0.88; p<0.01), which was correlated to an apparent protein catabolism. These results show that the best runners have enhanced both carbohydrate, lipid, and amino acid metabolisms to improve energetic supply to skeletal muscle during exercise.

Sensitivity of Deinococcus radiodurans to gamma-irradiation: a novel approach by Fourier transform infrared spectroscopy.

Deinococcus radiodurans is a red-pigmented coccus known to be particularly resistant to both chemical and radiative agents. Fourier transform infrared (FT-IR) spectroscopy was used as a convenient and easy-to-run method to monitor damage induced in this bacterium by ionizing radiations. First, stationary-phase cultures were submitted to increasing doses of gamma-irradiation ((137)Cs source). Beyond a threshold of 11 kGy, striking changes occurred in spectra of irradiated samples compared with unirradiated ones, especially in the 1750-900 cm(-1) region, which is spectroscopically assigned to amide I and II components, nucleotide bases, the phosphodiester backbone, and the sugar ring. Second, bacterial cultures were postirradiation reincubated. After a reincubation time of 15 h, the oxidative stress was in part overwhelmed, and the growth of D. radiodurans again occurred, although some biocellular components remained altered. Consequently, FT-IR analysis is an accurate means to rapidly visualize biomolecular changes undergone by cells both after gamma-irradiation and during the repair mechanism.

The in vivo toxicity of carbon tetrachloride and carrageenan on heart microsomes: analysis by Fourier transform infrared spectroscopy.

We investigated the sensitivity of rat heart microsomes to free radical attack using Fourier transform infrared (FT-IR) spectroscopy. This physico-chemical method seemed a valuable technique: quite sensitive to changes in the vibrational spectra. The spectral variations observed between normal and treated rats were in great part due to reactive oxygen species that led to changes in protein conformation involving beta-sheets, aggregation of proteins, and modification of protein synthesis. Carrageenan-induced inflammation slightly enhanced the total lipid content; rearrangement of acyl chains and accumulation of cholesterol esters and phospholipids also occurred in the treated rats. Carbon tetrachloride induced a decrease in both lipid and protein contents. The level of glucidic substrates was diminished with carbon tetrachloride and enhanced with carrageenan; these changes were due to metabolic interactions between cell components and drugs. FT-IR spectroscopy provided an accurate means to monitor, in rat heart, the in vivo effects of inflammatory and peroxidative damages, to discriminate and classify the affected cells, and to correlate the findings with known physiological and biochemical data in close relationship with metabolic disruptions induced by the two xenobiotics.

Enzymatic hydrolysis of (chloromethyldimethylsilyl)-2-propenyl acetate isomers: atypic specificity of Candida antarctica lipase.

Enzymatic hydrolysis of a mixture of (chloromethyldimethylsilyl)-2-propenyl acetate isomers was investigated by using immobilized Candida antarctica lipase as biocatalyst. TLC analysis and 1H NMR spectroscopy were used to monitor the extent of the reaction. At 60 degrees C, the enzyme exhibited a high selectivity towards 3-(chloromethyldimethylsilyl)-2-propenyl acetate which was almost quantitatively hydrolyzed, whereas, only 11% of 2-(chloromethyldimethylsilyl)-2-propenyl acetate reacted with the lipase. Consequently, the unreacted acetate was readily purified from the reaction medium by flash column chromatography and deacetoxylated in acidic methanol to give the corresponding hydroxy compound in a 71% global yield. On the other hand, without lipase, chemical treatment of the acetate mixture resulted in much lower yields in hydroxy compounds followed by a tedious purification process.

[Clinical diagnosis of overtraining using blood tests: current knowledge]. / L'étiologie clinique du surentraînement au travers de l'examen sanguin: état des connaissances.

PURPOSE: Overtraining results from an imbalance between training load-induced fatigue and organism's recovery abilities. Its etiology is complex and to date there is no useful clinical diagnostic tool. The purpose of this review is to discuss the blood chemistry parameters potentially useful for diagnosing overtraining in athletes. CURRENT KNOWLEDGE AND KEY POINTS: Chronic alterations of the myocyte structure may cause high plasma concentration increases of myoglobin, troponin I and creatine kinase enzyme, resulting in chemical and/or mechanical aggression. Monitoring reactive oxygen species' activity appears to be a good tool for evaluation of the metabolic stress level experienced by skeletal muscles. In energetic metabolism, a succession of chronic glycogen depletions might change the use of amino acids and lipids, inducing transient but severe hypoglycemia during exercise. A higher oxidation of circulating glutamine might cause immunosuppression (lower reactivity to inflammations and cellular traumatisms), inhibiting alarm signals during acute training. A higher branched-chain amino acid oxidation might favor free tryptophan's entry into the cerebral area, enhancing serotonin synthesis. As a consequence, asthenia and a loss of sensitivity to muscular and tendon traumatism might appear. Exercise anemia might also be a worsening factor of the physiological situation of the tired athlete, inducing predisposition to overtraining by the lower inflammation reactivity of depleted hepatic and muscular proteins. FUTURE PROSPECTS AND PROJECTS: Early diagnosis of overtraining diagnosis may be established only from a battery of analyses, which should include the whole of the potential parameters. These remain unpredictable and do not allow systematic determination of new cases. Only a longitudinal study of the physiological situation appears to allow the necessary conditions for detecting overtraining in the early stages of its process for each subject.

Fourier-transform infrared spectroscopy: a pharmacotoxicologic tool for in vivo monitoring radical aggression.

Among the physico-chemical methods that can be used to investigate induced peroxidation in living cells, Fourier transform infrared (FT-IR) spectroscopy appears to be a valuable technique as it is non-destructive and sensitive for monitoring changes in the vibrational spectra of samples. We examined microsomal fractions from rat liver and brain by FT-IR to study the effect of radical aggression induced in vivo by carbon tetrachloride (CCl4). The length of the acyl chains was increased as a consequence of peroxidation induced by the xenobiotic. Moreover, an enhanced level of cholesterol esters and an increase in phospholipids were observed in the liver and the brain, respectively. The conformational structure of the membrane proteins was changed in both the liver and the brain. In the polysaccharide region, we observed an important loss in glucidic structures, such as a decrease in liver glycogen and in some brain glycolipids. These alterations are probably due to the interactions between cells and CCl4 and the metabolic changes caused by CCl4. Thus, FT-IR spectroscopy appears to be an useful tool and an accurate means for rapidly investigating the in vivo biochemical alterations induced by CCl4 in microsomes, and for correlating them with biochemical and physiological data.

Plasma protein contents determined by Fourier-transform infrared spectrometry.

BACKGROUND: Fourier-transform infrared (FT-IR) spectrometry has been used to measure small molecules in plasma. We wished to extend this use to measurement of plasma proteins. METHODS: We analyzed plasma proteins, glucose, lactate, and urea in 49 blood samples from 35 healthy subjects and 14 patients. For determining the concentration of each biomolecule, the method used the following steps: (a) The biomolecule was sought for which the correlation between spectral range areas of plasma FT-IR spectra and concentrations determined by comparison method was greatest. (b) The IR absorption of the biomolecule at the most characteristic spectral range was calculated by analyzing pure samples of known concentrations. (c) The plasma concentration of the biomolecule was determined using the FT-IR absorption of the pure compound and the integration value obtained for the plasma FT-IR spectra. (d) The spectral contribution of the biomolecule was subtracted from the plasma FT-IR spectra, and the resulting spectra were saved for further analyses. (e) The same method was then applied to determining the concentrations of other biomolecules by sequentially comparing the resulting FT-IR spectra. RESULTS: Results agreed with those obtained by clinical methods for the following biomolecules when analyzed in the following order: albumin, glucose, fibrinogen, IgG(2), lactate, IgG(1), alpha(1)-antitrypsin, alpha(2)-macroglobulin, transferrin, apolipoprotein (Apo)-A(1), urea, Apo-B, IgM, Apo-C(3), IgA, IgG(4), IgG(3), IgD, haptoglobin, and alpha(1)-acid glycoprotein. CONCLUSION: FT-IR spectrometry is a useful tool for determining concentrations of several plasma biomolecules.

Differentiation of populations with different physiologic profiles by plasma Fourier-transform infrared spectra classification.

The pathologic condition of a patient presenting a metabolic disease can change rapidly, and a variety of pathologic conditions are possible. Plasma Fourier-transform infrared (FT-IR) spectra were used to differentiate patients with type 1 diabetes, healthy subjects, and endurance-trained rowers. Analytic and classification methods that use the same plasma FT-IR spectra are described. Complete spectra (4000 to 500 cm(-1)) classifications led to a differentiation between most patients with type 1 diabetes and other subjects but not between control and trained subjects. Classification of defined absorption regions of spectra allowed different metabolic distinctions between populations. These were performed on the amide I and II absorption regions of proteins (1720 to 1480 cm(-1)); on the nu=CH, nu(as)CH(2), and nu(as)CH(3) absorption regions of lipids (3020 to 2880 cm(-1)); and on the nuC-O absorption region of saccharides (1300 to 900 cm(-1)). A classification that uses a combination of four absorption regions-nu=CH (3020 to 3000 cm(-1)), nu(as)CH(3) (3000 to 2950 cm(-1)), nuC-O (amide I: 1720 to 1600 cm(-1)), and nuC-O (carbonyle: 1300 to 900 cm(-1))-led to the formation of three exclusive clusters that comprised the defined populations. FT-IR spectroscopy is an exciting technique that allows a versatile approach to biologic samples from which analytic and statistical methods might be used for metabolic profile characterization and evaluation.

FT-IR spectroscopy utilization to sportsmen fatigability evaluation and control.

PURPOSE: A longitudinal biological study of 20 elite rowers was performed using capillary blood (serum) FT-IR spectra to evaluate their training load adaptations and fatigue. METHODS: Difference spectra (rest serum spectra subtracted to exercise serum spectra) were used to evaluate subjects' metabolic response to exercise. Spectra classifications were used for serum contents differentiation on the basis of biomolecular absorption. RESULTS: For two subjects, several metabolic differentiations were observed. These started with sugars metabolism on the fifth training week, followed successively by lipid metabolism and protein metabolism, when overtraining was clinically diagnosed. Several weeks further into the training program, the same onset of metabolic differentiations was observed for eight other subjects. When differentiations reached lipid metabolism, they were asked to reduce their training loads. Unlike the overtrained subjects, a rapid recovery was observed (3 vs 22 wk) and metabolism alterations disappeared. CONCLUSION: The fatigability limit in sportsmen seemed to be situated at a certain level of metabolic stress, beyond which a rapid overtraining process recover was no longer possible.

Perspectives in the utilisation of Fourier-transform infrared spectroscopy of serum in sports medicine: health monitoring of athletes and prevention of doping.

Doping prevention is mainly directed to providing information on the dangers of doping to young athletes and to every profession concerned with athletic performance. Unfortunately, repression is also necessary in the fight against doping. Measurement of performance-enhancing drugs is complex, partly because of the large number of prohibited substances. A number of sophisticated analytical techniques are increasingly being used to provide the maximum detection time window. However, the effectiveness of methods to separate exogenous from endogenous biological molecules and the cost of antidoping analyses makes controls invalid or impossible. Moreover, most athletes, because of the metabolic and psychological stresses caused, legitimately refuse blood testing. It is becoming crucial to introduce new methods in the form of longitudinal health monitoring, since this is probably the most effective tool to prevent the use of doping agents when athletes become overtrained and/or overstressed. This paper describes new methods using Fourier-transform infrared spectroscopy to analyse serum from 50 microl samples of capillary blood. This technique has been shown to allow determination of the concentration of a wide range of biological molecules in a single microsample with clinically useful accuracy, and to provide a 'discriminatory biomolecular profile' to differentiate individuals on the basis of their physiological status. A specific application of this methodology is to perform longitudinal health monitoring in athletes, allowing prevention of overtraining. It is proposed to apply such methods in longitudinal studies for health monitoring and prevention of doping.

Pharmacologic application of fourier transform IR spectroscopy: in vivo toxicity of carbon tetrachloride on rat liver.

Microsomal fractions from rat liver were examined by means of Fourier transform IR (FTIR) spectroscopy to study the in vivo toxic effect of carbon tetrachloride administered by intraperitoneal injection. Lipid content was significantly enhanced in the liver of treated rats compared with untreated ones. The level of saturated fatty acids largely increased while that of unsaturated acids slightly decreased as a consequence of lipid peroxidation induced by the xenobiotic compound. The conformational structure of membrane proteins was changed, which was shown by the large decrease in the alpha-helical configuration. In the polysaccharide region we observed an important loss in glucidic structures that could be related to the metabolic changes caused by carbon tetrachloride intoxication. Thus, FTIR spectroscopy appears to be a useful tool to rapidly investigate the chemical alterations induced by this drug in liver microsomes and to correlate them with biochemical and physiological data.

Glucose and lactate concentration determination on single microsamples by Fourier-transform infrared spectroscopy.

This study is the first to assess the analytic potential of Fourier-transform infrared (FT-IR) spectroscopy in determining exercise-induced metabolic changes, such as glucose and lactate serum concentrations, with single 50 microL blood microsamples. One-hundred ninety-eight capillary blood samples were taken at rest (rest serum) and after rowing exercises at different intensities (exercise serum) to obtain a wide range of lactate concentrations. A quantitative method is described with FT-IR spectroscopy involving only dilution and dessiccation of serum samples. Within serum spectra, an absorption band was strongly specific of glucose (1033 cm(-1)) that allowed the determination of its concentration (r = 0.97; P < .001 with reference values). Once we had substrated measured glucose absorption in serum spectra, one other absorption band seemed to be specific for lactate (1127 cm(-1)), which allowed the determination of the concentration of this metabolite (r = 0.96; P < .001 with reference values). The convenience of a capillary blood sampling with the strong accuracy of FT-IR measurements is of particular interest for medicinal and biologic concerns.

Pharmacologic application of FTIR spectroscopy: effect of ascorbic acid-induced free radicals on Deinococcus radiodurans.

Fourier transform infrared (FTIR) spectroscopy was used as a convenient and easy-to-run method to monitor radical-induced damage on the radiation-resistant Deinococcus radiodurans strain. Increasing concentrations of ascorbic acid added to the culture medium during the stationary phase produced striking changes in the infrared spectra. These changes especially occurred in the 1700-900 cm(-1) region, which is spectroscopically assigned to the amide I and II components, nucleotide bases, phosphodiester backbone and sugar rings, and were correlated with the oxidant effect of ascorbic acid. Thus, FTIR analysis allows a rapid characterization of the changes induced by ascorbic acid in the cell environment, which can be correlated in part with the generation of free radicals. Beyond a critical ascorbic acid concentration of 40 mM, these free radicals can cause severe damage to the biomolecular components, as soon as the antioxidant defenses of the bacterium are overwhelmed.

Determination of glucose in dried serum samples by Fourier-transform infrared spectroscopy.

BACKGROUND: Practical improvements are needed to allow measurement of glucose concentrations by Fourier- transform infrared (FT-IR) spectroscopy. We developed a new method that allows determination of the glucose concentration in dried sera. METHODS: We studied 32 serum samples after fourfold dilution and desiccation before FT-IR analyses on a spectrometer operated at a resolution of 2.0 cm(-1). We integrated all spectral windows at the surface of the spectrum in the C--O region. For comparison, glucose was measured in the sera by a glucose oxidase method. RESULTS: One peak within the spectrum was most specific for glucose (997-1062 cm(-1)). Its surface integration showed a strong relationship with reference data (r = 0.998; P <0.001). FT-IR analyses of five glucose solutions were performed to determine its specific absorption at the same peak. In this way, glucose concentrations in serum spectra could be measured. For the first time while using FT-IR spectroscopy, no manipulation of spectra nor use of internal standard was necessary to obtain results in high accordance with glucose concentration measured by a conventional (glucose-oxidase) method (S(y|x) = 0.25 mmol/L; r = 0. 998). CONCLUSIONS: FT-IR spectroscopy appears to be an easy and accurate method to determine glucose concentration and could be widely used to simultaneously identify and quantify several metabolites in biological fluids or tissues.

Synthesis and evaluation of the in vivo trypanocidal activity of water soluble organotin compounds.

A series of (3-(2-methoxy)ethoxypropyl)tin derivatives were synthesized as potential trypanocidal drugs. The series included an alkyltin trichloride, a dialkyltin dichloride and the corresponding dialkyltin oxide, and six dialkyltin dithio derivatives. Compounds were evaluated for trypanocidal activity using in vitro cultures of Trypanosoma equiperdum and mice infected with the same strain of parasite for in vivo tests. Two of the title derivatives, the bis (3-(2-methoxy)ethoxypropyl)tin dichloride 2 and the corresponding bis (3-(2-methoxy)ethoxypropyl)tin oxide 3, appeared to be water soluble reagents. Furthermore, they are the first examples of organotin compounds presenting interesting in vivo trypanocidal activity.