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Erik Bersanetti Alessandro Pasini Gabriella Pezzoni Graziella Pratesi Guiseppina Savi Rossana Supino Franco Zunino 《Inorganica chimica acta》1984,93(4):167-172
In the search for a fine modulation of cisplatin analogues we have synthesized complexes with two different inert ligands bound to platinum in the cis- position. This paper reports on compounds of formula cis-[PtCl2(aaH)(tba)] (aaH, amino acid; tba, tert-butylamine). These complexes have been synthesized with the aim of obtaining liposoluble cisplatin analogues bound to natural carrier groups. The derivatives of glycine, D-alanine, L-threonine, and L-serine were found to be moderately active against murine P388 and L1210 leukemia models. The compound K[PtCl3(tba)] was also found to be active against the same tumor models. Their activity and potency was, however, much lower than that of cisplatin. 相似文献
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D Dardevet I Savary-Auzeloux D Remond L Mosoni E Marzetti TW Buford R Bernabei IJ Dionne TW Buford E Marzetti TM Manini B Buehring E Kirchner L Calabrese TM Manini BC Clark HM Fonseca O Delbono JR Taylor M Aubertin-Leheudre S Barbat-Artigas CH Pion LE Thornell T Gustafsson T Cederholm B Ulfhake 《Journal of applied physiology (Bethesda, Md. : 1985)》2012,113(4):680-684
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The same isoform of ryanodine receptor (RYR1) is expressed in both fast and slow mammalian skeletal muscles. However, differences
in contractile activation and calcium release kinetics in intact and skinned fibers have been reported. In this work, intracellular
Ca2+ transients were measured in soleus and extensor digitorum longus (EDL) single muscle fibers using mag-fura-2 (K
D
for Ca2+= 49 μm) as Ca2+ fluorescent indicator. Fibers were voltage-clamped at V
h
=−90 mV and sarcoplasmic reticulum calcium release was measured at the peak (a) and at the end (b) of 200 msec pulses at +10 mV. Values of a-b and b were assumed to correspond to Ca2+-gated and voltage-gated Ca2+ release, respectively. Ratios (b/a-b) in soleus and EDL fibers were 0.41 ± 0.05 and 1.01 ± 0.13 (n= 12), respectively. This result suggested that the proportion of dihydropyridine receptor (DHPR)-linked and unlinked RYRs
is different in soleus and EDL muscle. The number of DHPR and RYR were determined by measuring high-affinity [3H]PN200-110 and [3H]ryanodine binding in soleus and EDL rat muscle homogenates. The B
max values corresponded to a PN200-110/ryanodine binding ratio of 0.34 ± 0.05 and 0.92 ± 0.11 for soleus and EDL muscles (n= 4–8), respectively. These data suggest that soleus muscle has a larger calcium-gated calcium release component and a larger proportion of DHPR-unlinked RYRs.
Received: 31 August 1995/Revised: 25 January 1996 相似文献
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Moreno RJ Messi ML Zheng Z Wang ZM Ye P D'Ercole JA Delbono O 《The Journal of membrane biology》2006,212(3):147-161
We investigated the effects of exclusive and sustained transgenic overexpression of insulin-like growth factor (IGF)-I in
the central nervous system (CNS) on the age-dependent decline in muscle strength, excitation-contraction coupling, muscle
innervation and neuromuscular junction postterminal architecture. We found that (1) transgenic IGF-I overexpression in the
CNS does not modify the decline in extensor digitorum longus (EDL) and soleus muscle weight with aging and (2) strength significantly
decreases in transgenic (Tg) compared to wild-type mice. The latter finding is consistent with (3) the decreased absolute
and specific force measured in the EDL muscle in vitro and (4) the decreased charge movement and peak intracellular Ca2+ mobilization in individual muscle fibers from old IGF-I Tg mice compared to young wild-type mice, which also is associated
with (5) decreased dihydropyridine receptor α1-subunit expression in old compared to young IGF-I Tg mice. (6) Tg IGF-I prevents a change in muscle fiber type that is associated
with (7) improved muscle innervation and postterminal neuromuscular structure. (8) IGF-I is expressed extensively across the
spinal cord gray matter and the lateral motor column. Our results raise questions about the timing and cell location of CNS
IGF-I overexpression necessary to prevent or to ameliorate age-dependent alterations in the structure and function of skeletal
muscle.
Ramón Jiménez Moreno and María Laura Messi contributed equally to this work. 相似文献
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Patch-clamp recording of charge movement, Ca(2+) current, and Ca(2+) transients in adult skeletal muscle fibers 总被引:1,自引:0,他引:1 下载免费PDF全文
Intramembrane charge movement (Q), Ca(2+) conductance (G(m)) through the dihydropyridine-sensitive L-type Ca(2+) channel (DHPR) and intracellular Ca(2+) fluorescence (F) have been recorded simultaneously in flexor digitorum brevis muscle fibers of adult mice, using the whole-cell configuration of the patch-clamp technique. The voltage distribution of Q was fitted to a Boltzmann equation; the Q(max), V(1/2Q), and effective valence (z(Q)) values were 41 +/- 3.1 nC/&mgr;F, -17.6 +/- 0.7 mV, and 2.0 +/- 0.12, respectively. V(1/2G) and z(G) values were -0.3 +/- 0.06 mV and 5.6 +/- 0.34, respectively. Peak Ca(2+) transients did not change significantly after 30 min of recording. F was fit to a Boltzmann equation, and the values for V(F1/2) and z(F) were 6.2 +/- 0.04 mV and 2.4, respectively. F was adequately fit to the fourth power of Q. These results demonstrate that the patch-clamp technique is appropriate for recording Q, G(m), and intracellular [Ca(2+)] simultaneously in mature skeletal muscle fibers and that the voltage distribution of the changes in intracellular Ca(2+) can be predicted by a Hodgkin-Huxley model. 相似文献
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