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1.
RSC Adv ; 8(59): 34162-34167, 2018 Sep 28.
Article in English | MEDLINE | ID: mdl-35548818

ABSTRACT

Diagnostic nanomedicine constantly requires the development of novel contrast agents with intrinsic imaging capabilities. Phosphorescent Ir(iii)-complexes represent good candidates when delivered through polymeric nanoparticles. In this work, we propose a biocompatible nanoparticle made from an intrinsically phosphorescent copolymer, synthesized directly with an imaging tag present on its backbone. Polymeric nanoparticles can be obtained with the exact amount of phosphorescent moieties needed to maximize their output signal. Complete characterization and ex vivo studies confirmed that this nanosystem is suitable as a future diagnostic tool.

2.
Eur J Med Chem ; 117: 1-7, 2016 Jul 19.
Article in English | MEDLINE | ID: mdl-27081742

ABSTRACT

In this paper a straightforward synthesis of a novel pyrazole derivative is reported. Prominent feature of this synthetic process is a 1,3-Dipolar Cycloaddition of a suitable nitrile imine with an activated α,ß-unsaturated lactam to afford directly and regioselectively the corresponding ring-fused pyrazole. Having obtained the central core of the synthetic target, a double stepwise functionalization with a "side chain" characterized by a terminal cyclic aliphatic amine was carried out. This molecular structure was designed to interact strongly with typical biological residues, and indeed it showed potent anticancer capability: in vitro cytotoxicity test on five different cancer cell lines showed interesting IC50 values in the range of 15-60 µM for exposure time of 24-72 h, thus resulting comparable with commercially available and nowadays therapeutically exploited anticancer compounds, such as 5-FU and NVP-BEZ235.


Subject(s)
Antineoplastic Agents/chemical synthesis , Pyrazoles/chemical synthesis , Amino Acids, Cyclic/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cycloaddition Reaction , Drug Design , Humans , Imines/chemistry , Lactams/chemistry , Nitriles/chemistry , Pyrazoles/pharmacology
3.
J Evol Biol ; 18(1): 101-5, 2005 Jan.
Article in English | MEDLINE | ID: mdl-15669965

ABSTRACT

Because mortality accumulates with age, Fisher proposed that the strength of selection acting on survival should increase from birth up to the age of first reproduction. Hamilton later theorized that the strength of selection acting on survival should not change from birth to age at first reproduction. As organisms in nature do not live in uniform environments but, rather, experience periodic stress, we hypothesized that resistance to environmental stress should increase (Fisher) or remain constant (Hamilton) from birth to age at first reproduction. Using the pitcher-plant mosquito, Wyeomyia smithii, we imposed heat stress by simulating the passage of a warm-weather front at different pre-adult and adult stages. Contrary to either Fisher or Hamilton, stress tolerance declined from embryos to larvae to pupae to adults. Consequently, reproductive value appears to have been of little consequence in the evolution of stage-specific tolerance of heat stress in W. smithii.


Subject(s)
Culicidae , Hot Temperature , Reproduction , Adaptation, Physiological , Animals , Biological Evolution , Female , Male , Survival
4.
Proc Natl Acad Sci U S A ; 94(8): 3828-32, 1997 Apr 15.
Article in English | MEDLINE | ID: mdl-9108063

ABSTRACT

We compared morphology of two geographically close populations of the tropical lizard Tropidurus hispidus to test the hypothesis that habitat structure influences the evolution of morphology and ecology at the population level. T. hispidus isolated on a rock outcrop surrounded by tropical forest use rock crevices for refuge and appear dorsoventrally compressed compared with those in open savanna. A principal components analysis revealed that the populations were differentially distributed along an axis representing primarily three components of shape: body width, body height, and hind-leg length. Morphological divergence was supported by a principal components analysis of size-free morphological variables. Mitochondrial DNA sequences of ATPase 6 indicate that these populations are closely related relative to other T. hispidus, the rock outcrop morphology and ecology are derived within T. hispidus, and morphological and ecological divergence has occurred more rapidly than genetic divergence. This suggests that natural selection can rapidly adjust morphology and ecology in response to a recent history of exposure to habitats differing in structure, a result heretofore implied from comparative studies among lizard species.


Subject(s)
Biological Evolution , Lizards/genetics , Animals , Base Sequence , DNA, Mitochondrial/analysis , DNA, Mitochondrial/genetics , Molecular Sequence Data , Sequence Alignment , Sequence Analysis, DNA
5.
Am J Physiol ; 261(3 Pt 2): R626-32, 1991 Sep.
Article in English | MEDLINE | ID: mdl-1887950

ABSTRACT

Although several vertebrates are freeze tolerant, little is known of the relationship between body size and the kinetics of cooling and freezing. We compared these responses for six hatchling and eight adult Chrysemys picta from an Ohio population. All turtles initially recovered from freezing, and all adults, but only two hatchlings (which experienced ice contents of approximately 35%), exhibited long-term survival. Rapid thawing may have compromised hatchling survival. Turtle water content was inversely related to body mass, but we found no significant correlation between the extent of supercooling and body size. Prefreezing and postfreezing cooling rates scaled with body mass to the -0.55 and -0.40 power, respectively, but the latter rate was more than two orders of magnitude slower. Theoretical (assuming 20% bound water) and calorimetric estimates of body ice agreed reasonably well. Ice contents were both body mass and time dependent. The absolute rate of ice formation scaled with body mass to the 0.4 power. Body size strongly influences the freezing response of ectotherms and deserves more attention.


Subject(s)
Body Temperature Regulation , Body Temperature , Turtles/physiology , Aging/physiology , Animals , Body Constitution , Body Weight , Cold Temperature , Freezing , Time Factors
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