Studies on the in vitro and in vivo degradation behavior of amino acid derivative-based organogels

Introduction.The existence of the active metabolite (amino acid) residue in the of an indolocarbazole molecule changes physical-chemical and pro-medicinal properties of aminoacid derivatives glycosides of indolocarbazole. The computer method has earlier foretold low probability of their cytotoxic activity in vitro that was confirmed in the MTT-test on 5 lines of tumor cells. The same computer method predicted significant probability of antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole in vivo that demands the experimental check. Purpose of the study– assessment of aminoacid derivatives glycosides of indolocarbazole as potential antitumor medications.Materials and methods.The research of antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole was performed on mice tumoral models – cervical cancer СС5. Abdominal injections were made to CBA/Lac mice 5 times a day with 24 h interval. Observation of animals was continued till their death. The antineoplastic effect of medicines was estimated according to tumor growth inhibition, increase in life expectancy of experiental mice in comparison with control animals.Results.The optimum dose for this number of compounds, equal to 100 mg/kg is titrated. The antineoplastic activity of aminoacid derivatives glycosides of indolocarbazole on the model СС5 is estimated.Conclusions.On the basis of the obtained data the expanded research of antineoplastic properties of the selected 5 aminoacid derivatives glycosides of indolocarbazole is supposed to perform in vivo.

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Improvement in the osteoblastic cellular response to a commercial collagen membrane and demineralized freeze-dried bone by an amino acid derivative: an in vitro study

Clinical Oral Implants Research ◽

10.1111/j.1600-0501.2010.01975.x ◽

2010 ◽

Vol 22 (2) ◽

pp. 165-172 ◽

Cited By ~ 13

Author(s):

Masahiro Yamada ◽

Norinaga Kojima ◽

Wael Att ◽

Hajime Minamikawa ◽

Kaoru Sakurai ◽

...

Keyword(s):

Amino Acid ◽

Acid Derivative ◽

Cellular Response ◽

In Vitro Study ◽

Vitro Study ◽

Amino Acid Derivative ◽

Collagen Membrane ◽

Freeze Dried

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In vivo degradation behavior of PDC multiblock copolymers containing poly(para-dioxanone) hard segments and crystallizable poly(epsilon-caprolactone) switching segments

MRS Proceedings ◽

10.1557/proc-1190-nn06-05 ◽

2009 ◽

Vol 1190 ◽

Cited By ~ 3

Author(s):

Bernhard Hiebl ◽

Karl Kratz ◽

Rosemarie Fuhrmann ◽

Friedrich Jung ◽

Andres Lendlein ◽

...

Keyword(s):

Enzymatic Degradation ◽

Degradation Products ◽

In Vivo Studies ◽

Multiblock Copolymers ◽

Degradation Behavior ◽

Hard Segments ◽

In Vivo Degradation ◽

Good Agreement

AbstractThe degradation behavior of biodegradable multiblock copolymers (PDC) containing poly(p-dioxanone) hard segments (PPDO) and crystallizable poly(epsilon-caprolactone) switching segments (PCL) synthesized via co-condensation of two oligomeric macrodiols with an aliphatic diisocyanate as junction unit was explored in in vivo and in vitro experiments. The in vitro experiments for enzymatic degradation resulted that the poly(epsilon-caprolactone) segments are degraded faster, than the poly(p-dioxanone) segments. During degradation the outer layer of the test specimen becomes porous. Finally non-soluble degradation products in form of particles were found at the surface. This observation is in good agreement with the in vivo studies, where the non-soluble degradation products in the periimplantary tissues showed a diameter of 1 – 3 micron.

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alpha-Ketoisocaproate stimulates branched-chain amino acid transaminase in kidney and muscle.

AJP Endocrinology and Metabolism ◽

10.1152/ajpendo.1979.236.5.e514 ◽

1979 ◽

Vol 236 (5) ◽

pp. E514

Author(s):

W E Mitch ◽

W Chan

Keyword(s):

Amino Acid ◽

Rat Kidney ◽

In Vitro Perfusion ◽

Branched Chain Amino Acid ◽

Branched Chain ◽

Increased Activity ◽

In Vivo Degradation ◽

Sequential Measurements

We have reported that branched-chain amino acid transaminase (BATase) activity of isolated rat kidney is stimulated by perfusion with alpha-ketoisocaproate (KL). This study examines the mechanism of this effect in kidney and documents that stimulation occurs in intact skeletal muscle. Increased activity was not attributable to synthesis of enzyme because it occurred in the presence of cycloheximide. The in vivo degradation rate of BATase estimated from sequential measurements of activity following intravenous cycloheximide was longer than 90 min, whereas during in vitro perfusion stimulation could be detected within 5 min. Incubation of supernatant from kidney homogenate with KL stimulated BATase; incubation with alpha-keto-beta-methylvalerate (KI), alpha-ketoisovalerate (KV), leucine (leu), or isovaleryl CoA did not. Perfusion of rat hindquarter with KL increased muscle BATase activity; perfusion with acetoacetate, KI, KV, or leu did not. Again, cycloheximide studies indicated a direct effect of KL on muscle BATase. These findings suggest that alpha-ketoisocaproate can increase BATase activity and thus may be involved in regulation of its activity.

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