Property in vivo

McQuibban GA, Gong JH, Wong JP, Wallace JL, Clark-Lewis I, Overall CM. Matrix metalloproteinase processing of monocyte chemoattractant proteins generates CC chemokine receptor antagonists with anti-inflammatory properties in vivo. Blood 2002 100(4) 1160-1167. 

Protein toxin possessing cytotoxic properties in vivo... 

Protein Features of protein structure Effect on transcription Other properties In vivo expression and localization... 

Isolated cells, tissues, and organs may be grown in culture in a manner where their natural properties (in vivo) are maintained to some extent. Such in vitro biological systems have been used for many years in studies of mutagenic and genotoxic properties, and in studies of mechanisms. 

When the dehydration of 39 was carried out (H3PO4 or DMSO under reflux) instead of its dehydroxylation, a different class of stilbene derivatives, such as pinosilvine 44, resveratrol 45 or piceatannol 46, were easily obtained . From these compounds, resver-atrol has shown very potent anticancer properties in vivo, this activity being proven in rats . 

In Vitro Target In Vitro ADME Physical Properties In Vivo Safety... 

Studies have also demonstrated curcumin s therapeutic properties in vivo. In 6-week-old mice, the administration of a 2% curcumin diet via oral gavage resulted in a 53% reduction in lymphomas and leukemias. When topically applied prior to the administration of TPA in mice, curcumin down-regulated TPA-induced NF-kB and AP-1. It was also showed that oral administration of curcumin (50-200 mg/kg) inhibits the development of leukemia (HL 60) cell-induced xenografts in nude mice [Anand et al., 2008]. 

HSF3, identified in chicken, is induced by c-Myb in the absence of cellular stress (Nakai and Morimoto, 1993 Kanei-Ishii et al., 1997). Another isoform of HSF found in human cells, HSF4, possesses transcription represser properties in vivo (Frejtag et al., 2001). Comparisons of HSF protein structure in these organisms indicate the presence of conserved DNA binding domain and three hydrophobic heptad repeats that constitute the trimerization domain. These domains are located within the amino-terminal region of the protein. The stress-responsive transcriptional activation domain is located in the carboxyl-terminal region of the molecule. 

Effects of Induction. The effects of inducers are usually the opposite of those of inhibitors thus their effects can be demonstrated by much the same methods, that is, by their effects on pharmacological or toxicological properties in vivo or by the effects on enzymes in vitro following prior treatment of the animal with the inducer. In vivo effects are frequently reported the most common ones are the reduction of the hexobarbital sleeping time or zoxazolamine paralysis time. These effects have been reported for numerous inducers and can be quite dramatic. For example, in the rat, the paralysis time resulting from a high dose of zoxazolamine can be reduced from 11 hours to 17 minutes by treatment of the animal with benzo(a)pyrene 24 hours before the administration of zoxazolamine. 

Ginseng extracts exert antineoplastic effects and have cytotoxic properties and growth inhibitory properties in vivo. 

Farrell TJ, Patterson MS, Wilson B. A diffusion-theory model of spatially resolved, steady-state diffuse reflectance for the noninvasive determination of tissue optical properties in vivo. Medical Physics 1992, 19, 879-888. 

The approach taken here is to emphasize the types of reactions the pollutants can undergo, not only to afford understanding of observations made both in vivo and in vitro but also to indicate new possibilities for research. This method attempts to present the status of biochemical investigations of air pollutant toxicity and also suggests a framework for assessing future investigations. We shall, therefore, take four individual pollutants and discuss them from the points of view of chemical properties, in vivo effects and in vitro effects. 

Properties In Vivo of Chelate-Tagged Proteins and Polypeptides... 

In 1935, a red dye called Prontosil, 30, was discovered to have antibacterial properties in vivo (i.e., when given to laboratory animals). No antibacterial effect was observed in vitro (i.e., Prontosil could not kill bacteria grown in a test tube). This result remained a mystery until it was discovered that Prontosil was not in fact the antibacterial agent. Instead, it was found that the Prontosil was metabolized by bacteria present in the small intestine of the test animal, and broken down to sulfanilamide 31 [6]. 

The new second-generation antihistamines are more selective Hi histamine receptor antagonists, and many of them have additional anti-aUergic properties in vivo, for example they reduce the release of inflammatory mediators or inhibit the recruitment of inflammatory cells (3-7). They also enter the brain less well and are therefore less likely to cause central adverse effects. 

Tabet F, Remaley AT, Segaliny AI, Millet J, Yan L, Nakhla S, Barter PJ, Rye KA, Lambert G (2010) The 5A apolipoprotein AT mimetic peptide displays antiinflammatory and antioxidant properties in vivo and in vitro. Arterioscler Thromb Vase Biol 30 246-252... 

A series of carbazole analogs was prepared as neuropeptide Y (NPY) antagonists. Compound 47 was found to have a high affinity for NPY, but had poor permeability properties in vivo with a B/P ratio of 0.1. The pKr for 47 was calculated to be 11.0 and thought to be a major cause for the poor PK profile. Efforts to decrease the led to 48, which had a pK = 9.7 and a better B/P ratio of 0.8. Finally, by decreasing the pK even further to 7.9, compound 49 gave very good brain penetration and had a B/P ratio of 4.2. 

The first-generation pure antiestrogen ICI 164,384 (Figure 5.29) is a 7a-substituted derivative of E2 that has no detectable estrogen-like properties in vivo or in vitro [375, 380]. The compound was identified in a search for drugs that do not possess the estrogen-like effects of tamoxifen and that would, as a result, be more effective antitumor agents. 

Despite the evidence mentioned above that QUIN may indeed exert its main neurotoxic properties in vivo through the NMDA receptor, and despite synergistic properties with 3-HK, there is still a controversial discussion within the field if the concentration of these metabolites reached in vivo is indeed sufficient to substantially stimulate the NMDA receptor and thus lead to a toxic calcium overload, or whether alternative pathophysiological mechanisms are at work [26]. 

Alkyl phosphocholines of type 37 constitute a new class of antitumor agents with interesting properties in vivo [170]. They are substrates for the PLD catalyzed transesterification with serine to give the corresponding alkyl phosphoserine 38 [25,26]. Surprisingly, the phosphono-analogue 39 is also a substrate for the transesterification allowing the preparation of a number of alkylphosphonates... 

---