• Korean Journal of Veterinary Research
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• v.27 no.1
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• pp.35-40
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• 1987

Higenamine, a benzyltetrahydroisopuinoline analog isolated from aconite tuber, has potent isotropic action. Recent studies suggest it may have beta receptor agonistic property in that its inotropic action is blocked by propranolol in isolated rabbit heart. However, no study has been carried out on other organs than heart. Higenamine is expected to have pharmacological actions on smooth muscle on the ground that it has catecholamine moiety and tetrahydrosioquinoline nucleus in its chemical structure, both of which are well known to have smooth muscle relaxation effects. Therefore present study was aimed at determining whether higenamine has bronchodilating effect in isolated guinea pig trachea smooth muscle rich in adrenergic beta receptor and if any, it has agonistic effect on beta receptor. The results were summarized as follows : 1. Higenamine had remarkable bronchodilating effect in guinea pig tracheal smooth muscle in a dose-dependent manner. 2. Bronchodilator effect of higenamine in isolated guinea pig tracheal smooth muscle was blocked competitively by propranolol. The $pD_2$ value of higenamine in isolated guinea pig tracheal smooth muscle was 5.65 and the $pA_2$ value of propranolol against higenamine in the same preparation was 7.97.

• Animal cells and systems
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• v.8 no.2
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• pp.117-123
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• 2004

The purpose of this study was to analyze inhibitory effects of anti-4-1BB monoclonal antibody on melanoma metastasis The 4-1BB (CD137) T cell molecule is a member of the TNF receptor family and its activation by either 4-1BB ligand or antibody induces T cell activation and growth. In the present study, administration of anti-4-1BB mAb induced inhibition of melanoma metastasis. Agonistic anti-4-1BB mAb induced not only CD$8^+$4-1BBT cells but also CD$8^+$IFN-${\gamma}$$^{+}$ T cell population. In the presence of anti-CD3 antibody, lymphocytes produced high levels of IFN-${\gamma}$ and low levels of IL-4 in anti-4-1BB mAb treated group. Exposure of melanoma cells to IFN-${\gamma}$ induced expression of MHC-I molecules. Thus, the increase in number of CD$8^+$T cells and enhanced MHC-I expression on B16F10 cells by augmented IFN-${\gamma}$ production in response to anti-4-1BB mAb may result in suppression of tumor growth and metastasis.s.

• Animal cells and systems
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• v.1 no.4
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• pp.571-576
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• 1997

The playas of the Southern High Plains (SHP) of Texas, USA are an important habitat for over one million wintering waterfowl. However, the recent trend toward the modification of playas for agricultural use is threatening winter habitat of waterfowl in this region. Diurnal activity budgets of wintering mallards (Anas platyrhynchos) were conducted from 1 October to 31 March, 1983-1984, and 1984-1985) at three habitat types; steep-sided pits, terraced pits, and open lakes. All seven activity patterns (feeding, locomotion, resting, comfort, courtship, alert, and agonistic) were different (P<0.05) among the three habitat types for wintering mallards on the SHP of Texas. Terraced pits supported more feeding activity (27.8%) (P<0.001) than steep-sided pits (11.2%) or open lakes (2.6%) due to their abundance of natural seeds and aquatic invertebrates. Hens (17.5%) fed more than drakes (11.7%) (P<0.05). Locomotion (32.2%) and alert (2.8%) behavior across the three habitat types showed the highest level during the early morning (6:00-9:00 AM). Paired mallards rested more (37.9%) than unpaired mallards (25.8%) (P<0.05). Agonistic activity was highest (2.4%) in terraced pits throughout the season.

• IMMUNE NETWORK
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• v.11 no.6
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• pp.428-430
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• 2011

We previously demonstrated that in vivo engagement of CD137, a member of TNF receptor superfamily, can delete allorective $CD4^+$ T cells through the induction of activation-induced cell death (AICD) in chronic graft-versus-host disease (cGVHD) and subsequently reverse established cGVHD. In this study, we further showed that agonistic anti-CD137 mAb was highly effective in triggering AICD of donor $CD8^+$ T cells as well as donor $CD4^+$ T cells in the $C57BL/6{\rightarrow}unirradiated$ $(C57BL/6\;{\times}\;DBA/2)F1$ acute GVHD model. Our results suggest that strong allostimulation should facilitate AICD of both alloreactive $CD4^+$ and $CD8^+$ T cells induced by CD137 stimulation. Therefore, depletion of pathogenic T cells using agonistic anti-CD137 mAb combined with potent TCR stimulation may be used to block autoimmune or inflammatory diseases mediated by T cells.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.2
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• pp.111-118
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• 2021

27-Hydroxycholesterol (27OHChol) exhibits agonistic activity for liver X receptors (LXRs). To determine roles of the LXR agonistic activity in macrophage gene expression, we investigated the effects of LXR inhibition on the 27OHChol-induced genes. Treatment of human THP-1 cells with GSK 2033, a potent cell-active LXR antagonist, results in complete inhibition in the transcription of LXR target genes (such as LXRα and ABCA1) induced by 27OHChol or a synthetic LXR ligand TO 901317. Whereas expression of CCL2 and CCL4 remains unaffected by GSK 2033, TNF-α expression is further induced and 27OHChol-induced CCL3 and CXCL8 genes are suppressed at both the transcriptional and protein translation levels in the presence of GSK 2033. This LXR antagonist downregulates transcript levels and surface expression of CD163 and CD206 and suppresses the transcription of CD14, CD80, and CD86 genes without downregulating their surface levels. GSK 2033 alone had no effect on the basal expression levels of the aforementioned genes. Collectively, these results indicate that LXR inhibition leads to differential regulation of 27-hydroxycholesterol-induced genes in macrophages. We propose that 27OHChol induces gene expression and modulates macrophage functions via LXR-dependent and -independent mechanisms.

• Journal of Life Science
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• v.23 no.10
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• pp.1199-1208
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• 2013

Fibroblastic reticular cells (FRCs) form the structural backbone of the T zone provide a guidance path for immigrating T cells in the lymph node (LN). FRCs may contribute directly to developing T-cell biology in the LN and allow analyses of fundamental aspects of FRC biology related to T cells. FRCs inhibited T-cell apoptosis, and FRC culture supernatants strongly induced the expression of Bcl-xL in T cells against doxorubicin. Coculture of FRC and T cells resulted in rearrangements of the actin cytoskeleton, as well as global changes in the morphology of the FRCs. In addition, when cocultured, the T cells adhered to the FRC monolayer, and the membrane intercellular adhesion molecule (ICAM)-1 was slightly increased by day-dependent manner. In contrast, the expression of soluble ICAM-1 was dramatically increased in a day-dependent manner. Several chemokines, such as CCL5, CXCL1, CXCL5, CXCL16, CCL8, CXCL13, and ICAM-1, and MMPs were expressed in FRCs sensed by tumor necrosis factor (TNF) families. Nuclear factor kappa B ($NF{\kappa}B$)-RelA of the $NF{\kappa}B$ canonical pathway was translocated into FRC nuclear by $TNF{\alpha}$. In contrast, p52 proteolyzed from p100, a counterpart of RelB of the noncanonical $NF{\kappa}B$ pathway, accumulated in the peripheral FRC nucleus by agonistic anti-$LT{\beta}R$ antibody. In summary, we propose a model in which FRCs engage in bidirectional crosstalk to increase the efficiency of T-cell biology. This cooperative feedback loop may help to maintain tissue integrity and function during immune responses.

• Bulletin of the Korean Chemical Society
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• v.25 no.12
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• pp.1784-1790
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• 2004

A series of 2-(3-chlorophenyl)-2-hydroxyethylamine derivatives containing a tetrahydrocarbazole linker were prepared and evaluated for their ${\beta}_3$-adrenoceptor agonistic activity. Several compounds showed potency comparable to CL-316243.

• Proceedings of the PSK Conference
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• 2002.04a
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• pp.152.2-152.2
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• 2002

• IMMUNE NETWORK
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• v.10 no.3
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• pp.104-108
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• 2010

CD137 (4-1BB/tnfrsf9) has been shown to co-stimulate T cells. However, agonistic anti-CD137 monoclonal antibody (mAb) treatment can suppress $CD4^+$ T cells, ameliorating autoimmune diseases, whereas it induces activation of $CD8^+$ T cells, resulting in diverse therapeutic activity in cancer, viral infection. To investigate the CD137-mediated T cell suppression mechanism, we examined whether anti-CD137 mAb treatment could affect $CD11b^+Gr-1^+$ myeloid-derived suppressor cells (MDSCs). Intriguingly, anti-CD137 mAb injection significantly increased $CD11b^+Gr-1^+$ cells, peaking at days 5 to 10 and continuing for at least 25 days. Furthermore, this cell population could suppress both $CD8^+$ T cells and $CD4^+$ T cells. Thus, this study demonstrated that, for the first time, anti-CD137 mAb treatment could induce $CD11b^+Gr-1^+$ MDSCs under normal conditions, suggesting a possible relationship between myeloid cell induction and CD137-mediated immune suppression.

• Asian-Australasian Journal of Animal Sciences
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• v.18 no.4
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• pp.463-469
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• 2005

An attempt was made to analyze the factors affecting mating performance of rams in pen mating systems. Due to many types of social interactions, mating performance of rams may decrease or increase. Six intact Muzaffarnagari rams were used and divided into three dominant subordinate pairs by food and ewe competition test. For dominant rams subordinate ram became competitor and vice versa. In the first experiment, ram was exposed to ewe but the competitor ram was kept outside the pen with the facility of visibility only. In the second experiment each ram was exposed to ewe along with the competitor ram and in third experiment ram was exposed to ewes (two) along with competitor ram in observation pen. Recordings of different mating and agonistic behaviour were done in all the experiments. It was found that subordinate ram's mating behaviour was inhibited by mere presence of a dominant ram out side without physical contact. However, when ram exposed to oestrus ewe(s) along with competitor ram, both dominant and subordinate rams spent much of their time in guarding activities instead of mating. In addition dominant ram tried to curtail the subordinate ram mating by agonistic interaction like fight and butting. Different guarding activities were observed either as active or passive type depending on level of dominanace. It was concluded that in a limited space the interaction of two or more rams might affect the number of services adversely.