• Asian-Australasian Journal of Animal Sciences
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• v.26 no.11
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• pp.1577-1582
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• 2013

The effects of dietary supplementation of selenium (Se), iodine (I), and a combination of both on the blood haematology, serum free thyroxine (FT4) and free triiodothyronine (FT3) hormones and glutathione peroxidase enzyme (GSH-Px) activity were examined on twenty four (7 to 8 months old, $22{\pm}1.17$ kg live weight) Kacang crossbred male goats. Animals were randomly assigned to four dietary treatments (6 animals in each group). Throughout 100 d of feeding trial, the animals of control group (CON) received a basal diet, while the other three groups were offered basal diet supplemented with 0.6 mg/kg diet DM Se (SS), or 0.6 mg/kg diet DM I (PI), or a combination of both Se and I, each at 0.6 mg/kg diet DM (SSPI). The haematological attributes which are haemoglobin (Hb), red blood cell (RBC), packed cell volume (PCV), mean cell volume (MCV), white blood cells (WBC), band neutrophils (B Neut), segmented neutrophils (S Neut), lymphocytes (Lymph), monocytes (Mono), eosinophils (Eosin) and basophils (Baso) were similar among the four treatment groups, while serum levels of Se and I increased significantly (p<0.05) in the supplemented groups. The combined dietary supplementation of Se and I (SSPI) significantly increased serum FT3 in the supplemented animals. Serum GSH-Px activity increased significantly in the animals of SS and SSPI groups. It is concluded that the dietary supplementation of inorganic Se and I at a level of 0.6 mg/kg DM increased serum Se and I concentration, FT3 hormone and GSH-Px activity of Kacang crossbred male goats.

• Biomolecules & Therapeutics
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• v.20 no.3
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• pp.313-319
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• 2012

In recent years, inhibition of HDACs has emerged as a potential strategy to reverse aberrant epigenetic changes associated with cancer, and several classes of HDAC inhibitors have been found to have potent and specific anticancer activities in preclinical studies. But their precise mechanism of action has not been elucidated. In this study, a novel synthetic inhibitor of HDAC, 3-(4-dimethylamino phenyl)-N-hydroxy-2-propenamide [IN-2001] was examined for its antitumor activity and the underlying molecular mechanisms of any such activity on human breast cancer cell lines. IN-2001 effectively inhibited cellular HDAC activity ($IC_{50}$ = 0.585 nM) inMDA-MB-231 human breast cancer cells. IN-2001 caused a significant dose-dependent inhibition of cell proliferation in estrogen receptor (ER) negative MDA-MB-231human breast cancer cells. Cell cycle analysis revealed that the growth inhibitory effects of IN-2001 might be attributed to cell cycle arrest at $G_0/G_1$ and/or $G_2$/Mphase and subsequent apoptosis in human breast cancer cells. These events are accompanied by modulating several cell cycle and apoptosis regulatory genes such as CDK inhibitors $p21^{WAF1}$ and $p27^{KIP1}$ cyclin D1, and other tumor suppressor genes such as cyclin D2. Collectively, IN-2001 inhibited cell proliferation and induced apoptosis in human breast cancer cells and these findings may provide new therapeutic approaches, combination of antiestrogen together with a HDAC inhibitor, in the hormonal therapy-resistant ER-negative breast cancers. In summary, our data suggest that this histone deacetylase inhibitor, IN-2001, is a novel promising therapeutic agent with potent antitumor effects against human breast cancers.

• The Korea Journal of Herbology
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• v.32 no.5
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• pp.19-25
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• 2017

Objective : The Sinseon-yukza-hwan (SSY), a Korean medicinal formula which includes Radix Rehmanniae Preparata and other medicinal herbs, has long been used for treatment of alopecia and gray hair through oral administration. This study is designed to enhance the utilization of natural materials in hair and scalp-related cosmetics. Possibility of SSY as an antioxidant was examined from its 50% ethanol extract. Methods : The antioxidative capacities were evaluated by determining total phenolic and flavonoid contents, 1,1-diphenyl-2-picryl hydrazyl (DPPH), 2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), reducing power and hydroxyl radical scavenging activity. Results : Total polyphenol and flavonoid contents of SSY were 25.53 mg TE, tannic acid equivalent/g and 18.90 mg RE, rutin equivalent/g, respectively, which correlated strongly its antioxidative activity. The DPPH and ABTS free radical scavenging activities of SSY at $0.1mg/m{\ell}{\sim}5mg/ml$ were ranged from 20% to 85% and 10% to 58%, respectively. Also the hydroxyl radical scavenger activity and reducing power increased in SSY-treated group, which were significantly lower in SSY-compared to BHA-treated group. But the highest reducing power was shown as 79% from SSY-treated group, which was higher value than 65% from BHA-treatment. These results showed that SSY extract effectively inhibited the generation of free radicals in the all assay system with dose-dependent manners. Conclusions : Thus, the present study provide preclinical data to support the expanded application of SSY, which could be potential candidates for natural antioxidants.

• Parasites, Hosts and Diseases
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• v.62 no.3
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• pp.330-341
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• 2024

The Trichinella spiralis novel cystatin (TsCstN) inhibits cathepsin L (CatL) activity and inflammation of macrophages during lipopolysaccharide (LPS) induction. To identify the protease inhibitory region, this study applied an in silico modeling approach to simulate truncation sites of TsCstN (Ts01), which created four truncated forms, including TsCstN^∆1-39 (Ts02), TsCstN^∆1-71 (Ts03), TsCstN^{∆1-20, ∆73-117} (Ts04), and TsCstN^{∆1-20, ∆42-117} (Ts05). The superimposition of these truncates modeled with AlphaFold Colab indicated that their structures were more akin to Ts01 than those modeled with I-TASSER. Moreover, Ts04 exhibited the closest resemblance to the structure of Ts01. The recombinant Ts01 (rTs01) and truncated proteins (rTs02, rTs03, and rTs04) were successfully expressed in a prokaryotic expression system while Ts05 was synthesized, with sizes of approximately 14, 12, 8, 10, and 2.5 kDa, respectively. When determining the inhibition of CatL activity, both rTs01 and rTs04 effectively reduced CatL activity in vitro. Thus, the combination of the α1 and L1 regions may be sufficient to inhibit CatL. This study provides comprehensive insights into TsCstN, particularly regarding its protein function and inhibitory domains against CatL.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.19
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• pp.8047-8050
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• 2014

Cancer is a multifaceted and genomically complex disease and research over decades has gradually and sequentially shown that essential biological mechanisms including cell cycle arrest and apoptosis are deregulated. The benefits of essential oils from different plants have started to gain appreciation as evidenced by data obtained from cancer cell lines and xenografted mice. Encouraging results obtained from preclinical studies have attracted considerable attention and various phytochemicals have entered into clinical trials.

• Asian-Australasian Journal of Animal Sciences
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• v.26 no.6
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• pp.874-878
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• 2013

Unlike Europe (particularly, Italy and Spain), where a number of studies have been conducted on the stressful effects of transport on rabbit welfare, few studies have been conducted on transportation of rabbits under hot, humid tropical conditions experienced in countries like Malaysia. We studied the effects of transportation in hot humid tropical conditions of Malaysia on physiometabolic changes in New Zealand white rabbits. Eighty experimental animals were divided into two groups of 40 bucks each and transported for either 3 or 1 h. Transportation caused a significant upsurge of aspartate aminotransferase, alanine aminotransferase and creatine kinase activities (p<0.001) though did not significantly affect lactate dehydrogenase (LDH) activity (p = 0.0706). Both transportation periods caused elevation in plasma glucose levels, lactic acidosis and dehydration as evidenced through elevated packed cell volume and plasma protein concentration. It was concluded that regardless of the duration, transport of rabbits under hot humid tropical conditions, resulted in heat distress since the rabbits showed hyperglycemia, hypercalcemia, lactacidemia, lymphocytopenia, dehydration and increase in blood enzyme activities.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.15
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• pp.6321-6326
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• 2014

${\alpha}$-Methyl-n-butylshikonin (MBS), one of the active components in the root extracts of Lithospermum erythrorhizon, posses antitumor activity. In this study, we assess the molecular mechanisms of MBS in causing apoptosis of SW620 cells. MBS reduced the cell viability of SW620 cells in a dose-and time-dependent manner and induced cell apoptosis. Treatment of SW620 cells with MBS down-regulated the expression of Bcl-2 and up-regulated the expression of Bak and caused the loss of mitochondrial membrane potential. Additionally, MBS treatment led to activation of caspase-9, caspase-8 and caspase-3, and cleavage of PARP, which was abolished by pretreatment with the pan-caspase inhibitor Z-VAD-FMK. MBS also induced significant elevation in the phosphorylation of JNK and p38. Pretreatment of SW620 cells with specific inhibitors of JNK (SP600125) and p38 (SB203580) abrogated MBS-induced apoptosis. Our results demonstrated that MBS inhibited growth of colorectal cancer SW620 cells by inducing JNK and p38 signaling pathway, and provided a clue for preclinical and clinical evaluation of MBS for colorectal cancer therapy.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.8
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• pp.4485-4494
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• 2013

Epidermal growth factor receptor (EGFR) is considered to be one of the key driver genes in non-small cell lung cancer (NSCLC). Several clinical trials have shown great promise of EGFR tyrosine kinase inhibitors (TKIs) in the first-line treatment of NSCLC. Many advances have been made in the understanding of EGFR signal transduction network and the interaction between EGFR and tumor microenvironment in mediating cancer survival and development. The concomitant targeted therapy and radiation is a new strategy in the treatment of NSCLC. A number of preclinical studies have demonstrated synergistic anti-tumor activity in the combination of EGFR inhibitors and radiotherapy in vitro and in vivo. In the present review, we discuss the rationale of the combination of EGFR inhibitors and radiotherapy in the treatment of NSCLC.

• International Journal of Industrial Entomology and Biomaterials
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• v.7 no.2
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• pp.139-144
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• 2003

Over 350 million people worldwide are chronic carriers of hepatitis B virus (HBV). Chronic viral infections of the liver can progress to cirrhosis, which may ultimately lead to hepatic failure or the development of hepatocellular carcinoma. There are two antiviral drugs on the market approved for clinical management of chronic HBV infections; interferon-alpha and the nucleoside analog lamivudine. However, they showed adverse side-effects. In the rational drug design for such therapies we would like to utilize antiviral drugs that inhibit the HBV replication in the liver. Investigation of natural extracts of silkworm exhibiting antiviral potential was held in the functional HBV polymerase activity and the release of virion particle in the HepG2.2.15 cell lines. HBV-producing transgenic mouse fed with silkworm DNJ molecule was shown as an inhibitor of serum HBV particles. We could represent this DNJ molecule as an antiviral potential complementing conventional therapies after preclinical tests against WHBV-infected animal model, woodchuck.

• Biomolecules & Therapeutics
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• v.7 no.3
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• pp.292-299
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• 1999

SKI 2053 R, cis-Malonato [(4R, 5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane] platinum(II), is a newly developed antitumor platinum complex derived from cisplatin. Preclinical studies suggest that it may have greater antitumor activity and lower toxicity than cisplatin. Effects of test agent on general toxicity of does and embryonic development of Fl fetuses were investigated in rabbits. Sixty eight New Zealand white rabbits were distributed among three treated groups and a control group. SKI 2053R was administered intravenously to pregnant rabbits from days 6 to 18 of gestation at dose levels of 0, 0.67, 2.0, or 6.0 mg/kg/day. The pregnant does were subjected to the caesarean section on day 28 of gestation. No treatment-related changes in clinical signs, body weight, food consumption, and necropsy findings were observed in all groups. Fl fetuses showed no changes related to the treatment of SKI 2053R, except that an increase in the incidence of skeletal variations were observed at 6.0 mg/kg. There were no signs of material toxicity or embryotoxicity at 0.67 and 2.0 mg/kg. The results show that the administration of 6.0 mg/kg SKI 2053R induces skeletal variations in fetuses and that the no observed adverse effect levels(NOAELS) of SKI 2053R are considered to be over 6.0 mg/kg for does and 2.0 mg/kg for Fl fetuses in rabbits.