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Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana

  • Kim, Mi Seon;Lee, Yunmi;Sung, Gi-Ho;Kim, Ji Hye;Park, Jae Gwang;Kim, Han Gyung;Baek, Kwang Soo;Cho, Jae Han;Han, Jaegu;Lee, Kang-Hyo;Hong, Sungyoul;Kim, Jong-Hoon;Cho, Jae Youl
    • Biomolecules & Therapeutics
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    • v.23 no.4
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    • pp.367-373
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    • 2015
  • Cordyceps species including Cordyceps bassiana are a notable anti-cancer dietary supplement. Previously, we identified several compounds with anti-cancer activity from the butanol fraction (Cb-BF) of Cordyceps bassiana. To expand the structural value of Cb-BF-derived anti-cancer drugs, we employed various chemical moieties to produce a novel Cb-BF-derived chemical derivative, KTH-13-amine-monophenyl [4-isopropyl-2-(1-phenylethyl) aniline (KTH-13-AMP)], which we tested for anti-cancer activity. KTH-13-AMP suppressed the proliferation of MDA-MB-231, HeLa, and C6 glioma cells. KTH-13-AMP also dose-dependently induced morphological changes in C6 glioma cells and time-dependently increased the level of early apoptotic cells stained with annexin V-FITC. Furthermore, the levels of the active full-length forms of caspase-3 and caspase-9 were increased. In contrast, the levels of total forms of caspases-3, caspase-8, caspase-9, and Bcl-2 were decreased in KTH-13-AMP treated-cells. We also confirmed that the phosphorylation of STAT3, Src, and PI3K/p85, which is linked to cell survival, was diminished by treatment with KTH-13-AMP. Therefore, these results strongly suggest that this compound can be used to guide the development of an anti-cancer drug or serve as a lead compound in forming another strong anti-proliferative agent.

Inhibitory Effect of Biotransformed-Fucoidan on the Differentiation of Osteoclasts Induced by Receptor for Activation of Nuclear Factor-κB Ligand

  • Park, Bobae;Yu, Sun Nyoung;Kim, Sang-Hun;Lee, Junwon;Choi, Sung Jong;Chang, Jeong Hyun;Yang, Eun Ju;Kim, Kwang-Youn;Ahn, Soon-Cheol
    • Journal of Microbiology and Biotechnology
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    • v.32 no.8
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    • pp.1017-1025
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    • 2022
  • Bone homeostasis is regulated by constant remodeling through osteogenesis by osteoblasts and osteolysis by osteoclasts and osteoporosis can be provoked when this balance is broken. Present pharmaceutical treatments for osteoporosis have harmful side effects and thus, our goal was to develop therapeutics from intrisincally safe natural products. Fucoidan is a polysaccharide extracted from many species of brown seaweed, with valuable pharmaceutical activities. To intensify the effect of fucoidan on bone homeostasis, we hydrolyzed fucoidan using AMG, Pectinex and Viscozyme. Of these, fucoidan biotransformed by Pectinex (Fu/Pec) powerfully inhibited the induction of tartrate-resistant acid phosphatase (TRAP) activity in osteoclasts differentiated from bone marrow macrophages (BMMs) by the receptor for activation of nuclear factor-κB ligand (RANKL). To investigate potential of lower molecular weight fucoidan it was separated into >300 kDa, 50-300 kDa, and <50 kDa Fu/Pec fractions by ultrafiltration system. The effects of these fractions on TRAP and alkaline phosphatase (ALP) activities were then examined in differentiated osteoclasts and MC3T3-E1 osteoblasts, respectively. Interestingly, 50-300 kDa Fu/Pec suppressed RANKL-induced osteoclasts differentiation from BMMs but did not synergistically enhance osteoblasts differentiation induced by osteogenic agents. In addition, this fraction inhibited the expressions of NFATc1, TRAP, OSCAR, and RANK, which are all key transcriptional factors involved in osteoclast differentiation, and those of Src, c-Fos and Mitf, as determined by RT-PCR. In conclusion, enzymatically low-molecularized 50-300 kDa Fu/Pec suppressed TRAP by downregulating RANKL-related signaling, contributing to the inhibition of osteoclasts differentiation, and represented a potential means of inducing bone remodeling in the background of osteoporosis.

Development of a Multi-step Stamping Process for the Effective Fabrication of a Thin Sheet for High Aspect Ratio Corrugated Structures (고세장비 연속주름을 갖는 박판구조물 제작을 위한 다단성형공정 개발)

  • Choi, Sung-Woo;Park, Sang-Hu;Jeong, Ho-Seung;Min, June-Kee;Jeong, Jae-Hun;Cho, Jong-Rae;Kim, Hyun-June;Willians, Paul
    • Transactions of the Korean Society of Mechanical Engineers A
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    • v.34 no.2
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    • pp.219-226
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    • 2010
  • The stamping process is widely used in fabricating various sheet-parts for vehicle, airplane, and electronic devices due to its low processing cost and high productivity. Recently the use of thin sheets with corrugated structures has rapidly increased for the production of energy devices, e.g., heat exchangers and fuel cells. However, it is very difficult to make corrugated structures directly in the stamping process due to their geometrical complexity. To solve this problem, this paper proposes a multi-step stamping process with a combined heat treatment process: a sequence of the first stamping, heat treatment, and second stamping. By multi-stamping, we obtained successful results in fabricating very thin corrugated structures with thicknesses of $100{\mu}m$; these are applicable as part of a plate-type heat exchanger.

Quality characteristics of domestic and imported commercial plain wheat flour (시판 우리밀과 수입밀 중력 밀가루의 품질 특성 비교)

  • Kwak, Han Sub;Kim, Mi Jeong;Kim, Hoon;Kim, Sang Sook
    • Korean Journal of Food Science and Technology
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    • v.49 no.3
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    • pp.304-310
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    • 2017
  • The aim of this study was to compare the physicochemical properties of domestic and imported commercial plain wheat flour and dough. Four types of domestic wheat flour (DW; DW1-4) were compared to four types of imported wheat flour (IW; IW1-4). DWs exhibited lower moisture content, lightness (L), and whiteness, and higher protein content, redness (a), and yellowness (b), than those exhibited by IWs. Solvent retention capacity of DWs and IWs was similar; however, DWs showed higher gluten performance index. Pasting properties, analyzed by rapid visco analyzer (RVA), were similar for DW1, DW2, and IWs; however, DW3 and DW4 showed different RVA patterns. Considering that DW3 and DW4 were organic wheat flour, possible incorporation of damaged kernel might increase amylase activities resulting in decreased peak viscosity. Dough resistance (108.4-159.9 g) and extensibility (11.8-16.7 mm) of IWs were higher than those of DWs (78.0-118.7 g, 8.7-12.5 mm, respectively).

Extract of Fructus Corni Ameliorates Testosterone-induced Benign Prostatic Hypertrophy in Sprague Dawley Rats (산수유 추출물에 의한 testosterone으로 유발된 양성 전립선 비대증의 개선)

  • Ji, Seon Yeong;Kim, Min Yeong;Hwangbo, Hyun;Lee, Hyesook;Hong, Su Hyun;Kim, Tae Hee;Yoon, Seonhye;Kim, Hyun Jin;Jung, Ha Eun;Kim, Sung Yeon;Kim, Tae Jung;Kim, Min Ji;Kim, Sung Ok;Choi, Yung Hyun
    • Journal of Life Science
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    • v.31 no.6
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    • pp.550-558
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    • 2021
  • Fructus Corni, the fruit of Cornus officinalis, has long been used for the prevention and treatment of various diseases. We recently suggested that it was effective against benign prostatic hyperplasia (BPH). In this study, we investigated the inhibitory effect of Corni Fructus (CF) water extract on BPH induced by testosterone propionate (TP) in noncastrated and castrated animal models. BPH was induced in Sprague Dawley rats by an intramuscular injection of TP in castrated or noncastrated rats. Finasteride (FINA) treatment was used as a positive control for inhibition of BPH. According to our results, CF administration inhibited excessive enlargement of development of the prostate in both the noncastrated and castrated groups compared to the control and FINA-treated groups. The inhibitory effect of CF on BPH was associated with inhibition of expression of hypoxia-inducible factor-1α, 5α-reductase type 2, steroid receptor coactivator-1, androgen receptor (AR), and prostate-specific antigen. Serum levels of the stress hormone cortisol increased during BPH induction by TP in both the noncastrated and castrated groups, but they were attenuated significantly by CF administration. However, insulin and IGF-1 levels were not increased in the BPH-induced groups and CF, and no effective results were found by CF administration. These results point to a beneficial effect of CF on BPH through inhibition of AR signaling pathway activity and imply that CF shows excellent potential as a therapeutic agent for the prevention and treatment of BPH.

Inhibitory Effects of Tenebrio molitor Larvae Ethanol Extract on RANKL-Induced Osteoclast Differentiation (갈색거저리 유충 에탄올 추출물이 RANKL에 의해 유도되는 파골세포 분화에 미치는 영향)

  • Seo, Minchul;Baek, Minhee;Lee, Hwa Jeong;Shin, Yong Pyo;Lee, Joon Ha;Kim, In-Woo;Kim, Mi-Ae;Hwang, Jae-Sam
    • Journal of Life Science
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    • v.30 no.11
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    • pp.983-989
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    • 2020
  • The balance between bone-resorbing osteoclasts and bone-forming osteoblasts is key to bone health. An imbalance between osteoclasts and osteoblasts leads to various bone-related disorders, such as osteoporosis, osteomalacia, and osteopetrosis. However, the bone-resorption inhibitor drugs that are currently used may cause side effects. Natural substances have recently received much attention as therapeutic drugs for the treatment of bone health. This study was designed to determine the effect of Tenebrio molitor larvae ethanol extract (TME) on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast differentiation. To measure the effect of TME on osteoclast differentiation, RAW264.7 cells were treated with RANKL with or without TME for 5 days. The tartrate-resistant acid phosphatase (TRAP) activity was significantly inhibited by treatment of TME without cytotoxicity up to 2 mg/ml. In addition, TME effectively suppressed expression of osteoclast differentiation-related marker genes and proteins such as TRAP, NFATc1, and c-Src. TME also significantly inhibited the p38 mitogen-activated protein kinase (MAPK) signaling pathway without affecting ERK and JNK signaling in RANKL-induced RAW264.7 cells. Consequently, we conclude that TME suppresses osteoclast differentiation by inhibiting RANKL-induced osteoclastogenic genes expression through the p38 MAPK signaling pathways. These results suggest that TME and its bioactive components are potential therapeutics for bone-related diseases such as osteoporosis.