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Na Sun,Tong Yu,Jun-Xing Zhao,Yaogui Sun,Junbing Jiang,Zhi-Bian Duan,WenkuiWang,Yuan-Liang Hu,Hai-Min Lei,HongquanLi 한국생물공학회 2015 Biotechnology and Bioprocess Engineering Vol.20 No.1
Twenty natural compounds isolated fromtraditional Chinese medicines were examined for theirantiviral activities against PCV2 in vitro. Antiviral activitywas analyzed by the assays of blocking of virus entry,inhibition of virus replication and inactivation of virusparticles in the virus suspension. 50% cytotoxic concentration(CC50) and 50% effective concentration (EC50) for eachcompound were determined by using the MTT method andimmunofluorescence assay (IFA), respectively. The resultsobtained from the inhibition of virus replication andinactivation of virus particles showed that the maximuminhibition rates for matrine and scutellarin were 57 and72.69% and their SI were 29.87 and 18.66, respectively. However, the results from the assays of inhibition of virusentry and inhibition of virus replication demonstrated thatboth aesculetin and arecoline hydrochloride stimulatedPCV2 replication, with the maximum stimulation rate of387.3 and 219.4%. In summary, both matrine and scutellarinhad antiviral activity against PCV2, while aesculetin andarecoline hydrochloride promoted PCV2 infection replicationin vitro.
Preparation of Novel Pyrrolo[2,3-b]pyridine Derivatives via a New Concise Synthetic Approach
Na Guo,Haiyong Jia,Xing You,Du Jiang,Kui Lu,Peng Yu 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.4
The pyrrolo[2,3-b]pyridine core structure, a bioisostere of quinolones, is found in several molecules that possess important biological activity. We describe here a new, concise, three-step synthesis of pyrrolo[2,3-b]pyridines starting from L-alanine. A series of 4,7-dihydro-4-oxo-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid derivatives, which have not been previously reported, were synthesized using this approach.
Yumei Jiang,Na Zhang,Yawen Zhou,Zhongkai Zhou,Yu Bai,Padraig Strappe,Chris Blanchard 한국식품과학회 2021 Food Science and Biotechnology Vol.30 No.5
Our team previously demonstrated that Ganodermalucidum spores (GLS) and resistant starch (RS) hadhypoglycemic effects separately on type 2 diabetic mellitus(T2DM) rats. This work was to explore the effects ofadministering encapsulated GLS within RS (referred to asEGLS) in the T2DM rats, which were induced by streptozotocin(STZ). The EGLS was orally administered torats for 28 days. The parameters of glycometabolismand lipometabolism were evaluated, and fecal microbiotacomposition was investigated. The results showed thatEGLS significantly enhanced glycometabolism and lipometabolismparameters in T2DM rats, which might beassociate with the enhancement of the glucose and lipidmetabolism, insulin secretion, and glycogen synthesis andreduced lipogenesis. Furthermore, the intervention ofEGLS also reduced the Proteobacteria community andimproved dysfunctional gut microbiota. This study indicatedEGLS may be a potential candidate for dietaryintervention to modulate diabetes.
( Yan Fu Jiang ),( Hyun Gyu Choi ),( Ying Li ),( Yu Mi Park ),( Jong Hwa Lee ),( Do Hoon Kim ),( Je Hyun Lee ),( Jong Keun Son ),( Min Kyun Na ),( Seung Ho Lee ) 영남대학교 약품개발연구소 2012 영남대학교 약품개발연구소 연구업적집 Vol.22 No.0
Definitive identification of original plant species is important for standardizing herbal medicine. Although only the dried roots of Cynanchum wilfordii (Asclepiadaceae) are prescribed as Cynanchi WilfordiiRadix in Korean Pharmacopoeia, the roots of C. wilfordii and C. auriculatum are often misused in the Korean herbal market due to their morphological similarity and similar name. Therefore, it would be very useful to discover an effective chemical marker for the identification of the two species. To this end, we carried out a phytochemical study on the roots of C. wilfordii. As a result, twenty compounds were isolated from the roots of C. wilfordii and their chemical structures were identified as β-sitosterol (1), wilfoside C1N (2), wilfoside C3N (3), wilfoside K1N (4), methyleugenol (5), wilfoside C1G (6), cynauriculoside A (7), daucosterol (8), 2,4-dihydroxyacetophenone (9), cynandione A (10), 2,5-dihydroxyacetophenone (11), acetovanillone (12), p-hydroxyacetophenone (13), sucrose (14), conduritol F (15), geniposide (16), succinic acid (17), 3-(β-D-ribofuranosyl)-2,3-dihydro-6H-1,3-oxazine-2,6-dione (18), bungeiside A (19), cynanoneside B (20). Among them, compounds 15, 16, 18, 19, and 20 were isolated for the first time from this species. Furthermore, conduritol F (15) was demonstrated to be contained only in C. wilfordii. Therefore, it may be useful as a chemical marker to identify the two species C. wilfordii and C. auriculatum.
Chen Wenjia,Ma Zhaochen,Yu Lingxiang,MAO Xia,Ma Nan,Guo Xiaodong,Yin Xiaoli,Jiang Funeng,Wang Qian,Wang Jigang,Fang Mingliang,Lin Na,Zhang Yanqiong 생화학분자생물학회 2022 Experimental and molecular medicine Vol.54 No.-
Artesunate (ART) has been indicated as a candidate drug for hepatocellular carcinoma (HCC). Glucosylceramidase (GBA) is required for autophagic degradation. Whether ART regulates autophagic flux by targeting GBA in HCC remains to be defined. Herein, our data demonstrated that the dramatic overexpression of GBA was significantly associated with aggressive progression and short overall survival times in HCC. Subsequent experiments revealed an association between autophagic activity and GBA expression in clinical HCC samples, tumor tissues from a rat model of inflammation-induced HCC and an orthotopic mouse model, and human HCC cell lines. Interestingly, probe labeling identified GBA as an ART target, which was further verified by both a glutathione-S-transferase pulldown assay and surface plasmon resonance analysis. The elevated protein expression of LC3B, the increased numbers of GFP-LC3B puncta and double-membrane vacuoles, and the enhanced expression of SQSTM1/p62 indicated that the degradation of autophagosomes in HCC cells was inhibited by ART treatment. Both the in vitro and in vivo data revealed that autophagosome accumulation through targeting of GBA was responsible for the anti-HCC effects of ART. In summary, this preclinical study identified GBA as one of the direct targets of ART, which may have promising potential to inhibit lysosomal autophagy for HCC therapy.
Zhao, Yan-Jie,Jiang, Ni,Song, Qing-Kun,Wu, Jiang-Ping,Song, Yu-Guang,Zhang, Hong-Mei,Chen, Feng,Zhou, Lei,Wang, Xiao-Li,Zhou, Xin-Na,Yang, Hua-Bing,Ren, Jun,Lyerly, Herbert Kim Asian Pacific Journal of Cancer Prevention 2015 Asian Pacific journal of cancer prevention Vol.16 No.6
Background: There are few choices for treatment of advanced cancer patients who do not respond to or tolerate conventional anti-cancer treatments. Therefore this study aimed to deploy the benefits and clinical efficacy of continuous dendritic cell-cytokine induced killer cell infusions in such patients. Materials and Methods: A total of 381 infusions (from 67 advanced cases recruited) were included in this study. All patients underwent peripheral blood mononuclear cell apheresis for the following cellular therapy and dendritic cells-cytokine induced killer cells were expanded in vitro. Peripheral blood T lymphocyte subsets were quantified through flow cytometry to address the cellular immunity status. Clinical efficacy and physical activities were evaluated by RECIST criteria and Eastern Cooperative Oncology Group scores respectively. Logistic regression model was used to estimate the association between cellular infusions and clinical benefits. Results: An average of $5.7{\pm}2.94{\times}10^9$ induced cells were infused each time and patients were exposed to 6 infusions. Cellular immunity was improved in that cytotoxic $CD8^+CD28^+$ T lymphocytes were increased by 74% and suppressive $CD8^+CD28^-$ T lymphocytes were elevated by 16% (p<0.05). Continuous infusion of dendritic cells-cytokine induced killer cells was associated with improvement of both patient status and cellular immunity. A median of six infusions were capable of reducing risk of progression by 70% (95%CI 0.10-0.91). Every elevation of one ECOG score corresponded to a 3.90-fold higher progression risk (p<0.05) and 1% increase of $CD8^+CD28^-$ T cell proportion reflecting a 5% higher risk of progression (p<0.05). Conclusions: In advanced cancer patients, continuous dendritic cell-cytokine induced killer cell infusions are capable of recovering cellular immunity, improving patient status and quality of life in those who are unresponsive to conventional cancer treatment.
Da-Hua Shi,Jun-Hua Wu,Zhi-Qiang Yan,Li-Na Zhang,Yu-Rong Wang,Chun-Ping Jiang 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
To find the multi-target-directed compounds for the treatment of Alzheimer’s disease (AD), we synthesized 7-(4-(diethylamino)butoxy)-5-hydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, a novel 7-O-modified genistein derivative (GS-14), and investigated its acetylcholinesterase (AChE) inhibitory effect, estrogenic activity and neuroprotective effect. GS-14 acted as a selective AChE inhibitor in vitro, with an IC50 value of 0.17 μM and showed no inhibition activity against butyrylcholinesterase (BuChE). The Lineweaver–Burk plot revealed that GS-14 was a non-competitive AChE inhibitor with a Ki value of 0.23 μM and the molecular docking model indicated that GS-14 interacted with the peripheral anionic site (PAS) of AChE. The MCF-7 proliferation assay demonstrated that GS-14 possessed estrogenic activity and GS-14 exhibited a high specificity for estrogen receptor β (ERβ) with a dissociation constant (Ki) of 2.86 nM compared with that of 1.01 μM for estrogen receptor α (ERα) in the molecular docking study. GS-14 also possessed a neuroprotective effect and showed the best protective effect against the β-amyloid protein-induced injury on SH-SY5Y cells at a concentration of 1 nM. Considering its AChEinhibition activity, estrogenic activity and neuroprotective effect, GS-14 may be a potential multi-target agent for the treatment of AD.
Kim, Ji-Hye,Kim, You-Kyoung,Arash, Minai-Tehrani,Hong, Seong-Ho,Lee, Jae-Ho,Kang, Bit Na,Bang, Yong-Bin,Cho, Chong-Su,Yu, Dae-Yeul,Jiang, Hu-Lin,Cho, Myung-Haing American Scientific Publishers 2012 Journal of Nanoscience and Nanotechnology Vol.12 No.7
<P>Polyethyleneimine (PEI) has been described as a highly efficient gene carrier due to its efficient proton sponge effect within endosomes. However, many studies have demonstrated that PEI is toxic and associated with a lack of cell specificity despite high transfection efficiency. In order to minimize the toxicity of PEI, we prepared chitosan-graft-spermine (CHI-g-SPE) in a previous study. CHI-g-SPE showed low toxicity and high transfection efficiency. However, this compound also had limited target cell specificity. In the present study, we synthesized galactosylated CHI-g-SPE (GCS) because this modified GCS could be delivered specifically into the liver due to hepatocyte-specific galactose receptors. The DNA-binding properties of GCS at various copolymer/DNA weight ratios were evaluated by a gel retardation assay. The GCS copolymer exhibited significant DNA-binding ability and efficiently protected DNA from nuclease attack. Using energy-filtered transmission electron microscopy (EF-TEM), we observed dense spherical, nano-sized GCS/DNA complexes with a homogenous distribution. Most importantly, GCS was associated with remarkably low cytotoxicity compared to PEI in HepG2, HeLa, and A549 cells. Moreover, GCS carriers specifically delivered the gene-of-interest into hepatocytes in vitro as well as in vivo. Our results suggest that the novel GCS described here is a safe and highly efficient carrier for hepatocyte-targeted gene delivery.</P>