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Huan, Le Cong,Tran, Phuong-Thao,Phuong, Cao Viet,Duc, Phan Huy,Anh, Duong Tien,Hai, Pham The,Huong, Le Thi Thu,Thuan, Nguyen Thi,Lee, Hye Jin,Park, Eun Jae,Kang, Jong Soon,Linh, Nguyen Phuong,Hieu, Tr Elsevier 2019 Bioorganic chemistry Vol.92 No.-
<P><B>Abstract</B></P> <P>In search for novel small molecules with antitumor cytotoxicity via activating procaspase-3, we have designed and synthesized three series of novel (E)-<I>N</I>′-benzylidene-4-oxoquinazolin-3(4<I>H</I>)-yl)acetohydrazides (<B>5a-j, 6a-h,</B> and <B>7a-h)</B>. On the phenyl ring ò the benzylidene part, three different substituents, including 2-OH-4-OCH<SUB>3</SUB>, 4-OCH<SUB>3</SUB>, and 4-N(CH<SUB>3</SUB>)<SUB>2</SUB>, were introduced, respectively. Biological evaluation showed that the acetohydrazides in series <B>5a-j</B>, in which the phenyl ring of the benzylidene part was substituted by 2-OH-4-OCH<SUB>3</SUB> substituent, exhibited potent cytotoxicity against three human cancer cell lines (SW620, colon; PC-3, prostate; NCI-H23, lung). Most of the compounds, in this series, especially compounds <B>5c, 5b</B> and <B>5h,</B> also significantly activated caspase-3 activity. Among these, compound <B>5c</B> displayed 1.61-fold more potent than PAC-1 as caspase-3 activator. Cell cycle analysis showed that compounds <B>5b</B>, <B>5c</B>, and <B>5h</B> significantly arrested the cell cycle in G1 phase. Further apoptotic studies also demonstrated compounds <B>5b</B>, <B>5c</B>, and <B>5h</B> as strong apoptotic cell death inducers. The docking simulation studies showed that these compounds could activate procaspase <I>via</I> chelating Zn<SUP>2+</SUP> ion bound to the allosteric site of the zymogen.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Novel (<I>E</I>)-<I>N</I>′-benzylidene-2-(4-oxoquinazolin-<I>3(4H)-yl</I>)acetohydrazides were synthesized. </LI> <LI> The acetohydrazides <B>5a-i</B> exhibited potent cytotoxicity against three human cancer cell lines. </LI> <LI> A number of cytotoxic compounds exhibited good caspase activation activity. </LI> <LI> The cytotoxic compounds were shown to arrest cells at G1 phase. </LI> <LI> The cytotoxic compounds were shown as strong apoptotic inducers. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Huan Lan,Zhewen Dong,Yaqi Wu,Chaojie Chong,Zhiqiang Liu,Wanying Li,Zixian Wang,Junyang Liu,Qi Qi Pang,Jia-Le Song,Yanyuan Zhou 한국식품영양과학회 2021 한국식품영양과학회 학술대회발표집 Vol.2021 No.10
This study investigated the antifibrotic effects of SA on ovarian fibrosis in letrozole-induced PCOS in rats. SA treatment restored letrozole-induced alterations in the body weight (BW), relative weights of the ovaries, and visceral adipose tissues. Histological observation showed that SA reduced the number of atretic follicles, cystic follicles, and fibrosis of the ovaries in PCOS rats. SA treatment also modulated the serum levels of sex hormones, which decreased the luteinizing hormone (LH), and testosterone (T) and increased the follicle-stimulating hormone (FSH) in PCOS rats. Administration of SA reduced letrozole-induced metabolic dysfunction by decreasing the serum levels of triglyceride (TG) and total cholesterol (TC) and increasing the levels of high-density lipoprotein cholesterol (HDL-C) in PCOS rats. Finally, SA treatment appeared to increase the activity of PPAR-γ, reduce the activation of the TGF-β1/Smad pathway, and reduce the collagen I, α-SMA and CTGF levels in the ovaries of the PCOS rats. Our results demonstrated that SA significantly ameliorated ovarian fibrosis and abolic disturbances in the letrozole-induced PCOS rats.
Huan Lan,Zhewen Dong,Yaqi Wu,Chaojie Chong,Zhiqiang Liu,Wanying Li,Zixian Wang,Junyang Liu,Qi Qi Pang,Jia-Le Song,Yanyuan Zhou 한국식품영양과학회 2021 한국식품영양과학회 학술대회발표집 Vol.2021 No.10
In this study, we investigated the antifibrotic effects of Rha on letrozole-induced PCOS in rats. Rha treatment restored letrozole-induced alterations in the body weight (BW), relative weights of the ovaries, and relative weights of uterine and visceral adipose tissues. Histological observation showed that Rha reduced the number of atretic follicles, cystic follicles, and fibrosis of the ovaries in the PCOS rats. Administration of Rha reduced letrozole-induced metabolic dysfunction by decreasing the serum levels of TG and TC and increasing the levels of HDL-C in the PCOS rats. Rha treatment also modulated the serum levels of sex hormones, which decreased the LH, E2 and T and increased the FSH in PCOS rats. Finally, Rha treatment appeared to increase the activity of PPAR-γ, reduce the activation of the TGF-β1/Smad pathway, and reduce the collagen I, α-SMA and CTGF levels in the ovaries of the PCOS rats. Our results demonstrated that Rha significantly ameliorated metabolic disturbances and ovarian fibrosis in the letrozole-induced PCOS rats. Rha may be an effective compound in preventing ovarian fibrosis in the future.
Effects of naringin on fibrosis in a rats model with polycystic ovary syndrome (PCOS)
Zhewen Dong,Huan Lan,Wanying Li,Qi Qi Pang,Jia- Le Song,Yanyuan Zhou 한국식품영양과학회 2021 한국식품영양과학회 학술대회발표집 Vol.2021 No.10
To observe the effect of naringin intervention and its ameliorating effect on ovarian fibrosis in letrozole induced POCS rats. SD rats were divided into normal, PCOS and naringin group. The body weight(BW) was recorded every 3 days. ELISA kits were used to measure serum levels of FSH, LH, E2, and T in PCOS rats. The levels of CollagenI, CTGF, α-SMA were detected by Western Blotting assay. The BW of PCOS rats were significantly increased than that in control group (P<0.05). Naringin treatment reduced the BW in PCOS rats. Compared with normal group, the serum level of E2 in PCOS group was decreased, and the serum T, LH, FSH, LH/FSH ratio levels were increased. However, administrated with naringin increased the serum E2 levels, and also decreased the serum levels of T, LH, FSH, LH/ FSH levels in PCOS rats. The protein levels of CollagenI, CTGF and α-SMA were increased in varian of PCOS rats than that in normal group. Naringin treatment was able to decrease the protein levels of CollagenI, CTGF and α-SMA in varian of PCOS rats.The results showed that naringin intervention could improve the metabolic imbalance and the occurrence of fibrosis in PCOS rats.
Jing-Qing Le,Fang Yang,Xun-Huan Song,Ke-Ke Feng,Ling-Wu Tong,Meng-Die Yin,Wen-Zhong Zhang,Ying-Qi Lin,Hui Wu,Jing-Wei Shao 한국공업화학회 2023 Journal of Industrial and Engineering Chemistry Vol.123 No.-
Tumor microenvironment is characterized by low pH, high reactive oxygen species and hypoxia, whichprovides a suitable environment for cancer growth. The hypoxia not only elevates tumor angiogenesisand metastasis, but also is responsible for the development of treatment resistance, which graduallybecomes a significant impediment for cancer therapy. Therefore, we developed a biomimetic nanosystemcontaining hemoglobin extracted from red blood cells, chemotherapy drug sorafenib, sensitizer ursolicacid and photosensitizer indocyanine green for enhanced chemo-photo combination therapy of hepatocellularcarcinoma, which could not only enhance the chemotherapy effect of sorafenib bowing to thesensitizing effect of ursolic acid, but also achieved synergetic phototherapy in virtue of indocyaninegreen. Besides, the nanoparticles could effectively delivery exogenous oxygen to tumor site and amelioratethe tumor hypoxic environment with the assistance of hemoglobin. The dual-sensitization drugdelivery system was expected to effectively reduce the resistance of traditional treatment methodsagainst tumor hypoxia, providing a novel prospect for the synergistic hepatocellular carcinomatreatment.
Yang Yanhong,Chen Zhiyong,Le Huan 대한독성 유전단백체 학회 2023 Molecular & cellular toxicology Vol.19 No.1
Background It is reported that LncRNAs play an important role in various diseases, including myocardial ischemia–reperfusion injury. However, the regulatory mechanism of LncRNAs in I/R injury of cardiac has not been fully elucidated. Objective This study aimed to explore the interaction of LncRNA MALAT1 and aberrant histone modification in I/R injury cardiomyocytes. Results After myocardial I/R or H/R injury, the expression level of CTCF was up-regulated and MALAT1 was downregulated. Silencing of CTCF promoted the cardiomyocytes survival and apoptosis after H/R treatment. Moreover, the expression of H3K27me3 was significantly inhibited by CTCF down-regulation. H3K27me3 protein could directly bind to the promoter of MALAT1. In addition, we found that the inhibition CTCF could up-regulate the expression of MALAT1 in cardiomyocytes. In addition, down-regulation of MALAT1 could reverse the effects of silencing of CTCF on cardiomyocytes growth and apoptosis in H/R injury. Furthermore, the bioinformatic analysis showed 12 potential targets, while only miR- 26b-5p could directly bind with MALAT1. The inhibition of CTCF repressed the miR-26b-5p expression and the silencing of MALAT1 promoted miR-26b-5p expression. Besides, the miR-26b-5p was decreased in cardiomyocytes under H/R treatment. Overexpression of MALAT1 significantly promoted cardiomyocytes cell growth and repressed cell apoptosis, while the miR-26b-5p reversed these effects. In myocardial I/R injury mice model, overexpression of MALAT1 alleviated the myocardial tissue injury and repressed the H3K27me3 level, however, all those effects were reversed by CTCF. Conclusions CTCF was highly expressed in H/R cardiomyocytes and I/R myocardial tissue and the silencing of CTCFmediated H3K27me3 dissociating from the MALAT1 promoter to regulate cardiomyocytes survival and apoptosis by targeting miR-26b-5p. It provided a new therapeutic marker for myocardial I/R injury.
Automatic Extraction of Lean Tissue for Pork Grading
Cho, Sung-Ho,Huan, Le Ngoc,Choi, Sun,Kim, Tae-Jung,Shin, Wu-Hyun,Hwang, Heon Korean Society for Agricultural Machinery 2014 바이오시스템공학 Vol.39 No.3
Purpose: A robust, efficient auto-grading computer vision system for meat carcasses is in high demand by researchers all over the world. In this paper, we discuss our study, in which we developed a system to speed up line processing and provide reliable results for pork grading, comparing the results of our algorithms with visual human subjectivity measurements. Methods: We differentiated fat and lean using an entropic correlation algorithm. We also developed a self-designed robust segmentation algorithm that successfully segmented several porkcut samples; this algorithm can help to eliminate the current issues associated with autothresholding. Results: In this study, we carefully considered the key step of autoextracting lean tissue. We introduced a self-proposed scheme and implemented it in over 200 pork-cut samples. The accuracy and computation time were acceptable, showing excellent potential for use in online commercial systems. Conclusions: This paper summarizes the main results reported in recent application studies, which include modifying and smoothing the lean area of pork-cut sections of commercial fresh pork by human experts for an auto-grading process. The developed algorithms were implemented in a prototype mobile processing unit, which can be implemented at the pork processing site.