Disulfiram reduces the severity of mouse acute pancreatitis by inhibiting RIPK1-dependent acinar cell necrosis
In this study, we aim to investigate the effect of DSF on pancreatic acinar cell necrosis, and to explore the underlying mechanisms. Cell necrosis was induced by sodium taurocholate or caerulein, AP mice model was induced by nine hourly injections of caerulein. Network pharmacology, molecular docking, and molecular dynamics simulation were used to explore the potential targets of DSF in protecting against cell necrosis. The results indicated that DSF significantly inhibited acinar cell necrosis as evidenced by a decreased ratio of necrotic cells in the pancreas. Network pharmacology, molecular docking, and molecular dynami...
Source: Bioorganic Chemistry - January 30, 2023 Category: Chemistry Authors: Qiu-Yang Huang Rui Zhang Qing-Yu Zhang Chen Dai Xiu-Yan Yu Lu Yuan Yi-Yuan Liu Yan Shen Kui-Long Huang Zhi-Hua Lin Source Type: research

Aggregation-Induced emission photosensitizer with lysosomal response for photodynamic therapy against cancer
This study indicates that SIN has potential as a multifunctional organic photosensitizer for bioimaging and PDT of tumor.PMID:36716644 | DOI:10.1016/j.bioorg.2023.106349 (Source: Bioorganic Chemistry)
Source: Bioorganic Chemistry - January 30, 2023 Category: Chemistry Authors: Zhenxing Pan Yakun Wang Niping Chen Guining Cao Yaoxun Zeng Jiapeng Dong Mingzhao Liu Zhaoyi Ye Yushan Li Shun Huang Yu-Jing Lu Yan He Xujie Liu Kun Zhang Source Type: research

Novel terpestacin derivatives with l-amino acid residue as anticancer agents against U87MG-derived glioblastoma stem cells
Bioorg Chem. 2023 Jan 24;132:106392. doi: 10.1016/j.bioorg.2023.106392. Online ahead of print.ABSTRACTBased on the natural product terpestacin, seventeen derivatives (1-17) with various l-amino acid side chains were designed and synthesized. Their anticancer activities against U87MG-derived glioblastoma stem cells (GSCs) were evaluated, and compounds 5, 11, 13 and 15 showed strong abilities to inhibit the proliferation (IC50 = 2.8-6.9 μM) and tumorsphere formation of GSCs. Besides, compounds 13 and 15 could effectively induce apoptosis and significantly inhibit the invasion of GSCs (95 and 97 % inhibition, respectively, a...
Source: Bioorganic Chemistry - January 29, 2023 Category: Chemistry Authors: Shengrong Liao Nayeong Yuk Yu Jin Kim Huayan Xu Xiaolin Li Ling Wang Yonghong Liu Hye Jin Jung Source Type: research

Novel terpestacin derivatives with l-amino acid residue as anticancer agents against U87MG-derived glioblastoma stem cells
Bioorg Chem. 2023 Jan 24;132:106392. doi: 10.1016/j.bioorg.2023.106392. Online ahead of print.ABSTRACTBased on the natural product terpestacin, seventeen derivatives (1-17) with various l-amino acid side chains were designed and synthesized. Their anticancer activities against U87MG-derived glioblastoma stem cells (GSCs) were evaluated, and compounds 5, 11, 13 and 15 showed strong abilities to inhibit the proliferation (IC50 = 2.8-6.9 μM) and tumorsphere formation of GSCs. Besides, compounds 13 and 15 could effectively induce apoptosis and significantly inhibit the invasion of GSCs (95 and 97 % inhibition, respectively, a...
Source: Bioorganic Chemistry - January 29, 2023 Category: Chemistry Authors: Shengrong Liao Nayeong Yuk Yu Jin Kim Huayan Xu Xiaolin Li Ling Wang Yonghong Liu Hye Jin Jung Source Type: research

A near infrared two-channel fluorescent probe for the detection of hydrogen sulfide and viscosity with a negligible crosstalk influence
Bioorg Chem. 2023 Jan 20;132:106379. doi: 10.1016/j.bioorg.2023.106379. Online ahead of print.ABSTRACTBoth imbalance of H2S production and the change of viscosity in cells are associated with many diseases such as inflammation, Alzheimer's disease, and Parkinson's disease. Thus, the development of two-channel fluorescent probes for the detection of H2S and viscosity is of great significance for the study of pathogenic mechanisms. Herein, we design a two-channel NIR fluorescent probe RHO-DCO-DNP, which was able to selectively respond to H2S in one channel (λex = 580 nm, λem = 760 nm) and to viscosity in another channel (...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Meng Liu Jianwen Qiu Xinyi Xiong Shaofei Fu Linhao Guan Maihong He Yong Gao Source Type: research

Screening and characterization of a β-xylosidase from Bifidobacterium breve K-110 and its application in the biotransformation of the total flavonoids of epimedium to icariin with α-l-rhamnosidase
This study is the first to screen xylosidases for the targeted conversion of epimedin B to produce icariin, and the first to report that epimedin B and epimedin C in the raw epimedium flavonoids can convert efficiently to icariin by a collaborative of β-xylosidase and α-l-rhamnosidase.PMID:36706530 | DOI:10.1016/j.bioorg.2023.106364 (Source: Bioorganic Chemistry)
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Jingwen Su Tao Wu Shiping Cao Jianjun Pei Linguo Zhao Source Type: research

The antimicrobial peptide LK2(6)A(L) exhibits anti-inflammatory activity by binding to the myeloid differentiation 2 domain and protects against LPS-induced acute lung injury in mice
Bioorg Chem. 2023 Jan 18;132:106376. doi: 10.1016/j.bioorg.2023.106376. Online ahead of print.ABSTRACTAcute lung injury (ALI) is a life-threatening disease that is generally attributable to an uncontrolled inflammatory response in the lung, but there is a lack of effective treatments. At present, regulating the inflammatory response has become an important strategy for treating ALI. In the present study, LK2(6)A(L), a peptide derived from the natural antimicrobial peptide temporin-1CEa, inhibited lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), and NO in RAW264.7 ce...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Juan Zhang Yue Sun Chengpeng Sun Dejing Shang Source Type: research

Enantiomeric pairs of macrocyclic acylphloroglucinols from Syzygium szemaoense
Bioorg Chem. 2023 Jan 20;132:106381. doi: 10.1016/j.bioorg.2023.106381. Online ahead of print.ABSTRACTTwo enantiomeric pairs of macrocyclic acylphloroglucinols (1a/1b and 2a/2b) with an unprecedented carbon skeleton featuring a bicyclo[12.3.1]octadecane core, together with an undescribed biogenetically related long-chain acylphloroglucinol (3), were isolated from Syzygium szemaoense. Their structures were fully established by spectroscopic method, X-ray crystallographic analysis, and ECD calculation. Compounds 1b and 2a/2b exhibited inhibition against death-associated protein kinase-related apoptosis inducing protein kinas...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Jin-Chang Huang Hong-Hong Xu Qing Shi Chun Lei Jing-Ya Li Ai-Jun Hou Source Type: research

A near infrared two-channel fluorescent probe for the detection of hydrogen sulfide and viscosity with a negligible crosstalk influence
Bioorg Chem. 2023 Jan 20;132:106379. doi: 10.1016/j.bioorg.2023.106379. Online ahead of print.ABSTRACTBoth imbalance of H2S production and the change of viscosity in cells are associated with many diseases such as inflammation, Alzheimer's disease, and Parkinson's disease. Thus, the development of two-channel fluorescent probes for the detection of H2S and viscosity is of great significance for the study of pathogenic mechanisms. Herein, we design a two-channel NIR fluorescent probe RHO-DCO-DNP, which was able to selectively respond to H2S in one channel (λex = 580 nm, λem = 760 nm) and to viscosity in another channel (...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Meng Liu Jianwen Qiu Xinyi Xiong Shaofei Fu Linhao Guan Maihong He Yong Gao Source Type: research

Screening and characterization of a β-xylosidase from Bifidobacterium breve K-110 and its application in the biotransformation of the total flavonoids of epimedium to icariin with α-l-rhamnosidase
This study is the first to screen xylosidases for the targeted conversion of epimedin B to produce icariin, and the first to report that epimedin B and epimedin C in the raw epimedium flavonoids can convert efficiently to icariin by a collaborative of β-xylosidase and α-l-rhamnosidase.PMID:36706530 | DOI:10.1016/j.bioorg.2023.106364 (Source: Bioorganic Chemistry)
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Jingwen Su Tao Wu Shiping Cao Jianjun Pei Linguo Zhao Source Type: research

The antimicrobial peptide LK2(6)A(L) exhibits anti-inflammatory activity by binding to the myeloid differentiation 2 domain and protects against LPS-induced acute lung injury in mice
Bioorg Chem. 2023 Jan 18;132:106376. doi: 10.1016/j.bioorg.2023.106376. Online ahead of print.ABSTRACTAcute lung injury (ALI) is a life-threatening disease that is generally attributable to an uncontrolled inflammatory response in the lung, but there is a lack of effective treatments. At present, regulating the inflammatory response has become an important strategy for treating ALI. In the present study, LK2(6)A(L), a peptide derived from the natural antimicrobial peptide temporin-1CEa, inhibited lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), and NO in RAW264.7 ce...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Juan Zhang Yue Sun Chengpeng Sun Dejing Shang Source Type: research

Enantiomeric pairs of macrocyclic acylphloroglucinols from Syzygium szemaoense
Bioorg Chem. 2023 Jan 20;132:106381. doi: 10.1016/j.bioorg.2023.106381. Online ahead of print.ABSTRACTTwo enantiomeric pairs of macrocyclic acylphloroglucinols (1a/1b and 2a/2b) with an unprecedented carbon skeleton featuring a bicyclo[12.3.1]octadecane core, together with an undescribed biogenetically related long-chain acylphloroglucinol (3), were isolated from Syzygium szemaoense. Their structures were fully established by spectroscopic method, X-ray crystallographic analysis, and ECD calculation. Compounds 1b and 2a/2b exhibited inhibition against death-associated protein kinase-related apoptosis inducing protein kinas...
Source: Bioorganic Chemistry - January 27, 2023 Category: Chemistry Authors: Jin-Chang Huang Hong-Hong Xu Qing Shi Chun Lei Jing-Ya Li Ai-Jun Hou Source Type: research

Design, synthesis and biological evaluation of purine-based derivatives as novel JAK2/BRD4(BD2) dual target inhibitors
Bioorg Chem. 2023 Jan 21;132:106386. doi: 10.1016/j.bioorg.2023.106386. Online ahead of print.ABSTRACTBased on the pharmacological synergy of JAK2 and BRD4 in the NF-κB pathway and positive therapeutic effect of combination of JAK2 and BRD4 inhibitors in treating MPN and inflammation. A series of unique 9H-purine-2,6-diamine derivatives that selectively inhibited Janus kinase 2 (JAK2) and BRD4(BD2) were designed, prepared, and evaluated for their in vitro and in vivo potency. Among them, compound 9j exhibited acceptable inhibitory activity with IC50 values of 13 and 22 nM for BD2 of BRD4 and JAK2, respectively. The wester...
Source: Bioorganic Chemistry - January 26, 2023 Category: Chemistry Authors: Yong Guo Yurong Zou Yong Chen Dexin Deng Zihao Zhang Kongjun Liu Minghai Tang Tao Yang Suhong Fu Chufeng Zhang Wenting Si Ziyan Ma Shunjie Zhang Bin Peng Dingguo Xu Lijuan Chen Source Type: research

Phosphine chalcogenides and their derivatives from red phosphorus and functionalized pyridines, imidazoles, pyrazoles and their antimicrobial and cytostatic activity
Bioorg Chem. 2023 Jan 18;132:106363. doi: 10.1016/j.bioorg.2023.106363. Online ahead of print.ABSTRACTTertiary phosphine oxides, phosphine sulfides, and phosphine selenides containing pyridine, imidazole, and pyrazole groups have been synthesized via the reaction of elemental phosphorus or secondary phosphine oxides with functional pyridines, imidazoles, and pyrazoles. Alkyl tris(2-pyridylethyl)phosphonium iodide and bromide are also obtained by quaternization of the corresponding phosphine. Antimicrobial activity of the synthesized compounds, including nitrogen-containing heterocycles, phosphorus, selenium, and sulfur, wi...
Source: Bioorganic Chemistry - January 26, 2023 Category: Chemistry Authors: Svetlana Malysheva Vladimir Kuimov Lyudmila Belovezhets Natalia Belogorlova Marina Borovskaya Gennadii Borovskii Source Type: research

Design, synthesis and biological evaluation of purine-based derivatives as novel JAK2/BRD4(BD2) dual target inhibitors
Bioorg Chem. 2023 Jan 21;132:106386. doi: 10.1016/j.bioorg.2023.106386. Online ahead of print.ABSTRACTBased on the pharmacological synergy of JAK2 and BRD4 in the NF-κB pathway and positive therapeutic effect of combination of JAK2 and BRD4 inhibitors in treating MPN and inflammation. A series of unique 9H-purine-2,6-diamine derivatives that selectively inhibited Janus kinase 2 (JAK2) and BRD4(BD2) were designed, prepared, and evaluated for their in vitro and in vivo potency. Among them, compound 9j exhibited acceptable inhibitory activity with IC50 values of 13 and 22 nM for BD2 of BRD4 and JAK2, respectively. The wester...
Source: Bioorganic Chemistry - January 26, 2023 Category: Chemistry Authors: Yong Guo Yurong Zou Yong Chen Dexin Deng Zihao Zhang Kongjun Liu Minghai Tang Tao Yang Suhong Fu Chufeng Zhang Wenting Si Ziyan Ma Shunjie Zhang Bin Peng Dingguo Xu Lijuan Chen Source Type: research