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Article ; Online: Adenosine and its derivatives improve exercise performance and exert anti-fatigue effects via AMPK/PGC-1α signaling pathway in mice

Huimin Zhu / Tangna Zhao / Wanbo Zeng / Xiao Dong / Yuan Luo / Xiang Li / Aiping Zhang / Weiguo Shi / Liang Xu

Arabian Journal of Chemistry, Vol 17, Iss 1, Pp 105490- (2024)

1481

Abstract: Studies of the AMPK/PGC-1α signaling pathway and exercise-induced metabolism have facilitated the development of anti-fatigue agents and exercise mimetics. In this work, adenosine and its 22 derivatives, typical of substitutions at the hydroxyl group of ... ...

Abstract	Studies of the AMPK/PGC-1α signaling pathway and exercise-induced metabolism have facilitated the development of anti-fatigue agents and exercise mimetics. In this work, adenosine and its 22 derivatives, typical of substitutions at the hydroxyl group of the sugar moiety, were firstly evaluated as anti-fatigue agents. In the running wheel tests, adenosine and most derivatives demonstrated a significant increase in the exhaustion distance when compared to the control group. Particularly, the optimized compound 2 exhibited a 3.1-fold increase in exhaustion distance compared to the positive control group treated with AICAR, and a remarkable 9.8-fold increase compared to the blank control group. Furthermore, improved performances were observed in weight-loaded swimming, high jumping, hanging wire, and tail suspension tests. Compound 2 not only reduced levels of lactic acid (LA) and blood urea nitrogen (BUN), but also preserved hepatic and muscle glycogen content during exercise. Notably, compound 2 activated AMPK/PGC-1α pathway without stimulating the central nervous system. Moreover, compound 2 demonstrated a favorable safety in vivo at a dose of 1.96 × 10-5 mol/kg for 21 days. This study unveils, for the first time, the ability of adenosine and its derivatives to resist exercise-induced fatigue, thereby providing promising lead compounds for the development of drugs aimed to prevent and treat fatigue-related diseases. Moreover, it sheds light on the potential therapeutic approaches utilizing endogenous substance.
Keywords	Adenosine derivative ; Substitution ; Anti-fatigue ; AMPK ; Chemistry ; QD1-999
Subject code	796
Language	English
Publishing date	2024-01-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Studies on the Effect of Lipofectamine and Cell-Penetrating Peptide on the Properties of 10-23 DNAzyme

Huanhuan Liu / Yang Li / Shanshan Du / Chenhong Wang / Yuexiang Li / Ruiyuan Cao / Weiguo Shi / Shihui Liu / Junlin He

Molecules, Vol 28, Iss 3942, p

2023 Volume 3942

Abstract: Cationic polymeric materials and cell-penetrating peptides (CPPs) were often used as the delivery vectors in the evaluation of nucleic acid therapeutics. 10-23 DNAzyme is a kind of potential antisense therapeutics by catalytic cleavage of the disease- ... ...

Abstract	Cationic polymeric materials and cell-penetrating peptides (CPPs) were often used as the delivery vectors in the evaluation of nucleic acid therapeutics. 10-23 DNAzyme is a kind of potential antisense therapeutics by catalytic cleavage of the disease-related RNAs. Here, lipofectamine 2000 and Tat peptide were evaluated for their effect on the catalytic activity of 10-23 DNAzyme, with the observed rate constant, thermal stability, CD spectra, and PAGE analysis, with a duplex DNA mimicking DNAzyme-substrate as a control. It was shown that the cationic carriers had a negative effect on the catalytic performance of the 10-23 DNAzyme. Significantly, the destabilizing effect of the cationic carriers on the duplex formation was noteworthy, as a duplex formation is an essential prerequisite in the silencing mechanisms of antisense and RNAi.
Keywords	10-23 DNAzyme ; cell-penetrating peptide ; lipofectamine 2000 ; observed rate constant ; T m ; CD spetra ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2023-05-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis and biological evaluation of a peptide-remifentanil conjugate as a novel bifunctional mu/delta-opioid receptor agonist for the treatment of pain

Lu Wang / Jing Li / Fengxia Ren / Hongxin Jia / Zixing Yu / Jingchao Cheng / Tao Zhang / Weiguo Shi / Xuesong Feng

Arabian Journal of Chemistry, Vol 16, Iss 8, Pp 105018- (2023)

2023

Abstract: For the treatment of pain, the design of a bifunctional mu-opioid receptor (MOR)/delta-opioid receptor (DOR) agonist is an effective strategy to seek safer opioids with higher antinociceptive efficacy and diminished adverse side effects. Herein, we ... ...

Abstract	For the treatment of pain, the design of a bifunctional mu-opioid receptor (MOR)/delta-opioid receptor (DOR) agonist is an effective strategy to seek safer opioids with higher antinociceptive efficacy and diminished adverse side effects. Herein, we describe the design, synthesis, and evaluation of a novel bivalent ligand (SW-WL-2) with a methyl 1-(3-methoxy-3-oxopropyl)-4-(phenylamino) piperidine- 4-carboxylate moiety (remifentanil derivative) covalently linked to a dermorphin-like structure (H-Dmt-N-Me-D-Ala-Aba-Gly-NH2, BVD03) at the C-terminus. Our results showed that SW-WL-2 behaved as a potent dual agonist of MOR and DOR with significant and prolonged antinociceptive effects in acute pain models in vivo. Furthermore, SW-WL-2 exhibited reduced or no opioid-like side effects such as physical dependence or respiratory depression, in contrast to an equipotent analgesic dose of morphine or BVD03. Thus, SW-WL-2 should be used as a new lead compound for the discovery of safer opioid drugs for the treatment of pain.
Keywords	Safer opioids ; Peptide-fentanyl conjugate ; Bifunctional mu/delta opioid receptor agonists ; Antinociceptive ; Bivalent ligands ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2023-08-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: A novel camptothecin derivative, ZBH-01, exhibits superior antitumor efficacy than irinotecan by regulating the cell cycle

Yongqi Li / Dawei Zhao / Wenqiu Zhang / Miaomiao Yang / Zhihui Wu / Weiguo Shi / Shijie Lan / Zhen Guo / Hong Yu / Di Wu

Journal of Translational Medicine, Vol 21, Iss 1, Pp 1-

2023 Volume 17

Abstract: Abstract Background Irinotecan (CPT-11) is a classic chemotherapeutic agent that plays an important role in the clinical treatment of metastatic colon cancer and other malignant tumors. We previously designed a series of novel irinotecan derivatives. In ... ...

Abstract	Abstract Background Irinotecan (CPT-11) is a classic chemotherapeutic agent that plays an important role in the clinical treatment of metastatic colon cancer and other malignant tumors. We previously designed a series of novel irinotecan derivatives. In this study, we select one representative, ZBH-01, to investigate its sophisticated antitumor mechanism in colon tumor cells. Methods The cytotoxic activity of ZBH-01 on colon cancer cells was evaluate by MTT or Cell Counting Kit-8 (CCK8) assay, 3D and xenograft model. The inhibitory effect of ZBH-01 on TOP1 was detected by DNA relaxation assay and Immuno Complex of Ezyme (ICE) bioassay. The molecular mechanism of ZBH-01 was explored by Next-Generation Sequencing (NGS), bioinformatics analyses, flow cytometry, qRT-PCR, and western blot etc. Results ZBH-01 can induce obvious DNA damage and has superior antitumor activity against colon cancer cells compared to CPT-11 and SN38 (7-Ethyl-10-hydroxy camptothecin, the in vivo active form of CPT-11) both in vivo and in vitro. Its inhibitory effect on topoisomerase I (TOP1) was also comparable with these two control drugs. There are a much larger number of 842 downregulated and 927 upregulated mRNAs in ZBH-01 treatment group than that in the controls. The most significantly enriched KEGG pathways for these dysregulated mRNAs were DNA replication, the p53 signaling pathway, and the cell cycle. After constructing a protein–protein interaction (PPI) network and screening out a prominent cluster, 14 involved in the cell cycle process was identified. Consistently, ZBH-01 induced G0/G1 phase arrest in colon cancer cells, while CPT-11/SN38 caused S phase arrest. The initiation of apoptosis by ZBH-01 was also superior to CPT-11/SN38, followed by the increased expression of Bax, active caspase 3, and cleaved-PARP, and decreased expression of Bcl-2. Additionally, CCNA2 (cyclin A2), CDK2 (cyclin-dependent kinase 2), and MYBL2 (MYB proto-oncogene like 2) might be involved in the G0/G1 cell cycle arrest induced by ZBH-01. Conclusions ...
Keywords	Irinotecan derivative ZBH-01 ; Colorectal cancer ; Next-generation sequencing ; Differentially expressed genes ; Cell cycle ; Apoptosis ; Medicine ; R
Subject code	610
Language	English
Publishing date	2023-06-01T00:00:00Z
Publisher	BMC
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain

Kun Tong / Ruotian Zhang / Fengzhi Ren / Tao Zhang / Junlin He / Jingchao Cheng / Zixing Yu / Fengxia Ren / Yatong Zhang / Weiguo Shi

Molecules, Vol 26, Iss 1716, p

2021 Volume 1716

Abstract: Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a , 6e , and 6f containing the benzofuran group displayed more ... ...

Abstract	Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a , 6e , and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Na v 1.7 and anti-Na v 1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a , 6e , and 6f , which have inhibitory potency for two pain-related Na v targets, could serve as new leads for the development of analgesic medicines.
Keywords	α-aminoamides ; sodium channel blocker ; Na v 1.7 ; Na v 1.8 ; dual channel inhibitors ; Organic chemistry ; QD241-441
Language	English
Publishing date	2021-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis and Evaluation of Novel Biased μ-Opioid-Receptor (μOR) Agonists

Mengjun Ma / Jialin Sun / Menghua Li / Zixing Yu / Jingchao Cheng / Bohua Zhong / Weiguo Shi

Molecules, Vol 24, Iss 2, p

2019 Volume 259

Abstract: Biased’ ligands of G protein-coupled receptors (GPCRs) represent a type of promising analgesic with reduced on-target side effects. PZM21, a potent μ-opioid-receptor (μOR)-biased agonist with a new chemical scaffold compared to classic opioids, has been ...

Abstract	‘Biased’ ligands of G protein-coupled receptors (GPCRs) represent a type of promising analgesic with reduced on-target side effects. PZM21, a potent μ-opioid-receptor (μOR)-biased agonist with a new chemical scaffold compared to classic opioids, has been identified as a therapeutic lead molecule for treating pain. In the current study, novel PZM21 analogues were synthesized and evaluated for their in vitro and in vivo efficacy. Novel compound 7a and PZM21 demonstrated undetectable β-arrestin-2 recruitment, however, their analgesic effects need to be further confirmed. Compounds 7b, 7d, and 7g were stronger analgesics than PZM21 in both the mouse formalin injection assay and the writhing test. Compound 7d was the most potent analogue, requiring a dose that was 1/16th to 1/4th of that of PZM21 for its analgesic activity in the two assays, respectively. Therefore, compound 7d could serve as a lead to develop new biased μOR agonists for treating pain.
Keywords	μOR-biased agonist ; PZM21 ; Gi signaling pathway ; β-arrestin-2 recruitment ; structure–activity relationship ; Organic chemistry ; QD241-441
Language	English
Publishing date	2019-01-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Ethyl 2-[(tert-butoxycarbonyl)amino]thiazole-5-carboxylate

Bohua Zhong / Weisong Wang / Weiguo Shi

Acta Crystallographica Section E, Vol 68, Iss 3, Pp o747-o

2012 Volume 747

Abstract: In the crystal of the title compound, C11H16N2O4S, molecules are linked via pairs of N—H.N hydrogen bonds to form inversion dimers. The dimers are linked by a weak C—H.O interaction to form chains propagating along direction [100]. ...

Abstract	In the crystal of the title compound, C11H16N2O4S, molecules are linked via pairs of N—H.N hydrogen bonds to form inversion dimers. The dimers are linked by a weak C—H.O interaction to form chains propagating along direction [100].
Keywords	Chemistry ; QD1-999 ; Science ; Q ; DOAJ:Chemistry (General) ; DOAJ:Chemistry
Language	English
Publishing date	2012-03-01T00:00:00Z
Publisher	International Union of Crystallography
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis and Evaluation of Novel α-Aminoamides Containing an Indole Moiety for the Treatment of Neuropathic Pain

Haotian Li / Shiyong Fan / Jingchao Cheng / Ping Zhang / Bohua Zhong / Weiguo Shi

Molecules, Vol 21, Iss 7, p

2016 Volume 793

Abstract: The α-aminoamide family of sodium ion channel blockers have exhibited analgesic effects on neuropathic pain. Here, a series of novel α-aminoamides containing an indole ring were designed and synthesized. These compounds were evaluated in mice using a ... ...

Abstract	The α-aminoamide family of sodium ion channel blockers have exhibited analgesic effects on neuropathic pain. Here, a series of novel α-aminoamides containing an indole ring were designed and synthesized. These compounds were evaluated in mice using a formalin test and they exhibited significant anti-allodynia activities. However, the analgesic mechanism of these compounds remains unclear; a subset of the synthesized compounds can only moderately inhibit the sodium ion channel, Nav1.7, in a whole-cell patch clamp assay. Overall, these results suggest that introduction of an indole moiety to α-aminoamide derivatives can significantly improve their bioactivity and further study is warranted.
Keywords	neuropathic pain ; α-aminoamide derivatives ; voltage-gated sodium channel blockers ; Organic chemistry ; QD241-441
Language	English
Publishing date	2016-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: A novel bispecific peptide HIV-1 fusion inhibitor targeting the N-terminal heptad repeat and fusion peptide domains in gp41

Jiang, Xifeng / Qiyan Jia / Lu Lu / Fei Yu / Jishen Zheng / Weiguo Shi / Lifeng Cai / Shibo Jiang / Keliang Liu

Amino acids. 2016 Dec., v. 48, no. 12

2016

Abstract: HIV-1 fusion with the target cell is initiated by the insertion of the gp41 fusion peptide (FP) into the target cell membrane and the interaction between the gp41Â N- and C-terminal heptad repeats (NHR and CHR), followed by the formation of the six-helix ...

Abstract	HIV-1 fusion with the target cell is initiated by the insertion of the gp41 fusion peptide (FP) into the target cell membrane and the interaction between the gp41Â N- and C-terminal heptad repeats (NHR and CHR), followed by the formation of the six-helix bundle (6-HB) fusion core. Therefore, both FP and NHR are important targets for HIV-1 fusion inhibitors. Here, we designed and synthesized a dual-target peptidic HIV-1 fusion inhibitor, 4HR-LBD-VIRIP, in which 4HR-LBD is able to bind to the gp41 NHR domain, while VIRIP is able to interact with gp41 FP. We found that 4HR-LBD-VIRIP is about tenfold more potent than 4HR-LBD and VIRIP in inhibiting HIV-1IIIB infection and HIV-1 envelope glycoprotein (Env)-mediated cellâcell fusion, suggesting that this dual-target HIV-1 fusion inhibitor possesses a strong synergistic antiviral effect. A biophysical analysis indicates that 4HR-LBD-VIRIP can interact with N70 peptide that contains the gp41 NHR and FP domains and binds with lipid membrane. This study provides a new approach for designing novel viral fusion inhibitors against HIV and other enveloped viruses with class I membrane fusion proteins.
Keywords	Human immunodeficiency virus 1 ; antiviral properties ; cell membranes ; glycoproteins ; lipids ; membrane fusion ; viruses
Language	English
Dates of publication	2016-12
Size	p. 2867-2873.
Publishing place	Springer Vienna
Document type	Article
ZDB-ID	1121341-3
ISSN	1438-2199 ; 0939-4451
ISSN (online)	1438-2199
ISSN	0939-4451
DOI	10.1007/s00726-016-2325-x
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Synthesis and Biological Evaluation of Novel 10-Substituted-7-ethyl-10-hydroxycamptothecin (SN-38) Prodrugs

Mo Zhou / Meixia Liu / Xinhua He / Hong Yu / Di Wu / Yishan Yao / Shiyong Fan / Ping Zhang / Weiguo Shi / Bohua Zhong

Molecules, Vol 19, Iss 12, Pp 19718-

2014 Volume 19731

Abstract: In an attempt to improve the antitumor activity and reduce the side effects of irinotecan (2), novel prodrugs of SN-38 (3) were prepared by conjugating amino acids or dipeptides to the 10-hydroxyl group of SN-38 via a carbamate linkage. The synthesized ... ...

Abstract	In an attempt to improve the antitumor activity and reduce the side effects of irinotecan (2), novel prodrugs of SN-38 (3) were prepared by conjugating amino acids or dipeptides to the 10-hydroxyl group of SN-38 via a carbamate linkage. The synthesized compounds completely generated SN-38 in pH 7.4 buffer or in human plasma, while remaining stable under acidic conditions. All prodrug compounds demonstrated much greater in vitro antitumor activities against HeLa cells and SGC-7901 cells than irinotecan. The most active compounds, 5h, 7c, 7d, and 7f, exhibited IC50 values that were 1000 times lower against HeLa cells and 30 times lower against SGC-7901 cells than those of irinotecan, and the inhibitory activities of these prodrugs against acetylcholinesterase (AchE) were significantly reduced, with IC50 values more than 6.8 times greater than that of irinotecan. In addition, compound 5e exhibited the same level of tumor growth inhibitory activity as irinotecan (CPT-11) in a human colon xenograft model in vivo.
Keywords	antitumor agent ; camptothecins ; prodrugs ; SN-38 ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2014-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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