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Materials Today Bio · 2025 · IF 10.2

Aminoguanidine-assembled functional DNA tetrahedron alleviates acute lung injury by targeting the cGAS-STING signaling pathway

Yue Chen,Di Wu,Quan Li,Zhenghua Wei,Qian Liu,Jin Li,Daohui Gong,Chaowang Huang,Qianyi You,Hang Qian,Guansong Wang

Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) cause severe lung inflammation and damage, compromising respiratory function. Nanomedicine offers hope in controlling this inflammation. DNA nanostructures, as drug carriers, stand out due to their non-toxic, programmable, and precisely controllable traits. However, they face challenges in physiological stability and functionalization as carriers. Here, we introduce TET AG , DNA tetrahedra assembled and functionalized with aminoguanidine without magnesium. Aminoguanidine not only aids tetrahedron assembly but also inhibits the cyclic GMP-AMP synthase and stimulator of interferon (cGAS-STING) pathway, a key inflammatory signal. By integrating STING siRNA into TET AG (TET AG -STING), we achieve synergistic anti-inflammatory effects in ALI/ARDS. Our results show that TET AG offers improved stability and cellular uptake. Importantly, TET AG -STING exhibits potent anti-inflammatory activity in vitro and in a Lipopolysaccharides-induced mouse model following intratracheal administration. This significantly improves lung injury scores and pulmonary functions. These findings underscore aminoguanidine’s therapeutic potential in ALI/ARDS and highlight the promise of DNA nanostructures in medical applications.

CAS / MDL: 1937-19-5
研究领域: 医学 · 纳米医学 · 分子生物学
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JOURNAL OF MOLECULAR STRUCTURE · 2025 · IF 4.7

Facile synthesis of guanidyl-imidazoline as “Turn-on” Zn2+ fluorescent probe with excellent sensitivity and selectivity in aqueous environment

Guiqing Liu,Yunyi Han,Yuwei Hou,Yanjun Li,Xinxin Yang,Zhaocen Dong,Meili Guan,Xuezhong Gong,Jianguo Tang

In this work, a water-soluble guanidyl-imidazoline ( G ) was synthesized and used as a fluorescent probe to detect Zn 2+ in an aqueous environment without any mutually soluble organic solvent. G demonstrates excellent selectivity for Zn 2+ and strong anti-interference ability against other metal ions. It has an ultra-low detection limit of 25 nM for Zn 2+ ions, surpassing previously reported achievements. Job’s plot method, FTIR and XAFS revealed the binding mode of the G -Zn complex that the N atom in the G coordinates with Zn 2+ in a ratio of 2:1. Furthermore, this probe was successfully utilized for quantitative detection of Zn 2+ ions in tap water and synthetic water, and also applied to imaging Zn 2+ ions in living cells.

研究领域: 化学 · 生物分析 · 材料科学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2025 · IF 5.6

Polymeric porous microneedle-mediated transdermal metformin delivery system: A high-dose sustained-release platform for enhanced glycemic regulation

Yan Li,Sedrati Manar,Xinxiang Chai,Yanzhen Lou,Guohua Jiang

Microneedle technology has emerged as a potential new means of painless drug delivery for diabetic patients. Maintaining blood glucose levels (BGLs) within the normal range for a long time is important for people with diabetes. However, it is a new challenge to realize long-term therapy due to insufficient drug loading. In this study, a polymeric porous microneedle array with continuous micropores was prepared by combining the microtemplate method and pore-causing agent method. By changing the ratio of a pore-causing agent, the fluid uptake capacity and mechanical strength were adjusted to balance the trade-off between rapid imbibition and the mechanical properties of puncture. A special drug loading chamber was developed to realize a large package (135.69 mg) of metformin-loaded porous microneedle system. Experiments in diabetic rat models in vivo showed that the prepared porous microneedles can effectively puncture the skin and maintain stable BGLs up to 7 h × 5 cycles over five experimental cycles (108 h) without the risk of hypoglycemia. These results suggested that the high-dose polymeric porous microneedle-mediated metformin delivery system had the advantages of rapid response and durable release, and was a potential candidate for sustained-release transdermal drug delivery in patients with diabetes mellitus and even chronic conditions.

研究领域: 生物医学工程 · 药剂学 · 材料科学 · 内分泌学
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Journal of Functional Biomaterials · 2024 ·Vol. 15 ·期 12 ·388 · IF 5

Curcumin and Metformin Infinite Coordination Polymer Nanoparticles for Combined Therapy of Diabetic Mice via Intraperitoneal Injections

Siwei Sun,Xinyi Hou,Ke Li,Chenqi Huang,Yu Rong,Jiao Bi,Xueping Li,Daocheng Wu

Metformin (Met) is one of the most commonly prescribed first-line drugs for diabetes treatment. However, it has several issues, including low bioavailability, therapeutic platform, and side effects at high doses. In order to improve the therapeutic efficiency of Met, this study proposes a strategy of using Met and curcumin (Cur) to prepare Cur-Zn(II)-Met infinite coordination polymer nanoparticles (CM ICP NPs), and combining this with intraperitoneal injections, for the treatment of diabetic mice. Fourier transform infrared (FTIR) spectroscopy, X-ray photoelectron spectroscopy (XPS), transmission electron microscopy (TEM), nanoparticle analysis, cytotoxicity experiments, and mice experiments were used to investigate structure, properties, and application effects. The results showed that CM ICP NPs exhibit a high drug encapsulation rate (100%), good stability, and an absence of in vivo and in vitro toxicity. The blood glucose level of diabetic mice after treatment was reduced to 6.7 ± 0.65 mmol/L at the seventh week. In terms of therapeutic mechanism, it appears that Met and Cur can synergistically regulate blood glucose in mice from multiple paths. This study provides a promising method for the treatment of diabetes using Met and other drugs.

研究领域: 药理学 · 生物医学工程 · 代谢疾病研究
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Microbial Cell Factories · 2024 ·Vol. 23 ·期 1 ·1-12 · IF 4.3

Metformin regulates cellulase production in Trichoderma reesei via calcium signaling and mitochondrial function

Wang Jiajia,Chen Yumeng,Cong Jiawei,Wang Wei

Background Trichoderma reesei is renowned for its cellulase-producing ability and is used for biofuel production from lignocellulose. In plants and fungi, cellulase production is induced by cellulose and suppressed by glucose; however, whether metformin can enhance cellulase production and mitochondrial function in T. reesei remains unclear. Metformin reduces blood glucose levels by inhibiting hepatic gluconeogenesis; therefore, it is worth investigating whether metformin transmission modulates cellulase biosynthesis in T. reesei . Results Metformin increased cellulase production and the transcription of cellulase-related genes. It also enhanced the concentrations of Ca 2+ in the cytosol and mitochondria and regulated the transcription levels of cellulase-related genes by modulating calcium homeostasis in T. reesei QM6a. In addition, metformin was identified as an antioxidant that can enhance cellulase activity by reducing reactive oxygen species (ROS). Our results demonstrated that metformin influences the state of mitochondria by enhancing mitochondrial activity and membrane potential to promote cellulase production. Conclusion Collectively, these results indicate that metformin enhances cellulase production, scavenges ROS, and protects mitochondrial activity in T. reesei . Graphical Abstract

CAS / MDL: 9004-34-6
研究领域: 微生物学 · 生物化学 · 生物能源
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JOURNAL OF MOLECULAR LIQUIDS · 2018 · IF 4.513

Functionalization of nanosilica via guanidinium ionic liquid for the recovery of gold ions from aqueous solutions

Chao Xiong,Ying Li,Shixing Wang,Yang Zhou

A new adsorbent was prepared via modifying nanosilica with guanidinium ionic liquids for effectively adsorbing gold ions from aqueous solution. Fourier transform infrared spectrometer (FT-IR), thermogravimetric analysis (TGA) and X-ray photoelectron spectroscopy (XPS) were used to characterize the adsorbent. Batch experiments were applied to investigate the effects of initial pH, initial gold ions concentration, contact time and coexisting ions on the removal of gold ions from aqueous solutions. The adsorbent exhibits an excellent selectivity for gold ions in the presence of Pb(II), Mg(II), Ba(II) and Cu(II) ions. The removal rate of gold ions is higher than 97.06% in the pH ranges from 2 to 5. The maximum uptake was 120.56   mg/g under pH   5. The adsorption kinetic was well described by the pseudo-second-order model. The adsorption isotherm followed Hill model very well. Therefore, the new adsorbent has a potential application in the field of separation of gold ions from aqueous solutions.

研究领域: 材料科学 · 环境科学
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ACS Applied Materials & Interfaces · 2018 · IF 8.097

Facile and Versatile Modification of Cotton Fibers for Persistent Antibacterial Activity and Enhanced Hygroscopicity

Qiuquan Cai,Shuliang Yang,Chao Zhang,Zimeng Li,Xiaodong Li,Zhiquan Shen,Weipu Zhu

Natural fibers with functionalities have attracted considerable attention. However, developing facile and versatile strategies to modify natural fibers is still a challenge. In this study, cotton fibers, the most widely used natural fibers, were partially oxidized by sodium periodate in aqueous solution, to give oxidized cotton fibers containing multiple aldehyde groups on their surface. Then poly(hexamethylene guanidine) was chemically grafted onto the oxidized cotton fibers forming Schiff bases between the terminal amines of poly(hexamethylene guanidine) and the aldehyde groups of oxidized cotton fibers. Finally, carbon–nitrogen double bonds were reduced by sodium cyanoborohydride, to bound poly(hexamethylene guanidine) covalently to the surface of cotton fibers. These functionalized fibers show strong and persistent antibacterial activity: complete inhibition against Escherichia coli and Staphylococcus aureus was maintained even after 1000 consecutive washing in distilled water. On the other hand, cotton fibers with only physically adsorbed poly(hexamethylene guanidine) lost their antibacterial activity entirely after a few washes. According to Cell Counting Kit-8 assay and hemolytic analysis, toxicity did not significantly increase after chemical modification. Attributing to the hydrophilicity of poly(hexamethylene guanidine) coatings, the modified cotton fibers were also more hygroscopic compared to untreated cotton fibers, which can improve the comfort of the fabrics made of modified cotton fibers. This study provides a facile and versatile strategy to prepare modified polysaccharide natural fibers with durable antibacterial activity, biosecurity, and comfortable touch.

CAS / MDL: 5470-11-1 7790-28-5
研究领域: 材料科学 · 生物医学工程 · 纺织科学
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EUROPEAN POLYMER JOURNAL · 2022 · IF 5.546

Synthesis of side-chain functional Poly(ε-caprolactone) via the versatile and robust organo-promoted esterification reaction

Jinbao Xu,Weiguo Liang,Jie Zhang,Zhixian Dong,Caihong Lei

Side-chain functionalized poly( ε -caprolactone) (PCL) is of much ongoing interest in light of its biocompatible and biodegradable features being widely applied in the field of biomaterials, but the versatile and robust protocols for the preparation of PCL-based (co)polymers with functional pendants remaining a challenge. Herein, an organic base of tetramethylguanidine (TMG) promoted esterification reaction of a variety of carboxylic acids and a -Cl of poly( α -chloro- ε -caprolactone) (P( α- Cl - CL)), enabling the direct synthesis of side-chain functional PCL, is described with wide substrate scope in mild reaction condition. It is noteworthy that this protocol affords one versatile and robust method for the preparation of PCL-based functional polymers, which are of high attraction for their application in biological area.

研究领域: 生物材料 · 有机化学
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SEPARATION AND PURIFICATION TECHNOLOGY · 2023 · IF 8.6

“Bridging hydrogen bonds” from guanidine and amidoxime groups on natural bamboo strips as a superantibacterial and knitted adsorbent to efficiently adsorb uranium from simulated seawater

Donghua Jin,Ying Wang,Dalei Song,Jiahui Zhu,Jing Yu,Qi Liu,Jingyuan Liu,Rumin Li,Peili Liu,Jun Wang

Uranium adsorption from seawater can provide a sustainable development path for the future raw material supply of nuclear energy. However, in the process of uranium extraction from seawater, biofouling adheres to the surface of the adsorbent, wasting the adsorption sites and seriously affecting the adsorption capability of the adsorbent. Herein, inspired by the superanti-biofouling property of guanidine groups, a superantibacterial and knitted adsorbent with guanidine and amidoxime groups cografted on natural bamboo strips (G-AOBS) is synthesized to adsorb uranium from simulated seawater. The intrinsic structure of bamboo is not destroyed by the whole grafting process, and G-AOBS still maintains the porous and cellulose crystalline structure. The grafting of guanidine groups improves the hydrophilicity and significantly enhances the anti-biofouling performance, thereby increasing the adsorption capacity for uranium (q e  = 201.4 ± 13.23 mg g −1 at pH = 4 with C 0  = 100 mg L −1 and q e  = 1.04 ± 0.12 mg g −1 in simulated seawater with C 0  = 500 μg L −1 ). According to the results of DFT, the guanidine and amidoxime groups can not only replace one carbonate in uranyl tricarbonate alone to form a more stable coordination structure but also have a synergistic effect between the two, that is, using three “bridging hydrogen bonds” to form the most stable chelation mode with uranyl dicarbonate.

研究领域: 材料科学 · 环境科学 · 化学工程
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ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY · 2023 · IF 6.8

Metformin exposure altered intestinal microbiota composition and metabolites in amphibian larvae

Guang-Li Fu,Qin-Yuan Meng,Yu Chen,Jin-Zhao Xin,Jia-Hui Liu,Wei Dang,Hong-Liang Lu

The antidiabetic pharmaceutical metformin (MET) is largely unmetabolized by the human body. Its residues are readily detectable in various aquatic environments and may have adverse impacts on the growth and survival of aquatic species. To date, its toxicological effects have scarcely been explored in non-fish species. Here, we exposed the tadpoles of black-spotted pond frog ( Pelophylax nigromaculatus ) to different concentrations (0, 1, 10 and 100 μg/L) of MET for 30 days and measured the body size, intestinal microbiota and metabolites to evaluate potential effects of MET exposure in amphibian larvae. MET exposure did not affect the growth and intestinal microbial diversity of tadpoles. However, intestinal microbial composition changed significantly, with some pathogenic bacteria (e.g., bacterial genera Salmonella , Comamonas , Stenotrophomonas , Trichococcus ) increasing and some beneficial bacteria (e.g., Blautia , Prevotella ) decreasing in MET-exposed tadpoles. The levels of some intestinal metabolites associated with growth and immune performance also changed significantly following MET exposure. Overall, our results indicated that exposure to MET, even at environmentally relevant concentrations, would cause intestinal microbiota dysbiosis and metabolite alteration, thereby influencing the health status of non-target aquatic organisms, such as amphibians.

CAS / MDL: 1115-70-4
研究领域: 生态毒理学 · 环境科学 · 微生物学
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METABOLISM-CLINICAL AND EXPERIMENTAL · 2015 · IF 3.894

Methylglyoxal mediates streptozotocin-induced diabetic neuropathic pain via activation of the peripheral TRPA1 and Nav1.8 channels

Qian Huang,Yuan Chen,Nian Gong,Yong-Xiang Wang

Objective Methylglyoxal is known to be associated with the development of nephropathy , retinopathy , and other complications in diabetes. The present study tested the hypothesis that endogenously increased levels of methylglyoxal in diabetes are causally associated with the induction of neuropathic pain . Materials and methods Streptozotocin- and methylglyoxal-induced pain models were established in rats, and the anti-nociceptive effects of the methylglyoxal scavenging agents, selective transient receptor potential channel ankyrin 1 (TRPA1) antagonist, and Nav1.8 antagonist were tested. Results Systemic injection of streptozotocin in rats induced a prolonged increase in plasma methylglyoxal by approximately 60%, which was correlated with the progressive development of mechanical allodynia and thermal hyperalgesia . Local subcutaneous injection of methylglyoxal into the hindpaw produced dose-dependent and biphasic flinching nociceptive responses, which resembled formaldehyde (formalin)-induced nociception . The local methylglyoxal nociception was significantly blocked by co-injection into the hindpaw of the selective transient receptor potential channel ankyrin 1 (TRPA1) antagonist, A967079, and the Nav1.8 antagonist, A803467. Co-incubation with the methylglyoxal scavengers, aminoguanidine , d -arginine, and metformin , reduced the level of free methylglyoxal by more than 90%, and injection of their incubation solutions into the hindpaw produced negligible (3–17%) nociception. Like the clinically effective anti-diabetic neuropathic pain drug gabapentin , systemic injection of aminoguanidine, d -arginine, and metformin at doses that effectively inhibit paw-injected methylglyoxal-induced nociception significantly blocked streptozotocin-induced mechanical allodynia. Conclusion Endogenously increased methylglyoxal may mediate diabetic neuropathic pain via activation of both TRPA1 and Nav1.8 expressed on primary afferent sensory neurons , and injection of methylglyoxal into the hindpaw may serve as a simple and robust model for testing the anti-diabetic pain drugs.

CAS / MDL: 78-98-8 95-54-5
研究领域: 药理学 · 神经科学 · 糖尿病研究 · 疼痛管理
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2020 · IF 4.673

Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety

Xianqing Deng,Mingxia Song

Two series of aminoguanidines containing an alkynyl moiety were designed, synthesised, and screened for antibacterial and anticancer activities. Generally, the series 3a–3j with a 1,2-diphenylethyne exhibited better antibacterial activity than the other series (6a–6k) holding 1,4-diphenylbuta-1,3-diyne moiety antibacterial activity. Most compounds in series 3a–3j showed potent growth inhibition against the tested bacterial strains, with minimum inhibitory concentration (MIC) values in the range 0.25–8 µg/mL. Compound 3g demonstrated rapid and persistent bactericidal activity at 2 × MIC. The resistance study revealed that resistance of the tested bacteria towards 3g is not easily developed. Molecular docking studies revealed that compounds 3g and 6e bind strongly to the LpxC and FabH enzymes. Moreover, excellent activity of selected compounds against the growth of cancer cell lines A549 and SGC7901 was also observed, with IC50 values in the range 0.30–4.57 µg/mL. These findings indicate that compounds containing the aminoguanidine moiety are promising candidates for the development of new antibacterial and anticancer agents.

研究领域: 药理学 · 药物化学 · 微生物学 · 肿瘤学
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