Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment

Abstract Excessive fat accumulation and chronic inflammation are two typical characteristics of obesity. AMP‐activated protein kinase (AMPK), a master regulator of energy metabolism, is involved in adipogenesis, lipogenesis, and inflammation modulation in adipose tissue (AT). Thus, effective lipid r...

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Main Authors: Qiaqia Xiao, Lu Tang, Siying Chen, Yijun Mei, Chuying Wang, Jing Yang, Jing Shang, Shengliang Li, Wei Wang
Format: Article
Language:English
Published: Wiley 2024-11-01
Series:Advanced Science
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Online Access:https://doi.org/10.1002/advs.202406985
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author Qiaqia Xiao
Lu Tang
Siying Chen
Yijun Mei
Chuying Wang
Jing Yang
Jing Shang
Shengliang Li
Wei Wang
author_facet Qiaqia Xiao
Lu Tang
Siying Chen
Yijun Mei
Chuying Wang
Jing Yang
Jing Shang
Shengliang Li
Wei Wang
author_sort Qiaqia Xiao
collection DOAJ
description Abstract Excessive fat accumulation and chronic inflammation are two typical characteristics of obesity. AMP‐activated protein kinase (AMPK), a master regulator of energy metabolism, is involved in adipogenesis, lipogenesis, and inflammation modulation in adipose tissue (AT). Thus, effective lipid reduction and anti‐inflammation through AMPK regulation play vital roles in treating obesity. Herein, an anti‐obesity nanosandwich is fabricated through attaching polymetformin (PolyMet) onto photothermal agent black phosphorus nanosheets (BP). PolyMet activates AMPK to inhibit adipogenesis, promote browning, and mitigate AT inflammation by decreasing macrophage infiltration, repolarizing macrophage phenotype, and downregulating pro‐inflammatory cytokines. Additionally, BP induces lipolysis and apoptosis of adipocytes and macrophages through a photothermal effect. By further functionalization using hyaluronic acid (HA) and MMP2 substrate‐linking P3 peptide‐modified HA (P3‐HA), an enhanced anti‐obesity effect is obtained by dual‐targeting of P3 and HA, and HA‐mediated CD44 poly‐clustering after MMP2 cleavage. Upon laser irradiation, the designed nanosandwich (P3‐HA/PM@BP) effectively inhibits obesity development in obese mice, increases M2/M1 ratio in AT, reduces the serum levels of cholesterol/triglyceride and improves insulin sensitivity, exhibiting promising research potential to facilitate the clinical development of modern anti‐obesity therapies.
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issn 2198-3844
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publishDate 2024-11-01
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spelling doaj-art-1fde09a6cde4424b8fbc92f661f218082024-11-20T19:25:40ZengWileyAdvanced Science2198-38442024-11-011143n/an/a10.1002/advs.202406985Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity TreatmentQiaqia Xiao0Lu Tang1Siying Chen2Yijun Mei3Chuying Wang4Jing Yang5Jing Shang6Shengliang Li7Wei Wang8State Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaNMPA Key Laboratory for Research and Evaluation of Cosmetics China Pharmaceutical University Nanjing 211198 P. R. ChinaCollege of Pharmaceutical Sciences Soochow University Suzhou 215123 P. R. ChinaState Key Laboratory of Natural Medicines School of Pharmacy China Pharmaceutical University Nanjing 211198 P. R. ChinaAbstract Excessive fat accumulation and chronic inflammation are two typical characteristics of obesity. AMP‐activated protein kinase (AMPK), a master regulator of energy metabolism, is involved in adipogenesis, lipogenesis, and inflammation modulation in adipose tissue (AT). Thus, effective lipid reduction and anti‐inflammation through AMPK regulation play vital roles in treating obesity. Herein, an anti‐obesity nanosandwich is fabricated through attaching polymetformin (PolyMet) onto photothermal agent black phosphorus nanosheets (BP). PolyMet activates AMPK to inhibit adipogenesis, promote browning, and mitigate AT inflammation by decreasing macrophage infiltration, repolarizing macrophage phenotype, and downregulating pro‐inflammatory cytokines. Additionally, BP induces lipolysis and apoptosis of adipocytes and macrophages through a photothermal effect. By further functionalization using hyaluronic acid (HA) and MMP2 substrate‐linking P3 peptide‐modified HA (P3‐HA), an enhanced anti‐obesity effect is obtained by dual‐targeting of P3 and HA, and HA‐mediated CD44 poly‐clustering after MMP2 cleavage. Upon laser irradiation, the designed nanosandwich (P3‐HA/PM@BP) effectively inhibits obesity development in obese mice, increases M2/M1 ratio in AT, reduces the serum levels of cholesterol/triglyceride and improves insulin sensitivity, exhibiting promising research potential to facilitate the clinical development of modern anti‐obesity therapies.https://doi.org/10.1002/advs.202406985anti‐inflammationblack phosphorus nanosheetlipid reductionnanomedicineobesity
spellingShingle Qiaqia Xiao
Lu Tang
Siying Chen
Yijun Mei
Chuying Wang
Jing Yang
Jing Shang
Shengliang Li
Wei Wang
Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
Advanced Science
anti‐inflammation
black phosphorus nanosheet
lipid reduction
nanomedicine
obesity
title Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
title_full Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
title_fullStr Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
title_full_unstemmed Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
title_short Two‐Pronged Attack: Dual Activation of Fat Reduction Using Near‐Infrared‐Responsive Nanosandwich for Targeted Anti‐Obesity Treatment
title_sort two pronged attack dual activation of fat reduction using near infrared responsive nanosandwich for targeted anti obesity treatment
topic anti‐inflammation
black phosphorus nanosheet
lipid reduction
nanomedicine
obesity
url https://doi.org/10.1002/advs.202406985
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AT siyingchen twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT yijunmei twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT chuyingwang twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT jingyang twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT jingshang twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT shengliangli twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment
AT weiwang twoprongedattackdualactivationoffatreductionusingnearinfraredresponsivenanosandwichfortargetedantiobesitytreatment