Prostaglandin E2(PGE2) serves as the ultimate mediator of fever induced by infiammatory factors. In contrast to cyclooxygenase inhibitors that suppress arachidonic acid metabolism, antipyretic herbs possess a well-est...Prostaglandin E2(PGE2) serves as the ultimate mediator of fever induced by infiammatory factors. In contrast to cyclooxygenase inhibitors that suppress arachidonic acid metabolism, antipyretic herbs possess a well-established clinical history in effectively managing fever. However, the specific mechanisms underlying their efficacy remain unclear. Following the screening for lead compounds that inhibit PGE2from antipyretic herbs, alkynylated active molecule probes were designed and synthesized to track and identify potential targets. The target investigation revealed that three antipyretic compounds, namely cinnamaldehyde, 2,4-decadienal, and perillaldehyde, containing α,β-unsaturated aldehyde groups irreversibly targeted the microsomal PGES1-TM4 helix(m PGES1-TM4) at Ser139. This specific interaction effectually inhibited PGE2 production in the cerebral vasculature, leading to exert potent antipyretic effects.α,β-Unsaturated aldehydes targeting m PGES1-TM4 offer a new approach for antipyretic effects with significant potential for various applications.展开更多
The Panxi Rift Zone is a famous metallogenic province in Southwest China. Continental rifting developed in Hercynian period (P 2, 260～250Ma) accompany with a series of basic\|ultrabasic rocks. Various in lithologies,...The Panxi Rift Zone is a famous metallogenic province in Southwest China. Continental rifting developed in Hercynian period (P 2, 260～250Ma) accompany with a series of basic\|ultrabasic rocks. Various in lithologies, such as layered intrusions (V\|Ti\|Fe formation), small\|sized mafic\|ultramafic bodies (stocks) and large\|scale basalt (Emeishan Basalt) are constituted of a complete melanocratic rock system.Most of Cu\|Ni\|PGE sulfide deposits are related to small\|sized ultramafic rock bodies. It is a perfect possibility for them to be an affinity of basic eruptive lava and for the neck facies. But in ① Panzhihua\|Center Yunnan Province, the Gaojiacun, also Jinbaoshan, as large stratiform basic\|ultrabasic complex used to be thought that is older one intruded to basement rocks in Precambrian. However, new evidences suggest it is similar with the small\|sized ultramafic rock bodies containing Cu\|Ni\|PGE, and also the both are affinity of the Emeishan Basalt; ② Miyi district, Cu\|Pt mineralization was discovered in the Xinjie bedded basic complex, and in where ophitic olivine\|pyroxenite\|peridotite facies are exactly Pt\|bearing layers; ③ Longzhoushan district, we have recently researched basic\|ultrabasic clusters which intruded into fracture zones, and Cu\|Ni\|Pt, Pd mineralization developed at the salbands.Generally, the basalt is poor in PGE and rich in Cu. It is suggested as the result of PGE dispersion\|concentration processing in the melanocratic rock system when rifting happened.展开更多
基金supported by the National Key R&D Program of China (Nos. 2022YFC3500800 and 2022YFC3500805)。
文摘Prostaglandin E2(PGE2) serves as the ultimate mediator of fever induced by infiammatory factors. In contrast to cyclooxygenase inhibitors that suppress arachidonic acid metabolism, antipyretic herbs possess a well-established clinical history in effectively managing fever. However, the specific mechanisms underlying their efficacy remain unclear. Following the screening for lead compounds that inhibit PGE2from antipyretic herbs, alkynylated active molecule probes were designed and synthesized to track and identify potential targets. The target investigation revealed that three antipyretic compounds, namely cinnamaldehyde, 2,4-decadienal, and perillaldehyde, containing α,β-unsaturated aldehyde groups irreversibly targeted the microsomal PGES1-TM4 helix(m PGES1-TM4) at Ser139. This specific interaction effectually inhibited PGE2 production in the cerebral vasculature, leading to exert potent antipyretic effects.α,β-Unsaturated aldehydes targeting m PGES1-TM4 offer a new approach for antipyretic effects with significant potential for various applications.
文摘The Panxi Rift Zone is a famous metallogenic province in Southwest China. Continental rifting developed in Hercynian period (P 2, 260～250Ma) accompany with a series of basic\|ultrabasic rocks. Various in lithologies, such as layered intrusions (V\|Ti\|Fe formation), small\|sized mafic\|ultramafic bodies (stocks) and large\|scale basalt (Emeishan Basalt) are constituted of a complete melanocratic rock system.Most of Cu\|Ni\|PGE sulfide deposits are related to small\|sized ultramafic rock bodies. It is a perfect possibility for them to be an affinity of basic eruptive lava and for the neck facies. But in ① Panzhihua\|Center Yunnan Province, the Gaojiacun, also Jinbaoshan, as large stratiform basic\|ultrabasic complex used to be thought that is older one intruded to basement rocks in Precambrian. However, new evidences suggest it is similar with the small\|sized ultramafic rock bodies containing Cu\|Ni\|PGE, and also the both are affinity of the Emeishan Basalt; ② Miyi district, Cu\|Pt mineralization was discovered in the Xinjie bedded basic complex, and in where ophitic olivine\|pyroxenite\|peridotite facies are exactly Pt\|bearing layers; ③ Longzhoushan district, we have recently researched basic\|ultrabasic clusters which intruded into fracture zones, and Cu\|Ni\|Pt, Pd mineralization developed at the salbands.Generally, the basalt is poor in PGE and rich in Cu. It is suggested as the result of PGE dispersion\|concentration processing in the melanocratic rock system when rifting happened.
