Results 51 to 60 of about 118,468,089 (143)

Isocyanate‐Modified Melatplatin(IV) Enhances Antitumor Efficacy via TCF4/COL6A3‐Mediated Extracellular Matrix Remodeling and cGAS‐STING Pathway Activation in Bladder Cancer

Advanced Science, EarlyView.
A series of melatonin‐conjugated platinum(IV) prodrugs was functionalized with isocyanate chains (compounds 5‒12). MP‐12C (compound 11) was identified as the lead candidate, with optimal potency and safety. MP‐12C exhibited greater efficacy than cisplatin by increasing intracellular uptake, reshaping the extracellular matrix, activating the cGAS‐STING ...
Linhui Wang, Xiaomeng Liu, Tao Zhu, Zirun Su, Ruiping Liu, Zhe Li, Kaixuan Du, Kaipeng Jia, Chong Fu, Yuda Lin, Zihan Xue, Zhe Zhang, Chong Shen, Yunkai Qie, Zhouliang Wu, Zhiheng Liu, Kangkang Liu, Jingyuan Xu, Hailong Hu   +18 more
wiley   +1 more source

Regional Intestinal Drug Permeability and Effects of Permeation Enhancers in Rat [PDF]

, 2020
Sufficient colonic absorption is necessary for all systemically acting drugs in dosage forms that release the drug in the large intestine. Preclinically, colonic absorption is often investigated using the rat single-pass intestinal perfusion model.
Hans Lennernäs, David Dahlgren, Sjöblom, Markus, Tobias Olander, Lennernäs, Hans, Olander, Tobias, Cano Cebrián, María José, Mikael Hedeland, Markus Sjöblom, Maria-Jose Cano-Cebrián, Cano-Cebrian, Maria-Jose, Dahlgren, David, Hedeland, Mikael, Lennernäs, Hans,, Dahlgren, David,, Cano-Cebrian, Maria-Jose,, Hedeland, Mikael,, Olander, Tobias,, Sjöblom, Markus,   +18 more
core   +1 more source

SCTR–Expressing Astrocyte–Serotonergic Neuron Signaling Drives Sexual Dimorphism in Depression Through KAT7/H4ac–Foxc2 Epigenetic Axis in an AMPK‐Dependent Manner

Advanced Science, EarlyView.
Astrocytic SCTR modulates depressive‐related phenotypes via AMPKα1, whereas lowered Mt1 blunts Megalin‐dependent AMPKα2 signaling in serotonergic neurons. Diminished AMPKα2 hinders KAT7 nuclear translocation, curtails KAT7 occupancy and H4K8ac at the Foxc2 promoter, and represses Foxc2 transcription, revealing cell‐type‐specific AMPK‐linked epigenetic ...
Fantao Meng, Jing Liu, Juanjuan Dai, Min Wu, Wentao Wang, Mengdi Zhang, Shujun Jiang, Yifan Cao, Lihong Xu, Lin Du, Dan Wang, Di Zhao, Gaofeng Qin, Dong Wang, Wei Li, Chen Li   +15 more
wiley   +1 more source

Effect of supersaturation on absorption of indomethacin and tadalafil in a single pass intestinal perfusion rat model, in the absence and presence of a precipitation inhibitor

, 2020
The effect of the degree of supersaturation (DS) on absorption of the model drugs indomethacin and tadalafil was elucidated in a single-pass intestinal perfusion (SPIP) model in rats.
Strindberg, Sophie, Plum, Jakob, Christiansen, Martin Lau, Stie, Mai Bay, Mullertz, Anette, Nielsen, Line Hagner, Rades, Thomas   +6 more
core   +1 more source

Huntingtin Aggregate‐Responsive Autophagy Gene Circuit Mitigates Disease Pathology in R6/2 Mice

Advanced Science, EarlyView.
CD98‐mediated receptor‐mediated transcytosis enables LIP‐CD98 nanocarriers to cross the blood–brain barrier and deliver ARAA to neurons. mHTT aggregates activate the 11G–NarX sensor, initiating Auto‐P and Trans‐P signaling through the VP48–NarL relay.
Jie Zhu, Xi‐xiu Xie, Lei Li, Chen Tian, Hao‐tian Wang, Xiao‐jie Wang, Xiao‐lin Yu, Gui‐feng Zhang, Rui‐tian Liu   +8 more
wiley   +1 more source

Excipients enhance intestinal absorption of ganciclovir by P-gp inhibition : assessed in vitro by everted gut sac and in situ by improved intestinal perfusion

, 2011
In rats we examined the effects of some common excipients on the intestinal absorption of ganciclovir (GCV), a BCS-III drug and substrate of P-gp, by assessing its in vitro transfer from mucosa to serosa and in situ transepithelial permeation. In vitro,
Li, Ming, Qiu, Jun, Ming Li, Fang Yan, Li, Gao, Luqin Si, Yan, Fang, Abdullah K. Rabba, Pan, Hongping, Rabba, Abdullah K., Jun Qiu, Hongping Pan, Gao Li, Si, Luqin   +13 more
core   +1 more source

Experimental studies on coronary perfusion with pump-oxygenator [PDF]

, 1959
1. Methods of retrograde coronary perfusion and direct coronary artery perfusion in combination with a bubble oxygenator were investigated in dogs. 2.
Hayashi, Naomi
core   +1 more source

Mitochondrial Protection and Neural Repair via ROS‐Responsive Biomimetic Nanoparticles in Intracerebral Hemorrhage

Advanced Science, EarlyView.
A ROS‐responsive biomimetic nanoparticle platform co‐delivers DIDS and Mdivi‐1 to protect mitochondria and promote neural repair after intracerebral hemorrhage. By targeting LPAR1/VDAC1‐related mitochondrial dysfunction, the nanotherapy reduces oxidative injury, neuronal apoptosis, and blood‐brain barrier disruption, improving neurological recovery and
Ling Gao, Li Peng, Xiaobin Zheng, Cong Tan, Chuang Wang, Qijiang Xiong, Weiming Chen, Zhao Yang   +7 more
wiley   +1 more source

Intestinal permeability of N-acetylcysteine is driven by gut microbiota-dependent cysteine palmitoylation

Nature Communications
Trillions of intestinal microbiota are essential to the permeability of orally administered drugs. However, identifying microbial-drug interactions remains challenging due to the highly variable composition of intestinal flora among individuals.
Yu-Hang Zhang, Chen-Shu Dai, Ya-Jie Wang, Wen-Yu Wang, Tian-Tian Qi, Man-Cheng Xia, Gan Zhou, Yi-Min Cui   +7 more
doaj   +1 more source

A Hypothalamic Oxytocinergic–Sympathetic Axis Couples Anxiety Dysregulation With Impaired Tendon–Bone Repair

Advanced Science, EarlyView.
RCI is associated with functional suppression of oxytocinergic neurons in the PVN. Reduced PVNOXT neuronal activity contributes to altered sympathetic regulation involving the IML–sympathetic chain pathway, accompanied by changes in norepinephrine signaling at the BTI.
Liyang Wan, Tingmo Huang, Liyue Zeng, Ruixue Du, Hengshuo Zhang, Shen Liu, Tao Zhang, Jianzhong Hu, Hongbin Lu   +8 more
wiley   +1 more source