Toad venom, a traditional Chinese medicine, has long been used to treat various challenging ailments. Its effectiveness and toxicity can vary depending on the types and concentrations of bufadienolides, which vary from region to region. However, identifying the origin of toad venom is challenging due to the absence of distinct visual characteristics of the original animals. Therefore, developing a scientific and practical method for origin identification is crucial to ensure the safety and efficacy of toad venom. Integrating a fluorescent sensing array with cross-reactive aptamers provides a promising solution to this issue. We isolated cross-reactive aptamers using a combination of complex target-directed SELEX and convergent selection strategies. During the selection process, we used an immobilized stem-loop library to select aptamers and evaluated the enrichment rate and pool affinity using gel elution assays. After high-throughput sequencing, we selected three cross-reactive aptamers designated N4.8, N2.4, and S1 that exhibit distinct binding profiles for bufadienolides as the biorecognition elements for the fluorescent sensing array. This sensor is capable of distinguishing toad venom from different origins with high accuracy (98.7 %), offering convenient operation, and providing a new method for detecting the origin of toad venom.

24 Mar 2025·Recent Patents on Anti-Cancer Drug Discovery

Resibufogenin and Oxaliplatin Synergistically Inhibit Diffuse Gastric Cancer by Inactivating the FAK/AKT/GSK3β/β-Catenin Signaling Pathway

Article

Author: Li, Zhi-Fei ; Ren, Yongjing ; Li, Tiepeng ; Gong, Ya-Nan ; Chen, Xiao-Bing ; Lv, Hui-Fang ; Hu, Hui-Hui ; Shang, Hai-Li ; Zhang, He ; Wang, Yuhang ; Wang, Jian-Zheng ; Chen, Bei-Bei ; Tu, Shuiping ; Wang, Sai-Qi

Background:Diffuse Gastric Cancer (DGC) is a highly aggressive form of gastric cancer with a poor prognosis. Oxaliplatin (OX) is one of the first-line chemotherapeutic agents for the treatment of gastric cancer. However, some patients with DGC do not benefit from OX therapy. Resibufogenin (RBF), one of the main active components of the Chinese medicine Huachansu, has demonstrated significant anti-cancer effects. Nevertheless, the potential of RBF to enhance the sensitivity of OX treatment in DGC and its underlying mechanisms have not been reported.Objective:The aim of this study is to investigate the sensitizing effect of RBF on OX therapy for DGC, as well as to elucidate the potential targets and mechanisms of action. This exploration is of significant importance for the development of sensitizers that can improve the therapeutic efficacy of OX and for the advancement of patentable innovations in this field.Methods:MTT assay, flow cytometry, Western blotting, and immunofluorescence assays were employed to assess the inhibitory effects of Resibufogenin (RBF) in combination with OX on DGC in vitro. Human DGC cell xenografts were established in a mouse model to evaluate the efficacy and safety of RBF and OX for treating DGC in vivo.Results:It was found that RBF inhibited the proliferation of DGC cells in a time- and dose-dependent manner. When RBF was used in combination with OX, the sensitivity of DGC cells to OX was improved. Significantly, the combination of OX and RBF acts synergistically to induce apoptosis and autophagy while inhibiting migration and invasion of DGC cells in vitro. In vivo, the combination of OX and RBF dramatically inhibited the progression of DGC in the subcutaneous xenograft model without observable toxicity. Mechanistically, RBF significantly inhibited the expression and activation of FAK. OX and RBF synergistically inhibited the phosphorylation of FAK, AKT, and GSK3β to abrogate the entry of β-catenin into the cell nucleus.Conclusion:RBF exhibits a pronounced suppressive effect on FAK, and its combination with OX synergistically blocks the FAK/AKT/GSK3β/β-catenin signaling cascade, thereby inhibiting the growth and metastasis of DGC. This study provides a novel avenue for future research and patent development of FAK inhibitors, with the potential to enhance the therapeutic efficacy of DGC treatment and overcome drug resistance.

01 Jan 2025·Chemical Engineering Journal

Anchoring biomimetic Zn site in metal–organic framework nanozyme to enhance phosphatase-like catalytic activity for discrimination of organophosphorus pesticides

Author: Xie, Chengli ; Qin, Wenling ; Wang, Min ; Gong, Longcheng ; Huang, Yusha ; Xia, Zhining ; Hu, Lianzhe

Herein, a biomimetic approach is developed to improve the phosphatase-like catalytic activity of a metal-organic framework (MOF) nanozyme.Specifically, biomimetic Zn sites, featuring a coordination environment similar to that of natural phosphatase, were covalently anchored into UiO-66-NH₂ nanozyme through a step-by-step modification process.Compared with pristine UiO-66-NH₂, the resultant 66-IS-Zn exhibited a 130-fold increase in K_cat.Mechanism studies suggest that the anchoring of Zn sites can only enhance the catalytic performance of MOFs that possess intrinsic phosphatase-like activity, and the enhancement of catalytic activity strongly relies on the coordination environment of Zn sites, which involves the co-coordination of N and O with Zn.Besides the excellent phosphatase-like activity, 66-IS-Zn also exhibited enhanced intrinsic fluorescence emission and high phosphodiesterase-like catalytic activity.Consequently, 66-IS-Zn was used as the sensing unit to construct a three-channel sensor array for distinguishing organophosphorus pesticides (OPs).This sensor array can successfully distinguish six OPs and allow the quantification of profenofos and phoxim.Moreover, the binary mixtures of OPs and cherry tomato samples were precisely discriminated without any overlapping, indicating the reliability and practicability of the sensor array.

100 Deals associated with Bufogenin

External Link

KEGG	Wiki	ATC	Drug Bank
D01378	-	-	-

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Pancreatic Cancer	Phase 2	-	Northwest University	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis