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Updated: Apr 8, 2026

Quantitation of Protein Expression and Co-localization Using Multiplexed Immuno-histochemical Staining and Multispectral Imaging
Published on: April 8, 2016
In situ imaging and proteome profiling indicate andrographolide is a highly promiscuous compound
Lin Li1, Hadhi Wijaya2, Sanjay Samanta2
11] Department of Chemistry, National University of Singapore, Singapore 117543 [2] Key Laboratory of Flexible Electronics (KLOFE) &Institute of Advanced Materials (IAM), National Jiangsu Synergistic Innovation Center for Advanced Materials (SICAM), Nanjing Tech University (NanjingTech), Nanjing 211816, P. R. China.
Natural products like andrographolide can be drug leads, but target identification is challenging. New probes reveal andrographolide interacts with many cellular targets in live cells.
Area of Science:
- Natural Product Chemistry
- Chemical Biology
- Drug Discovery
Background:
- Natural products are vital starting points for drug discovery but often lack defined mechanisms of action.
- Current methods for identifying natural product targets in vitro do not accurately reflect cellular environments.
- Andrographolide, a natural product, has potential but requires detailed mechanistic understanding.
Purpose of the Study:
- To develop novel dual-purpose probes for studying natural product interactions in live cells.
- To investigate the in situ proteome-wide targets of the natural product andrographolide.
- To enable real-time bioimaging and target identification of natural products within mammalian cells.
Main Methods:
- Design and synthesis of dual-purpose probes based on the andrographolide scaffold.
- Application of probes for reaction-based, real-time bioimaging in live mammalian cells.
- In situ proteome profiling for comprehensive target identification.
Main Results:
- The developed probes successfully enabled real-time bioimaging and target identification.
- Andrographolide was identified as a promiscuous compound with broad cellular target engagement.
- Numerous previously unknown cellular targets of andrographolide were identified in a cell type-specific manner.
- Covalent interactions were confirmed between andrographolide and its cellular targets.
Conclusions:
- Dual-purpose probes are effective tools for studying natural product mechanisms of action in live cells.
- Andrographolide exhibits extensive and specific target engagement, highlighting its promiscuity.
- Further investigation is warranted to understand the therapeutic implications of andrographolide's broad target interactions.

