Abstract

Natural products (NPs) are an important source for new drug discovery over the past decades, which have been demonstrated to be effectively used in cancer prevention, treatment, and adjuvant therapy. Many methods, such as the genomic and metabolomic approaches, immunochemistry, mass spectrometry, and chromatography, have been used to study the effects of NPs on cancer as well as themselves. Because of the advantages in specificity, sensitivity, high throughput, and cost-effectiveness, optical imaging (OI) approaches, including optical microscopic imaging and macroscopic imaging techniques have also been applied in the studies of NPs. Optical microscopic imaging can observe NPs as cancer therapeutics at the cellular level and analyze its cytotoxicity and mechanism of action. Optical macroscopic imaging observes the distribution, metabolic pathway, and target lesions of NPs in vivo, and evaluates NPs as cancer therapeutics at the whole-body level in small living animals. This review focuses on the recent advances in NPs as cancer therapeutics, with particular emphasis on the powerful use of optical microscopic and macroscopic imaging techniques, including the studies of observation of ingestion by cells, anticancer mechanism, and in vivo delivery. Finally, we prospect the wider application and future potential of OI approaches in NPs as cancer therapeutics.

Highlights

  • As an important tool to break through the bottleneck of drug development, natural products (NPs) and their derivatives have contributed about 50% of new drugs over the past 30 years (Camp et al, 2012; Newman and Cragg 2016), including anti-cancer, anti-inflammatory, and antibiotics (Shukla and Singh 2011)

  • Chatziathanasiadou et al synthesized quercetinalanine bioconjugation based on quercetin which is cytotoxic to cancer cells, and detected its cellular internalization to observe the cytotoxicity using confocal microscopy

  • In order to improve the delivery capacity of gambogic acid (GA), a Natural products (NPs) having anticancer ability, Wenzhe Huang et al prepared a nano-formulation of GA using a series of telodendrimers and applied it to living nude mice implanted with HT-29 cells

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Summary

INTRODUCTION

As an important tool to break through the bottleneck of drug development, natural products (NPs) and their derivatives have contributed about 50% of new drugs over the past 30 years (Camp et al, 2012; Newman and Cragg 2016), including anti-cancer, anti-inflammatory, and antibiotics (Shukla and Singh 2011). Haibin Shi et al developed a cell-permeable kinase probe derived from staurosporine for proteomic analysis of potential cellular targets in HepG2 cells (Shi et al, 2011) These methods mentioned above require some special tools such as chromatography, mass spectrometry, and Western blotting (Wu and Liang, 2010; Yang et al, 2015; da Silva et al, 2018; Wu et al, 2018). The OI technologies include optical microscopic imaging technology represented by fluorescence microscopy and super-resolution microscopy, and optical macroscopic imaging technology with an example of near infrared (NIR) fluorescence imaging technique having a good targeting ability and detecting depth in the in vivo imaging of NPs. we prospect the wider application and future potential of OI approaches in NPs as cancer therapeutics

APPLICATION OF OPTICAL MICROSCOPIC IMAGING FOR NATURAL PRODUCTS
Observation of Natural Products Ingested by Cancer Cells
Investigation of Anticancer Mechanism of Natural Products
Verification of Apoptosis
APPLICATION OF OPTICAL MACROSCOPIC IMAGING FOR NATURAL PRODUCTS
Monitoring the Delivery of Natural Products In Vivo
Combining With Natural Products to Assist Cancer Treatment
CONCLUSION AND PERSPECTIVE
AUTHOR CONTRIBUTIONS
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