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Natural products, a rich source of bioactive chemical compounds, have served humans as a safer drug of choice since times. Eriocalyxin B, an ent-Kaurene diterpenoid, has been extracted from a traditional Chinese herb Isodon eriocalyx. Experimental data support the anticancer and anti-inflammatory activities of EriB. This natural entity exhibits anticancer effects against breast, pancreatic, leukemia, ovarian, lung, bladder, and colorectal cancer. EriB has capability to inhibit the proliferation of cancer cells by prompting apoptosis, arresting cell cycle, and modulating cell signaling pathways. The regulation of signaling pathways in cancerous cells by EriB involves the modulation of various apoptosis-related factors (Bak, Bax, caspases, XIAP, survivin, and Beclin-1), transcriptional factors (nuclear factor kappa B [NF-κB], STAT3, Janus-activated kinase 2, Notch, AP-1, and lκBα), enzymes (cyclooxygenase 2, matrix metalloproteinase 2 [MMP-2], MMP-9, and poly (ADP-ribose) polymerase), cytokines, and protein kinases (mitogen-activated protein kinase and ERK1/2). This review proposes that EriB supplies a novel opportunity for the cure of cancer but supplementary investigations along with preclinical trials are obligatory to effectively figure out its biological and pharmacological applications.

Chemical biology is the scientific discipline that deals with the application of chemical techniques and often small molecules produced through synthetic chemistry, to the manipulation and study of biological systems. Its working framework ranges from simple chemical entities to complex drugs by employing the principles of biological origin. This chapter particularly focuses on the principles and working models of chemical biology to discover new drug leads. Drug discovery is an extensive and multifaceted complex process. Chemical biology uses both natural and synthetic compounds with the best therapeutic potential and verifies them by employing the best possible chemical toolsets. Screening of compounds is done by the use of phenotypic as well as the target-based screening to identify and characterize the potent hits. After the identification of target, it is characterized, and validated by extensive testing. The next step is the validation of hits obtained, and lead compounds are tested in clinical trials before introducing them for commercial application.

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