Mithun Singh RajputNilesh Prakash NirmalSrushti Jagdish NirmalChalat SantivarangknaRamanbhai Patel College of PharmacyMahidol UniversityMET’s Institute of Pharmacy2022-08-042022-08-042021-01-01South African Journal of Botany. (2021)025462992-s2.0-85119914016https://repository.li.mahidol.ac.th/handle/20.500.14594/75762Caesalpinia sappan Linn. or Sappanwood is a redwood, full-fledged in numerous parts of Southeast Asia and well known for its red pigments, dye, food additive, and several medicinal properties. Many active chemical compounds in sappanwood extract have been identified and evaluated for medicinal properties such as anticancer, antimicrobial, anti-inflammatory, anti-arthritic, neuroprotective effect, also protective effect on organs like heart, kidney, liver, and intestine. Additional attempts are underway to isolate novel phytochemicals and to evaluate their possible bioactivities. The present review reported the newly isolated and identified phytochemicals from C. sappan including diterpenes (cassane derivatives), homoisoflavones (sappanol and protosappanins derivatives) and phenolics (epicaesalpin J and dracaenone derivatives). Pharmacokinetics of major bioactive compounds in C. sappan has been revisited. The recently investigated biological activities (pharmacodynamics) of various bioactive compounds from C. sappan has been a brief discussion. Additionally, the protective effect of various bioactive compounds on different organs including the kidney, liver, heart, and gastrointestinal tract have been scrutinized. Moreover, the toxicological effect of the significant active molecules in C. sappan has been outlined. Finally, the challenges and hurdles for herbal medicine development have been discussed.Mahidol UniversityAgricultural and Biological SciencesReviewSCOPUS10.1016/j.sajb.2021.11.021