One of the main forms of cancer treatment is chemotherapy. Chemotherapy failure is a common occurrence, primarily because of dose-limiting toxicity linked to medication resistance. Effective treatment resistance management is essential for chemotherapy to be successful. Numerous reports in Chinese literature suggest that organic materials can overcome medication resistance in cancer cells, and these findings should be shared with scientific and industrial groups. The reports were condensed into four categories by us: 1. research on cell line models in-vitro; 2. serum pharmacokinetics; 3. in-vivo research employing animal models; and 4. clinical research. For the first time, antidrug resistance activity was found in 14 single compounds. Drugs have been proven to overcome drug resistance in-vitro in a dose-dependent manner by blocking drug transporters, cell detoxification ability, or cell apoptosis sensitivity, even at nontoxic and subtoxic concentrations. Research conducted in-vivo revealed that herbal extracts, single components, and formulations all exhibited strong antidrug resistance properties. A significant number of individual chemicals, herbal extracts, and combinations have been applied in clinical settings to treat a range of illnesses, including cancer. Comprehensive information on the utilization of natural compounds in China to combat drug resistance in cancer cells is provided by this review, which could help in the creation of organic substances for the therapeutic treatment of drug resistance in cancer patients.