In recent years, a number of natural products isolated from Chinese herbs have been found to inhibit proliferation, induce apoptosis, suppress angiogenesis, retard metastasis and enhance chemotherapy, exhibiting anti-cancer potential both in vitro and in vivo. This article summarizes recent advances in in vitro and in vivo research on the anti-cancer effects and related mechanisms of some promising natural products. These natural products are also reviewed for their therapeutic potentials, including flavonoids (gambogic acid, curcumin, wogonin and silibinin), alkaloids (berberine), terpenes (artemisinin, β-elemene, oridonin, triptolide, and ursolic acid), quinones (shikonin and emodin) and saponins (ginsenoside Rg3), which are isolated from Chinese medicinal herbs. In particular, the discovery of the new use of artemisinin derivatives as excellent anti-cancer drugs is also reviewed.

The anti-cancer activity of terpenoids appears promising and will potentially open more opportunities for cancer therapy. However, current studies are restricted to descriptive findings and lack mechanistic insights and systematic structure-activity relationship (SAR) studies. Future efforts into the systematic identification of the targets of terpenoids are believed to increase chances of gaining breakthrough insights in the field.

Cucurbitacin and its derivatives (cucurbitacins) are a class of highly oxidized tetracyclic triterpenoids. They are widely distributed in the plant kingdom, where they act as heterologous chemical pheromones that protect plants from external biological insults. Their bioactivities first attracted attention in the 1960s. Documented data demonstrate that cucurbitacins possess strong pharmacological properties, such as antitumor, anti-inflammatory, and hepatoprotective effects, etc. Several molecular targets for cucurbitacins have been discovered, such as fibrous-actin, signal transducer and activator of transcription 3, cyclooxygenase-2, etc. The present study summarizes the achievements of the 50 years of research on cucurbitacins. The aim was to systematically analyze their bioactivities with an emphasis on their anticancer effects. Research and development has shed new insight into the beneficial properties of these compounds.

Saponins are glycosides with triterpenoid or spirostane aglycones that demonstrate various pharmacological effects against mammalian diseases. To promote the research and development of anticancer agents from saponins, this review focuses on the anticancer properties of several typical naturally derived triterpenoid saponins (ginsenosides and saikosaponins) and steroid saponins (dioscin, polyphyllin, and timosaponin) isolated from Chinese medicines. These saponins exhibit in vitro and in vivo anticancer effects, such as anti-proliferation, anti-metastasis, anti-angiogenesis, anti-multidrug resistance, and autophagy regulation actions. In addition, related signaling pathways and target proteins involved in the anticancer effects of saponins are also summarized in this work.