Licochalcone A (LicA) is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch and has a wide spectrum of pharmacological activities such as anti-oxidant, anti-bacterial, anti-viral, and anti-cancer. However, its pharmacological mechanism is not well defined. The anti-Inflammatory effects of LicA on IL-1β-Stimulated human osteoarthritis chondrocytes was reached by activating Nrf2 signaling pathway. LicA showed anti-proliferative and apoptotic effects in breast cancer cells through regulating Sp1 and apoptosis-related proteins in a dose- and a time-dependent manner. In addition, the chemotherapeutic potential of LicA for treatment of human cervical cancer was achieved by inhibition of PI3K/Akt/mTOR signaling.

MKC-1 is an orally available cell cycle inhibitor with downstream targets that include tubulin and the importin-β family. MKC-1 has shown broad antitumor activity in preclinical models. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. MKC-1 had been in phase II clinical trials for the treatment of ovarian cancer, endometrial cancer, pancreatic cancer and breast cancer. This compound was originally discovered by Roche, then licensed to EntreMed (now CASI Pharmaceuticals) the exclusive worldwide rights to develop and commercialize. However, no recent development has been reported.

Arenobufagin, a representative natural bufadienolide compound, is the major active component extracted from toad venom. Arenobufagin is a part of Chinese medicine Chan'su. It possesses significant antineoplastic activity in vitro. Antineoplastic activity of arenobufagin was tested using cell lines from different cancers: breast cancer, hepatocellular carcinoma, prostatic cancer, etc. Arenobufagin acts by intercalating with DNA and disrupting the cell cycle. Also it was shown to inhibit PI3K/Akt/mTOR pathway (in hepatocellular carcinoma cells) and inhibit Na, K-ATPase.

Hypaphorine is the alkaloid isolated from the seeds of Brazilian medicinal plant Erythrina spp. This compound was investigated for sleep-promoting effects in mice, and the results showed that it significantly increased non-rapid eye movement (NREM) sleep time during the first hour after its administration. Hypaphorine prevented the differentiation of 3T3-L1 preadipocytes into adipocytes by down-regulating hormone-stimulated protein expression of peroxisome proliferator activated receptor γ (PPARγ) and CCAAT/enhancer binding protein (C/EBPα), and their downstream targets, sterol regulatory element binding protein 1 c (SREBP1c) and fatty acid synthase (FAS). Hypaphorine may exert anti-inflammatory actions through the regulation of TLR4 and PPAR-γ dependent on PI3K/Akt/mTOR signal pathways. It is considered as a therapeutic agent that can potentially relieve or ameliorate endothelial inflammation-associated diseases. Hypaphorine was also a key component of Vaccaria segetalis. Vaccaria hypaphorine might be considered as a potential therapeutic agent for treating osteoclast-based bone loss.

Ophiopogonin B is a glycosid (saponin) isolated from the butanol-soluble fraction of the fresh subterranean part of Ophiopogon japonicus, which is often used in Chinese traditional medicine to treat pulmonary disease and cancer. Ophiopogonin B was tested against non-small cell lung carcinoma, cervical cancer and gastric cancer cell lines, demonstrating inhibition of PI3K-Akt and mTOR-Akt signaling.

Hypaphorine is the alkaloid isolated from the seeds of Brazilian medicinal plant Erythrina spp. This compound was investigated for sleep-promoting effects in mice, and the results showed that it significantly increased non-rapid eye movement (NREM) sleep time during the first hour after its administration. Hypaphorine prevented the differentiation of 3T3-L1 preadipocytes into adipocytes by down-regulating hormone-stimulated protein expression of peroxisome proliferator activated receptor γ (PPARγ) and CCAAT/enhancer binding protein (C/EBPα), and their downstream targets, sterol regulatory element binding protein 1 c (SREBP1c) and fatty acid synthase (FAS). Hypaphorine may exert anti-inflammatory actions through the regulation of TLR4 and PPAR-γ dependent on PI3K/Akt/mTOR signal pathways. It is considered as a therapeutic agent that can potentially relieve or ameliorate endothelial inflammation-associated diseases. Hypaphorine was also a key component of Vaccaria segetalis. Vaccaria hypaphorine might be considered as a potential therapeutic agent for treating osteoclast-based bone loss.