Celastrol is a pentacyclic triterpenoid that is 24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid bearing an oxo substituent at position 2, a hydroxy substituent at position 3 and two methyl groups at positions 9 and 13. An antioxidant and anti-inflammatory agent. Potently inhibits lipid peroxidation in mitochondria and inhibits TNF-alpha-induced NFB activation. Also shown to inhibit topoisomerase II activity in vitro (IC50 = 7.41 M). Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol is also a novel HSP90 inhibitor, it has anti-proliferative, anti-inflammatory, anti-tumor , antiangiogenesis, and antioxidant activities. Celastrol inhibits Plasmodium falciparum enoyl-acyl carrier protein reductase and inhibits VEGF receptors expression.

Jatrorrhizine has neuroprotective, antioxidative, anti-inflammatory, antihypercholesterolemic, and anti-hyperglycemia effects.Jatrorrhizine is expected to be developed as a new gastric prokinetic drug, it is metabolized by human CYP1A2 and multiple UGT1A isoforms. It has inhibitory activities against the expression of inducible NO syntase (iNOS) and cyclooxygenase-2 (COX-2), and can improve the utilization and excretion of cholesterol by up-regulating the mRNA and protein expression of LDLR and CYP7A1.

Atherosperminine shows cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Atherosperminine shows strong anti-plasmodial activity against Plasmodium falciparum, with the IC50 value of 5.80 uM, it also shows antioxidant activity in a DPPH assay with the IC50 value of 54.53 ug/mL. Atherosperminine exerts a non-specific relaxant effect on the trachealis, its major mechanism of action appears to be inhibition of cAMP phosphodiesterase.

Daphnetin is a dihydroxycoumarin that is being used in China for the treatment of coagulation disorders, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit antimalarial, anti-rheumatoid arthritis, anti-proliferative, anti-inflammatory and anti-oxidant activities. it is also a chelator and an antioxidant. Daphnetin can enhance immunological functions of B lymphocytes, the expression of IL-12 in B lymphocytes can be up-regulated by daphnetin through natural immunity approach.

Lapachol is a hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone substituted by hydroxy and 3-methylbut-2-en-1-yl groups at positions 2 and 3, respectively. It is a natural compound that exhibits antibacterial and anticancer properties, first isolated in 1882 from the bark of Tabebuia avellanedae. It has a role as an antibacterial agent, an antineoplastic agent, an anti-inflammatory agent and a plant metabolite. It is a hydroxy-1,4-naphthoquinone and an olefinic compound. Lapachol shows both antimicrobial, trypanocidal and antiviral activities, it also shows antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. Probiotics are capable of converting Lapachol into the most effective cytotoxic compound against a breast cancer cell line.

Strictosamide possesses antibacterial and antiviral activities, it also may have important effects on inflammation and inflammatory pain. Strictosamide is slightly toxic to Charles River mouse (LD(50)=723.17 mg/kg), producing CNS depression and kidney toxicity. Strictosamide has nonsignificant in vitro and in vivo effect on kidney Na(+),K(+)-ATPase activity but produced an in vivo increase of Na(+),K(+)-ATPase activity of brain.

Ailanthone is a triterpenoid. Ailanthone has anti-inflammatory, anti-HIV, anti-malarial, anti-allergic, antiulcer and antimicrobial activities; it also has potent antineoplastic activity against hepatocellular carcinoma (HCC), it can inhibit huh7 cancer cell growth via cell cycle arrest and apoptosis in vitro and in vivo. Ailanthone has significant pre-emergence herbicide activity , is directly correlated to Ailanthone concentration. Ailantone (Δ 13 Dehydrochaparrinone) is an effective androgen receptor (AR) inhibitor, with IC50 values of 69 nM for intact androgen receptors and 309 nM for sustained active splicing variants.

Beta-boswellic acid and its derivatives (the major constituents of Boswellin) have anti-carcinogenic, anti-tumor, and anti-hyperlipidemic activities. Beta-boswellic acid can significantly enhance neurite outgrowth, branching, and tubulin polymerization dynamics.

Artemether is an artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria. It has a role as an antimalarial. It is an organic peroxide, a sesquiterpenoid, a cyclic acetal, an artemisinin derivative and a semisynthetic derivative. Artemether is a novel sonosensitizer,which has neurotoxicity, anti-schistosomiasis, anticancer and antitumor activities. It is an antimalarial for the treatment of resistant strains of falciparum malaria. Artemiser is an anti malarial compound that can act on drug-resistant strains of malignant malaria.