Pseudohypericin is a predominant naphthodianthrone from St. John’s wort (Hypericum perforatum L.) phytomedicinal drug. It has been shown to specifically inhibit protein kinase C and dopamine-β-hydroxylase. Also, pseudohypericin induces apoptosis and selectively antagonizes corticotropin-releasing factor in murine models. Inhibition of thioredoxin system by pseudohypericin showed appreciable anticancer properties of this natural compound. Pseudohypericin has antiretroviral activity, it has potential therapeutic value in diseases such as AIDS. Pseudohypericin is implicated in the antidepressant efficacy of St. John's wort.

Asarinin, an urofuran lignan, is the epimer of sesamin. Asarinin is listed in Chinese Pharmacopoeia and used as a quality control (QC) index of crude herbs by the State Food and Drug Administration of China. Asarinin exhibits several biological activities such as decreasing cholesterol levels, exhibiting antihypertensive and antiangiogenic properties and providing immunosuppressive and hepatoprotective activities. Asarinin can also inhibit myocardial injury in metabolic syndrome of rats and decrease the possibility of acute heart transplant rejection. Sesamin was first isolated from sesame seed oil, while asarinin was first isolated from prickly ash bark. Both sesamin and asarinin have been shown to act as insecticidal synergists with pyrethrins.

The triterpene chikusetsusaponin IVa, also called, as Chikusetsu saponin Iva and CALENDULOSIDE F, was isolated from the fruit of Ilex paraguariensis. Using animal model it was shown that this compound could be a promising novel therapeutic agent for diabetic cardiomyopathy, due to its cardio protection; this effect can be reached by activation of the SIRT1/ERK1/2/Homer1a pathway. In addition was demonstrated, that chikusetsusaponin IVa exerts antithrombotic effects, including minor hemorrhagic events, by inhibition of thrombin in a competitive manner.

Eupatorin is a natural flavonoid isolated from the herbs of Eupatorium semiserratum. It has the anti-inflammatory and anti-proliferative properties, which may be utilized in the development of novel anti-inflammatory and anti-tumor treatments. Eupatorin moderately inhibited human cytochrome P450 1A2 (CYP1A2). Eupatorin showed IC50 values of 0.4 ug/mL on T. cruzi epimastigotes and 61.8 ug/mL on trypomastigotes, respectively. It was demonstrated, that eupatorin exerts a vasorelaxative effect on aortic rings through the NO/sGC/cGMP and PGI2 pathways, calcium and potassium channels, muscarinic and beta-adrenergic receptors.

Arctiin, isolated from Forsythia suspensa has been reported to have anti-inflammatory, anti-oxidant, antibacterial, and antiviral effects in vitro. It has been found to act as agonist of the adiponectin receptor 1. Has a potential role in the treatment of obesity. Arctiin has being shown to have anticancer effects in animal research.

Benzoylaconine (Isaconitine; Pikraconitin) is an alkaloid in the Chinese traditional medicine Radix Aconiti Lateralis Preparata (Fuzi). Benzoylaconine is a metabolite of aconitine. Benzoylaconine increased P-gp expression in LS174T and Caco-2 cells, it also increased the P-gp transport activity. Benzoylaconine has being shown to stimulate dynorphin A expression in cultured primary spinal microglia.

Saponarin (SA), a natural flavonoid, is known for its antioxidant and hepatoprotective activities. Saponarin is found in diverse plants, including Tinospora cordifolia, which is used in an anti-diabetic drug, Aloe barbadensis, and barley leaves.Saponarin, isolated from Gypsophila trichotoma Wend., showed in vitro and in vivo hepatoprotective and antioxidant activity against CCl₄-induced liver damage. Saponarin pretreatment also decreased cocaine toxicity both by increasing GSH levels and antioxidant enzyme activities. SA isolated from barley sprouts exerts anti-inflammatory effects in LPS-induced RAW 264.7 macrophages via inhibition of NF-κB, ERK and p38 signaling. Thus, SA may be a promising natural anti-inflammatory agent. Saponarin improves gluconeogenesis and glucose uptake. Saponarin regulates AMPK through induction of intracellular calcium levels. Saponarin has a hypoglycemic effect through the activation of the AMMKb–AMPK–CREB signaling axis in hepatocytes.

Roquefortine C, a cyclopeptide derived from the diketopiperazine cyclo(Trp-dehydroHis), is a secondary metabolite produced by several Penicillium species, especially by Penicillium roqueforti, which is used as starter culture for blue cheese production. Although roquefortine C is frequently detected in the products, it obviously has an insignificant toxicity to humans after ingestion. However, intoxications in dogs and cattle have been reported. Its bacteriostatic activities against Gram-positive bacteria lead to Roquefortine C potential use in antibiotics, but its development as a drug has been stopped due to its neurotoxic effects in mice. Roquefortine C activates P-gp and inhibits P450-3A and other haemoproteins. Roquefortine C can serve as a sensitive biomarker for penitrem A intoxication.