Pellitorine is a major amide alkaloid, isolated from Piper longum, Zanthoxylum piperitum or heitzii, Anacyclus pyrethrum, Piper nigrum. Pellitorine can serve as an antagonist of the TRPV1 and may inhibit exovanilloid-induced pain. It exhibits anti-inflammatory activity via activating the Nrf2/HO-1 pathway. Pellitorine shows a good gut permeation and rapidly permeates the BBB once in the blood, indicating a possible role in the treatment of central nervous system diseases. Pellitorine, which was isolated from the roots of Piper nigrum, showed strong cytotoxic activities against HL60 and MCT-7 cancer cell lines. The drug possesses antithrombotic activities and offers bases for development of a novel anticoagulant.

Esculetin (aka Aesculetin) is a derivative of coumarin. It is a naturally occurring lactone which is present in chicory and in many toxic medicinal plants; often found in a glycosidic form or conjugated to caffeic acids. It is used as an ingredient in some sunscreens, but there is evidence that it acts as a photosensitizer for DNA damage. Esculetin has been investigated in a number of cellular and animal cancer models, and for other conditions such as dry eyes.

Brazilin isolated from Caesalpinia sappan has long been known as a natural red pigment. Brazilin is the safe natural compound having the potential to develop as a medicinal compound with application in food, beverage, cosmetics and pharmaceutical industries. It was shown, that brazilin exerts protective effects against renal ischemia-reperfusion injury by inhibiting the NF-κB signaling pathway. In addition, was revealed, that this compound prevented hyperglycemia, renal fibrosis, and inflammation, thus ameliorating renal functional decline in diabetic mice and may be a useful treatment for diabetic nephropathy. Brazilin isolated from H. brasiletto exhibited a moderate antiproliferative activity on the human non-cancer cell line, at the same time demonstrated to have antiproliferative activity against human cancer cell lines, and thus can be a potential source of anticancer agents.

Benzyl-beta-D-glucoside (benzyl beta-D-glucopyranoside, BG) is a benzoyl glucoside, a natural substance that can be found in Pteris ensiformis. Benzyl beta-D-glucopyranoside, the constituent of the fruit of Prunus mume has been shown to relieve tension in experimental menopausal model rats (M-rats) caused by ether stress.

Acetoxycycloheximide is a protein synthesis inhibitor. Acetoxycycloheximide has been previously shown to induce rapid apoptosis mediated by the release of cytochrome c in human leukemia Jurkat cells. It has also been shown to block the TNF-alpha-induced activation of NF-kappaB via ectodomain shedding of TNF receptor 1 (TNF-R1) in human lung carcinoma A549 cells. Acetoxycycloheximide triggers the downregulation of cell surface TNF-R1 via the activation of ERK and p38 MAP kinase, thereby preventing activation of the NF-kappaB signaling pathway by TNF-alpha.

Precocene II is a cyclic propenylic plant metabolite and asarone analog. It shows antijuvenile hormone activity in insects and inhibits trichothecene production in fungi. Precocene II showed strong hepatotoxic, nephrotoxic and hepatocarcinogenic activity. Precocene II exhibited inhibitory activity on the P-388 cancer cell line and the HT-29 cancer cell line. It is a bioactive component of Ageratum houstonianum, responsible for circadian CLOCK-mediated up-regulation of AQP3 in human keratinocytes. It can be used as a potential adjunct to enhance the treatment of various skin diseases by providing adequate hydration in the epidermis.

Oryzalin is a selective preemergence surface-applied herbicide used for control of annual grasses and broadleaf weeds in fruit trees, nut trees, vineyards, established bermudagrass turf and established ornamentals. It inhibits the growth of germinating weed seeds. Oryzalin is an effective inhibitor of human carbonic anhydrases (CAs). Eleven out of 12 catalytically active human CAs were strongly inhibited by oryzalin and exhibited affinities of approximately 2–2000 nM. Oryzalin has been shown to bind specifically to plant tubulin in vitro, inhibited its polymerization, and partly depolymerize taxol-stabilized microtubules. It also inhibits polymerization of leishmania microtubules in vitro.

AM580 is a selective agonist of retinoic acid receptor α (RARα) with IC50 and EC50 values of 8 nM and 0.36 nM, respectively. AM580 has been shown to induce differentiation in leukemic cell lines and inhibit angiogenesis in chick embryos. AM580 exhibited anti-angiogenic activity in vivo. Treatment involving AM580 might have potential therapeutic efficacy in various angiogenesis-dependent disorders, including solid tumors, psoriasis, rheumatoid arthritis and diabetic retinopathy.

Gossypetin (3,5,7,8,3',4'-hexahydroxyflavone) is a flavonoid which has anti-mutagenic, anti-atherosclerotic, antioxidant, as well as cytoprotective and antimicrobial effects. Gossypetin is usually extracted from the flowers of the hibiscus species. Gossypetin has antiproliferative effects on breast cancer (MCF-7) and hepatocellular cancer (HepG2) cell lines. Gossypetin could protect cells against both radiation induced oxidative stress and radiation induced cellular damage via decreasing reactive oxygen species (ROSs).

9-methoxyellipticine is an indole alkaloid from the roots of Ochrosia acuminata. Antitumor properties of 9-methoxyellipticine were demonstrated. 9-Methoxyellipticine possesses a relatively broad spectrum of antitumor activity, 10 of 17 mouse neoplasms tested having responded. Both intraperitoneal and oral activity have been noted. Significant activity was seen against both the ascites and solid forms of the Walker rat carcinosarcoma 256. 9-methoxyellipticine binds DNA through a single step mechanism, can be considered as a pure intercalator.