Sesquiterpenes

Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).

Dihydroartemisinin is an orally active metabolite of rtemisinin (HY-B0094) and antimalarial agent. Dihydroartemisinin induces Autophagy by inhibiting NF-κB activation. Dihydroartemisinin promotes ROS accumulation. Dihydroartemisinin exhibits anticancer activity in esophageal cancer cells. Dihydroartemisinin shows schistosomicidal activity against juvenile and adult worms of Schistosoma japonicum, reduces worm burden, and displays antiparasitic activity. Dihydroartemisinin can be used in research related to multiple myeloma, promyelocytic leukemia, esophageal cancer, and Schistosoma japonicum infection.

Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects.

Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.

Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H⁺-ATPase) and leads to the plasma membrane depolarization in a Ca²⁺-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.

Phytuberin is an Antifungal terpenoid and phytoalexin. Phytuberin exists in potato tubers. Phytuberin exhibits antifungal activity against Phytophthora infestans. Phytuberin shows antifungal activity against both pathogenic and non-pathogenic fungi of potato. Phytuberin can be used in studies related to late blight and potato fungal infections.

Farnesylacetone acts as a transcriptional regulator, RNA synthesis modulator, and male hormone. Farnesylacetone can be extracted from the androgenic glands of the green crab (Carcinus maenas). Farnesylacetone modulates transcriptional processes, inhibits uridine incorporation into all types of RNA and leucine incorporation into ovaries, while stimulating uridine incorporation into tRNA/poly (A)⁺ RNA and leucine incorporation into testes. It suppresses electron transport in mitochondrial Complex I and Complex II. Farnesylacetone inhibits vitellogenesis in crustacean ovaries and stimulates uridine incorporation in crustacean intestines. It functions as an androgen in crustaceans.

1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide is a neuroprotective agent. 1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide reduces the protein expression levels of iNOS and COX-2, blocks the DNA-binding activity of NF-κB, and inhibits nitric oxide production. 1-Hydroxy-4αH-1,10-secoeudesma-5(6),10(14),11(13)-trien-12,8β-olide promotes the polarization of microglia to the M2 phenotype by inducing the production of Arg-1, and alleviates cell damage induced by H₂O₂ and 6-Hydroxydopamine (HY-B1081).

β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma aromatica with an antitumor activity. β-Elemene can induce cell apoptosis.

Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors.

Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria.

Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells.

Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

β-Caryophyllene is a CB2 receptor agonist.

Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM.

Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.

Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects. Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease.

(E)-β-Farnesene (trans-β-Farnesene) is an aphid alarm pheromone, which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene shows good binding score with a value of -30.64 kcal/mol to the CDK2 receptor. (E)-β-Farnesene also exhibits good affinity to odorant-binding protein 3 (OBP3). (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis.

Britannin is an NLRP3 inhibitor with an IC₅₀ of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics.

Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding.