Apocynaceae

Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) sulfate is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a K_i of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine sulfate inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine sulfate upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine sulfate is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas.

Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC₅₀ of 8.9 μM.

Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC₅₀ of 1.25 nM.

Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.

Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a K_i of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas.

Isoconessimine is a steroidal alkaloid that can be found in the seeds of Holarrhena antidysenterica, and the IC₅₀ value of its acetylcholinesterase inhibitory activity is > 300 μM.

Tylogenin is a Na⁺/K⁺ ATPase inhibitor with an IC₅₀ of 93.3 μM against rabbit-derived targets. Tylogenin inhibits antigen-induced mediator release from rabbit basophils and IgE-dependent histamine release from human leukocytes. Tylogenin exhibits antiallergic activity. Tylogenin can be used in research related to allergic diseases.

Auricledleaf swallowwort root extract is an extract of Cynanchum otophyllum Schneid, which can be used to study Alzheimer's disease.

Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na⁺ channels. The IC₅₀ value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.

Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

Quercetin 3-O-β-D-glucofuranoside is an effective antioxidant and an eosinophilic inflammation suppressor.

Proscillaridin A is a potent poison of topoisomerase I/II activity with IC₅₀ values of 30 nM and 100 nM, respectively.

9-Hydroxyoctadecanoic acid (9-HSA) is an HDAC1 inhibitor that inhibits ∼66.4% HDAC1 enzymatic activity at 5 μM. 9-Hydroxyoctadecanoic acid shows anticancer activity.

Baimaside (Quercetin 3-O-sophoroside) is a flavonoid cholinergic function modulator that binds to SARS-CoV-2-related targets. Baimaside regulates the expression of cholinergic system-related proteins and acetylcholine levels, improves scopolamine-induced learning and memory impairment, protects hippocampal neurons, inhibits pollen protein fluorescence, and protects pollen DNA. Its biosynthesis is regulated by multiple enzymes. Baimaside is completely absorbed in rats, undergoes phase Ⅱ metabolism and gut microbiota decomposition, and inhibits the invasion and proliferation of SARS-CoV-2 and its variants, making it suitable for research related to Alzheimer's disease and COVID-19.

Vindesine sulfate is a potent tubulin inhibitor with an K_i of 0.110 μM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo.

Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia.

Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

trans-Zeatinriboside is a zeatin-type cytokinin and plant growth regulator. trans-Zeatinriboside is produced by the terrestrial filamentous cyanobacterium Nostoc sp. HK-01 and Agrobacterium tumefaciens (including Ti plasmid-dependent and Ti plasmid-independent strains). trans-Zeatinriboside is detectable as a cytokinin component in growing crown galls, and accumulates in large amounts in CHRK1-silenced transgenic tobacco accompanied by pleiotropic developmental abnormalities. trans-Zeatinriboside can be used in studies related to crown galls.

Oleandrin (PBI-05204) inhibits the Na⁺, K⁺-ATPase activity with an IC₅₀ of 620 nM.

Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.