cytotoxic alkaloid

Jineol (NSC-694081) 是一种来自蜈蚣 Scolopendra subspinipes 的喹啉生物碱。Jineol 在体外对人类肿瘤细胞系的生长具有细胞毒活性。

Homoharringtonine (HHT) 属于生物碱类天然产物，可以抑制蛋白质的翻译，具有细胞毒性。Homoharringtonine 作用于肿瘤细胞的核糖体，抑制蛋白质翻译的延伸步骤，从而抑制蛋白质合成，具有抗肿瘤活性。

Jatrorrhizine (neprotin) 是一种从黄连中分离得到的生物碱，具有抗菌、抗氧化、抗疟原虫和神经保护活性。它通过抑制 uptake-2 transporter 的活性减少血清素和去甲肾上腺素的摄取。它是一种有口服活性的乙酰胆碱酯酶制剂。

Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent with cytotoxicity against human cancer cell lines.

Deacetylvinblastine hydrazide, a cytotoxic vinca alkaloid often conjugated with folic acid to produce EC145, a novel folate-receptor targeted agent.

Chaetominine is a type of cytotoxic alkaloid obtained from endophytic Chaetomium sp. IFB-E015.

Racemosidine A is a cytotoxic bisbenzylisoquinoline alkaloid from the roots of Cyclea racemosa.

Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Polyindolinic alkaloids from Psychotria forsteriana. Potent inhibitors of the aggregation of human plateletsPlanta Med.51(4)300-303(1985) 2.Roth, A., Kuballa, B., Bounthanh, C., et al.Cytotoxic activity of polyindoline alkaloids of Psychotria forsteriana (Rubiaceae) (1)Planta Med.6450-453(1986) 3.Amador, T.A., Verotta, L., Nunes, D.S., et al.Involvement of NMDA receptors in the analgesic properties of psychotridinePhytomedicine8(3)202-206(2001)

Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatocellular carcinoma cells when used at a concentration of 4 μM.3 1.Qian-Cutrone, J., Huang, S., Shu, Y.-Z., et al.Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cellsJ. Am. Chem. Soc.124(49)14556-14557(2002) 2.Wulff, J.E., Herzon, S.B., Siegrist, R., et al.Evidence for the rapid conversion of stephacidin B into the electrophilic monomer avrainvillamide in cell cultureJ. Am. Chem. Soc.129(16)4898-4899(2007) 3.Hu, L., Zhang, T., Liu, D., et al.Notoamide-type alkaloid induced apoptosis and autophagy via a P38/JNK signaling pathway in hepatocellular carcinoma cellsRSC Adv.9(34)19855-19868(2019)

(+)-Intermedine, a pyrrolizidine alkaloid (PA), shows remarkable cytotoxic activity against neural progenitor cells (NPCs).

Guattegaumerine, a bisbenzylisoquinoline alkaloid, exhibits antimitotic, cytotoxic, and neuroprotective activities.

Agrochelin, an alkaloid cytotoxic antibiotic, is synthesized via fermentation of a marine Agrobacterium sp. This compound demonstrates cytotoxic activity against tumor cell lines.

Jatrorrhizine chloride (Neprotine chloride) 是从黄连中分离得到的生物碱，具有神经保护、抗菌、抗氧化和抗疟原虫活性。它通过抑制摄取2转运蛋白的活性减少血清素和去甲肾上腺素的摄取。它是具有口服活性的乙酰胆碱酯酶抑制剂。

Xylopine 是一种具有细胞毒活性的阿朴啡生物碱，能诱导癌细胞氧化应激，从而引发 G2 M 细胞周期停滞及细胞凋亡(apoptosis)。

Aristolactam A III (Aristololactam A III) 为一生物碱，具潜在细胞毒性，并可从鱼腥草中分离。

Vinzolidine 是一种半合成的长春花生物碱。它通过破坏微管蛋白 (tubulin) 的聚合来抑制细胞分裂，对肿瘤细胞发挥细胞毒性。Vinzolidine 可用于研究其与其他化疗或生物治疗药物的协同效应，以及癌细胞的耐药性或抗药性，并探索克服这些问题的方法。

4,5-Dimethoxycanthin-6-one 从 Picrasma quassioides BENNET (Simaroubaceae)是一种从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到生物碱。4,5-Dimethoxycanthin-6-one 是一种有效的、非竞争性的 CYP1A2 介导的 phenacetin O-deethylation 抑制剂（IC50 ： 1.7 μM, Ki ： 2.6 μM），对环磷酸腺苷（cAMP）磷酸二酯酶有很强的抑制作用。4,5-Dimethoxycanthin-6-one 具有抗菌活性，对金黄色葡萄球菌及其耐药菌株有抑制作用。4,5-Dimethoxycanthin-6-one 对肿瘤细胞株 U937 和 HepG2 具有细胞毒性。

(–)-Voacangarine, an indole alkaloid isolated from V. africana, exhibits cytotoxicity towards various cell lines including HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 values of 20 µg ml. Additionally, it demonstrates cytostatic effects on wild-type S. cerevisiae and is cytotoxic to Δrad3-e5 and Δrad6-1 mutant strains of S. cerevisiae, which have defects in DNA strand break repair and the mutagenic repair pathway, respectively.

Glycozolidal (Compound 12) 是一种具有抗菌效果的咔唑类生物碱，主要针对牙龈卟啉单胞菌 (P. gingivalis)。它在体外对人牙龈成纤维细胞 (HGFs) 和单核细胞 (U937) 显示出的细胞毒性水平相当，其 IC50 值分别是 120.86 µg mL 和 97.74 µg mL。