tumor cell

Paclitaxel (Taxol) 属于天然产物，是一种微管聚合物稳定剂。Paclitaxel 具有抗肿瘤活性；通过诱导有丝分裂停滞、细胞凋亡、细胞自噬等，导致细胞死亡。

Brefeldin A (Cyanein) 属于大环内酯类抗生素，是一种 ATPase 抑制剂 (IC50=0.2 μM)。Brefeldin A 可以诱导肿瘤细胞分化和凋亡，也具有抑制自噬的活性。

Vinorelbine ditartrate (KW-2307) 属于天然生物碱，是一种抗有丝分裂剂。Vinorelbine ditartrate 具有抗肿瘤活性，可以抑制细胞增殖，诱导细胞凋亡。

ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂，也是一种Pre-mRNA Splicing 抑制剂。

Reticulol is an isocoumarin derivative produced by certain species of Streptomyces. Reticulol inhibits cAMP phosphodiesterase (IC50 = 41 µM). Recticulol (M.W. 222.2) exhibits a potent in vitro cytotoxicity against the human lung tumor cell line A427 and the mouse melanoma cell line B16F10.

Quinizarin (1,4-Dihydroxyanthraquinone) 是一种杀菌剂和杀虫剂，可抑制肿瘤细胞生长。

Perillyl alcohol (Isocarveol) 是一种单萜，可在不影响正常细胞的情况下诱导肿瘤细胞凋亡。

Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮，是一种抗癌试剂，具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡，有潜力用于膀胱癌的相关研究。

Erythromycin (E-Mycin) 是由放线菌产生的大环内酯类抗生素。它结合细菌的 50S 核糖体亚基，通过阻断转肽和易位反应来抑制 RNA 依赖性蛋白的合成。

Sophoridine (Dihydro-5-episophocarpine) 是一种从豆科植物槐豆斜生植物的叶子中分离出来的喹喔啉生物碱。它是胰腺癌的候选药物，诱导细胞凋亡。

(E Z)-Polydatin (Polydatin) 是从虎杖的根和根茎中分离得到的一种单晶化合物。它具有抗血小板聚集、心脏保护作用、抗低密度脂蛋白 (LDL) 氧化作用、抗炎和免疫调节功能。

Vitamin D2 (Calciferol) 来源于植物或膳食补充剂，能够用作维生素 D 的补充剂。

Daunorubicin hydrochloride (Rubidomycin hydrochloride) 是一种蒽环类氨基糖苷类化合物，一种拓扑异构酶 II (Topo II) 抑制剂。Daunorubicin hydrochloride 可以抑制 DNA 和 RNA 的合成，具有抗肿瘤活性。

Bestatin (Ubenimex) 是 CD13 (Aminopeptidase N) APN 和 leukotriene A4 hydrolase 抑制剂，可用于癌症研究。

Vitamin K2 (Menatetrenone) 是内源性代谢产物的一种。

Stigmasterol (Stigmasterin) 是一种植物甾醇，具有维持细胞膜结构和生理的主要功能。Stigmasterol 可以降低胆固醇水平，具有抗肿瘤、抗炎、免疫调节作用。

i-Inositol (myo-Inositol) 是一种细胞内磷酸化合物，参与细胞信号传导，可能刺激肿瘤细胞分化。

N4-Benzoyl-2′-deoxycytidine 是天然核苷脱氧胞苷（dC）的合成核苷类似物，是一种DNA 聚合酶的竞争性抑制剂。体外研究表明，它可以抑制病毒、细菌和真核细胞的复制。在动物模型中，它也被证明可以抑制肿瘤细胞的生长。

4,7-DIHYDROXYCOUMARIN 是一种天然存在的香豆素衍生物，存在于多种植物中，包括欧芹和洋甘菊。已经发现它可以抑制几种酶的活性，包括细胞色素P450、环氧合酶和脂氧合酶；也可以与DNA 结合，调节基因表达，并抑制细胞周期进展；还可以诱导肿瘤细胞凋亡并减轻炎症。

(S)-Coriolic acid (13(S)-HODE) 是一种重要的细胞内信号剂，是亚油酸与植物和哺乳动物脂氧合酶反应生成的，在各种生物系统中参与细胞增殖和分化。(S)-Coriolic acid 在 1 μM 左右时，它能抑制肿瘤细胞与血管内皮的粘附，能下调 IRGpIIb IIIa 受体的表达。(S)-Coriolic acid 是15-脂氧合酶 (15-LOX) 代谢产物，常作为内源性配体激活 PPARγ。(S)-Coriolic acid 诱导线粒体功能障碍 和气道上皮损伤。

Terrestrosin D 是从刺蒺藜中提取得到一种的甾体皂苷，可诱导细胞周期阻滞和癌细胞凋亡，具有抗血管生成的活性。

Halofuginone hydrobromid 是Febrifugine 的衍生物，是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂，并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。

2-Methoxyestradiol (2-ME2) 是一种口服生物可利用的雌二醇代谢物，具有抗肿瘤活性。它通过减少内皮细胞增殖和诱导内皮细胞凋亡来抑制血管生成，也可破坏微管的稳定。它可诱导半胱天冬酶活化，导致细胞周期停滞在 G2 期、DNA 断裂和细胞凋亡。

Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

Phytohemagglutinin (PHA-M) 是一种普通豆菜豆的主要种子凝集素，聚集在子叶的薄壁细胞中。它是一种 T 细胞激活剂，能够刺激人单核白细胞，可诱导 ChAT mRNA 表达，增强 ACh 合成。

Sanggenon C (Sanggenone C) 是一种从桑属的根皮中分离得到的黄烷酮 Diels-Alder 加合物化合物。它可抑制NF-κB 活性，抑制 RAW264.7 细胞中诱导型一氧化氮合酶的表达，以及肿瘤坏死因子-α 刺激的细胞粘附和血管细胞粘附分子-1 的表达。 它具有抗氧化和抗炎作用，也有抑制胰脂肪酶作用。

Tanespimycin (KOS 953) 是一种 Hsp90 抑制剂，可选择性抑制 BT474 肿瘤细胞 Hsp90，IC50为 5 nM。它消耗细胞内 STK38 NDR1，并降低 STK38 激酶活性，还能下调stk38基因表达。

(-)-Alkannin (Shikonin) 是从紫朱草中发现的一种天然产物，具有抗癌活性，可抑制细胞周期，诱导细胞凋亡，用作食品着色剂，在 Rho 激酶途径中可改善肝脏炎症。

Crocin (Gardenia Yellow) 是从Crocus sativus 柱头中分离出的主要成分，是一种营养保健品，具有抗炎，抗癌，抗抑郁和抗惊厥等强大的药理作用。

Chlorin E6 (CE6) 是一种第二代光敏剂，在与辐照结合使用时具有抗肿瘤活性。在植入性纤维肉瘤的小鼠模型中，Chlorin E6（2.5-10 毫克 千克，静脉注射，50-200 焦耳 平方厘米的辐照）在不同程度的辐照后会导致肿瘤完全消失。在一项针对支气管源性早期浅表鳞状细胞癌患者的 I 期临床研究中，对包括 Chlorin E6 在内的制剂进行了测试，结果良好（40 毫克 平方米，静脉注射，100 焦耳 平方厘米的激光辐照）。在一项针对早期肺癌患者的二期临床试验中，同样的给药模式使 82.9% 的患者获得了完全应答。Chlorin E6 已被研究为一种纳米技术给药工具。

Picfeltarraenin IB 是一种Picriafel-terraeLour (P.fel-terrae) 中提取的三萜类化合物，是一种乙酰胆碱酯酶抑制剂。它可用于感染，癌症和炎症的研究。

Theasaponin E1，一种可从茶籽分离的茶皂苷，对人肿瘤细胞系K562和HL60展示了抗肿瘤潜能。此外，Theasaponin E1具备醌还原酶(QR)诱导活性，有助于作为抗癌预防药物的研究。

17-Hydroxyneomatrine 是一种从苦参 (Sophora flavescens) 提取的化合物，有效抑制人宫颈癌Hela细胞生长，并展现抗菌、抗过敏、抗肿瘤、抗心律失常、消肿、利尿、免疫调节等多种生物活性。

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0/G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg/kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013). Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0/G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg/kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3 References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013).

Flavokawain C is a melanogenesis inhibitor, it inhibited melanogenesis with IC50 values of 6.9 μM. Flavokawain C has anti-tumor activity, it inhibited cell cycle and promoted apoptosis, associated with endoplasmic reticulum stress and regulation of MAPKs and Akt signaling pathways in HCT 116 human colon carcinoma cells.

Asukamycin is polyketide isolated from the S. nodosus subspecies asukaensis that demonstrates a broad range of antibiotic functions. It has been shown to inhibit growth of various tumor cell lines by activating caspases 8 and 3.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg ml) and Gram-negative bacteria (MICs = 136-200 µg ml), as well as yeasts (MICs = 10-20 µg ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Licochalcone B 是从Glycyrrhiza inflate 根中提取的。它能够抑制淀粉样蛋白 β 自聚集作用 (IC50=2.16 μM) ，分解预先形成的 Aβ42原纤维，并通过螯合金属离子抑制金属诱导的 Aβ42聚集。

Chamaejasmenin B 是一种从 Stellera chamaejasme L 中分离得到的化合物。Chamaejasmenin B 具有抗癌和抗肿瘤活性，可抑制癌细胞迁移和侵袭，抑制肿瘤转移。Chamaejasmenin B 可用于研究如乳腺癌类的癌症。

6-O-Nicotinoylscutebarbatine G shows cytotoxic activities against three human tumor cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 2.1 5.7 μM.

Rauvovertine C shows cytotoxicity in vitro against human tumor cell lines.

Tessaric acid has antifeedant and allelochemical effects. Tessaric acid derivatives induce G/M cell cycle arrest in human solid tumor cell lines.

2α,3α,24-Trihydroxyurs-12-en-28-oic acid, a triterpenoid phytoalexin, shows antifungal activity against the fungus mentioned. It also shows in vitro cytotoxic activity against tumor cell lines including PLC,Hep3B,HepG2,HeLa,SW480,MCF-7 and Bel7402.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

Confluentin has antimicrobial activity against the gram-positive bacteria.Confluentin significantly inhibits compound 48 80-induced histamine release from rat peritoneal mast cells. Confluentin also shows weak cytotoxicity against four human tumor cell li

Tetrac (Tetraiodothyroacetic acid)是L-甲状腺素(T4)的衍生物，是一种甲状腺整合素受体拮抗剂。Tetrac通过阻断EGFR介导的结直肠癌细胞信号传导来诱导抗增殖。Tetrac 可阻断 T4 和 3,5,3'-triiodo-L-thyronine (T3)在细胞表面甲状腺素整合素 αvβ3 受体上的作用。Tetra 具有抗血管生成、抗肿瘤活性和促凋亡活性。

3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg/mL and a 50% inhibitory concentration (IC50) of 72.0microg/mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).

Ophiopogonin R (compound 3)，一种甾体皂苷，源自麦冬的分离纯化。该化合物对包括HepG2、HLE、BEL7402、BEL7403和Hela在内的五种人类肿瘤细胞系均未显示细胞毒性。