drug-resistant

Niranthin 是一种木脂素，具有广泛的药理活性。它是L. donovaniIB 拓扑异构酶的非竞争性抑制剂，可用于研究耐药利什曼病的治疗。

Tectol 是从Lippia sidoides 中分离的，对人白血病细胞株 HL60 和 CEM 具有显著的抑制作用。它是法尼基转移酶抑制剂，在人和布氏锥虫的IC50分别为 2.09 和 1.73 μM。它具有抗疟原虫活性，是一种中等活性的生长抑制剂，IC50 为 3.44±0.20μM。

D-Cycloserine (RO-1-9213) 是一种抗生素，靶向细菌细胞壁肽聚糖生物合成酶。它是一种NMDA 部分激动剂，可以改善认知功能，可研究耐多药结核病。

Fosfomycin sodium 是一种能透过血脑屏障的广谱抗生素，不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性，包括耐多药、广泛耐药和耐全药的细菌。

2-Aminoimidazole（2-氨基咪唑）是一种有效的抗菌剂，通过破坏质子动力和阻断电子传递链，有效地靶向耐药性结核分枝杆菌，通过减少β-内酰胺酶的分泌和增加细胞膜的通透性来增强β-内酰胺类抗生素对抗结核分枝杆菌的作用，激活耐药细菌和改善治疗效果。

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).

Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a concentration of 100 μM.3 Dietary administration of collinin (0.05% w/w) reduces the number of mice with tumors and the number of tumors per mouse in a mouse model of colitis-related carcinogenesis.4 |1. Kim, S., Seo, H., Al Mahmud, H., et al. In vitro activity of collinin isolated from the leaves of Zanthoxylum schinifolium against multidrug- and extensively drug-resistant Mycobacterium tuberculosis. Phytomedicine 46, 104-110 (2018).|2. Nguyen, P.-H., Zhao, B.T., Kim, O., et al. Anti-inflammatory terpenylated coumarins from the leaves of Zanthoxylum schinifolium with α-glucosidase inhibitory activity. J. Nat. Med. 70(2), 276-281 (2016).|3. I.S., C., Lin, Y.C., Tsai, I.L., et al. Coumarins and anti-platelet aggregation constituents from Zanthoxylum schinifolium. Phytochemistry 39(5), 1091-1097 (1995).|4. Kohno, H., Suzuki, R., Curini, M., et al. Dietary administration with prenyloxycoumarins, auraptene and collinin, inhibits colitis-related colon carcinogenesis in mice. Int. J. Cancer 118(12), 2936-2942 (2006).

Tellimagrandin II是一种具有口服活性的天然产物，对耐药的Staphylococcus aureus具有抑制活性，还能抑制AchE和改善记忆障碍。

9-dihydro-13-acetylbaccatin III (9-DHAB III) 是一种制备紫杉醇类似物的中间体。

Deoxyshikonin (Arnebin 7) 是从紫草中分离的天然产物，具有抗肿瘤活性，在体外具有促血管生成作用。它和没食子酸十二烷基酯在体内外均与青霉素有显着的协同抗菌活性。

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

Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分，有抗炎和抗癌作用。

Staphyloferrin A，一种铁载体蛋白，与抗生素结合对抗抗药性细菌性皮肤病进行研究。

Oroxylin A (Standard) 是 Oroxylin A 的标准品。适用于定量分析、质量控制及生化实验等相关研究。Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

Demethoxycurcumin (Standard) 是 Demethoxycurcumin 的标准品。适用于定量分析、质量控制及生化实验等相关研究。Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分，有抗炎和抗癌作用。

D-Cycloserine (Standard) 是一种可用于分析的标准物质，通常用作 D-Cycloserine 的研究和分析中参考的标准样品。D-Cycloserine (RO-1-9213) 是一种抗生素，靶向细菌细胞壁肽聚糖生物合成酶。它是一种NMDA 部分激动剂，可以改善认知功能，可研究耐多药结核病。

Ardisiacrispin B是一种具有抗癌活性的天然三萜皂素，能够诱导凋亡和铁死亡，对A549，HL-60，MDA-MB-231等细胞具有抑制活性。

Graveobioside A是一种天然的花青素苷，可用于生物化学实验和药物合成研究。

Imperialine 3-β-D-glucoside (Sipeimine-3-beta-D-glucoside) 是 Imperialine 的糖苷。它对多重耐药肿瘤细胞表现出抗肿瘤特性。

Wulignan A1 exhibits activity against leukemia P-388 in vitro; it also may have anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities.

Jatrophane 5 demonstrates the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-TxR).

2,5,7,8,9,14-Hexaacetoxy-3-benzoyloxy-15-hydroxyjatropha-6(17),11E-diene (Jatrophane 2 ) exhibits significant antifeedant activity against a generalist plant-feeding insect, the cotton bollworm (Helicoverpa armigera). Jatrophane 2 also demonstrates the mo

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).

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。