l. donovani

2-Benzoxazolinone (2-Hydroxybenzoxazole) 存在于黑麦幼苗中，是一种抗利什曼原虫试剂，抗 L. donovani 的 LC50为40 μg mL。它的衍生物具有抗微生物活性，可针对一系列的革兰氏阳性和阴性细菌。

GSK3186899 是 Cdc2 相关激酶 12 的抑制剂，对 L. donovani 的 EC50 为 1.4 μM。

CHEMBL1276927 (N-(3-(1H-benzo[d]imidazol-2-yl)phenyl)-3-methylbenzamide) 对肺炎衣原体和多诺瓦尼利什曼原虫具有抗菌和抗寄生虫活性。

Amphotericin B (NSC-527017) 是一种多烯类抗真菌剂，对许多真菌物种具有广谱活性。Amphotericin B 不可逆地结合麦角甾醇，破坏细胞膜完整性，从而起到抗真菌活性。

Compound 17k (Antileishmanial agent-30) 对L. donovani显示出卓越的抑制效果，其IC50值为0.2 μM，而CC50值超过100 μM，SI值超过500。

Dihydrocyclosporin A (Dihydrocyclosporin-A) 是 cyclosporin A 的密切相关的共同代谢物。它显着抑制前鞭毛体和细胞内无鞭毛体。

1-Palmitoyl-2-hydroxy-sn-glycero-3-PE is a naturally-occurring lysophospholipid. [1] It inhibits the growth of L. donovani promastigotes (GIC50 = 8 uM). [2]1-Palmitoyl-2-hydroxy-sn-glycero-3-PE serum levels are decreased in a mouse model of alcohol-induced liver injury and in a hepatocellular carcinoma mouse xenograft model. [3] Human serum levels are also decreased immediately and 14 hours following an exercise regimen of 2.5 hours of running for three days. [1]1-Palmitoyl-2-hydroxy-sn-glycero-3-PE has been used as an internal standard for the quantification of saturated lysophosphoethanolamines. [4]

Diacetylcercosporin is a perylenequinone produced by Cercospora and Septoria that has diverse biological activities. It inhibits the growth of P. falciparum strains that are sensitive and resistant to chloroquine and L. donovani parasites (IC50 = 3.1 μM) in vitro. Diacetylcercosporin exhibits cytotoxicity against SK-MEL, KB, BT549, and SK-OV-3 human cancer cell lines (IC50s = 4.8-8.7 μM). It is also a phytotoxin that inhibits the growth of lettuce and bentgrass at a concentration of 1.62 mM

Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin fragmentation, and depolarization of the mitochondrial membrane potential, markers of apoptosis, inL. donovanipromastigotes. 1.López-Martín, C., Pérez-Victoria, J.M., Carvalho, L., et al.Sitamaquine sensitivity in Leishmania species is not mediated by drug accumulation in acidocalcisomesAntimicrob. Agents Chemother.52(11)4030-4036(2008) 2.Carvalho, L.J.M., Luque-Ortega, J.R., López-Martín, C., et al.The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenaseAntimicrob. Agents Chemother.55(9)4204-4210(2011)

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).

LXE408 fumarate 是一种口服有效的，非竞争性的，动素体选择性蛋白酶体 (proteasome) 抑制剂。LXE408 fumarate 抑制 L. donovani 蛋白酶体 (IC50=0.04 μM) 和 L. donovani (EC50=0.04 μM)。LXE408 fumarate 具有较弱的透过血脑屏障能力。LXE408 fumarate 具有用于内脏利什曼病 (VL) 研究的潜力。

Antileishmanial agent-8 (compound 18) 对杜氏利什曼原虫 (L. donovani) 显示出有效的和选择性的杀伤活性(IC50 = 5.64 μM)，并且对 L-6 细胞显示相对较低的细胞毒性 (IC50=73.9 μM)。

Antileishmanial agent-9 (compound 16c) exhibits potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM. In addition, this compound demonstrates relatively low cytotoxicity in L-6 cells, with an IC50 value of 40.1 μM [1].

Antileishmanial agent-7 (compound 23) exhibits strong antileishmanial activity against Leishmania donovani and L-6, with IC50 values of 6.89 and 259 μM, respectively [1].

Antileishmanial agent-6 是一种有效的抗利什曼虫剂。Antileishmanial agent-6 对Leishmania donovani 和 L-6 具有抗利什曼虫活性 (IC50: 0.54 μM) 和细胞毒性 (IC50: 10.2 μM) 作用。

Harpagide 是从Scrophularia cryptophila 中分离出来的一种鸢尾糖苷，具有抗炎和抗寄生虫活性，对T.b. rhodesiense 具有体外锥虫杀虫活性，IC50为 21 μg mL，它对L. donovani 的IC50值为 2.0 μg mL。

3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50 = 13.4 µM). It is also active against L. donovani amastigotes when used at a concentration of 50 µM.

Antileishmanial agent-14，一种磺胺类类似物，展现了对Leishmaniadonovani promastigotes的潜在活性(IC50=4.1 μM)。该化合物同时对L. donovani amastigotes的感染也具有抑制作用(IC50=11.1 μM)。

Antiparasitic agent-18 (compound 3a) 对T. brucei (EC50=0.4 μM)、T. cruzi (EC50=0.21 μM) 和 L. donovani (EC50=0.26 μM) 表现出高度的活性和选择性，证明其为一种有效的抗原虫化合物。

Antileishmanial agent-19 (Compound F27)是一种有效的抗利什曼病试剂，其对L. donovani promastigotes的IC50值为3.39 μM。该化合物能够抑制L. donovani promastigotes中的脯氨酰-tRNA合成酶，并干预宿主PI3K Akt CREB轴，从而抑制IL-10的分泌。此外，Antileishmanial agent-19能诱导L. donovani promastigotes自噬介导的细胞凋亡(apoptosis)过程，并在感染的动物体内显著减少寄生虫负担。

TopoisomeraseI inhibitor 9 (compound 3d) 是针对leishmanial topoisomerase IB的抑制剂，具有针对L. donovani promastigotes的抗利什曼原虫活性，其IC50值为34.81 μM。

TopoisomeraseI inhibitor 10 (compound 13)为一种抗利什曼原虫活性药物，特别针对L. donovani promastigotes的leishmanial topoisomerase IB表现出抑制作用，IC50值为27.91 μM。

1-Palmitoyl-d9-2-hydroxy-sn-glycero-3-PE serves as an internal standard for quantifying 1-palmitoyl-2-hydroxy-sn-glycero-3-PE, a lysophospholipid naturally found to inhibit L. donovani promastigotes growth (GI50= 8 µM). Its levels are reduced in mice after alcohol-induced liver damage, in hepatocellular carcinoma mouse xenografts, and in humans following a rigorous three-day exercise regimen of 2.5 hours running daily and 14 hours post-regimen. This compound is also applied in measuring saturated lysophosphoethanolamines, highlighting its broad utility in biochemical research and disease model studies.