DENV-IN-6

DENV-IN-6是一种高效DENV (I-IV)抑制剂，对DENV (I-IV)复制的EC50值为17.5, 13.20, 6.8 和 11.41 μM。此外，DENV-IN-6对HIV-1IIIB也展示出良好的抗病毒活性，其EC50为0.0181 µM，CC50为64.92 µM。

(E)-Guggulsterone是一种Guggulsterone的异构体。(E)-Guggulsterone是一种FXR拮抗剂，能够降血脂，还能够诱导血红素氧化酶-1表达、阻断DENV NS2B/3B活性，抑制DENV复制。

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

NS2B/NS3-IN-6 (Compound 1a) 是一种变构的 DENV 和 ZIKV NS2B/NS3 蛋白酶抑制剂，对 ZIKV 和 DENV 的 NS2B/NS3 蛋白酶的IC50值分别为 2.23 μM 和 25.2 μM。

DENV-IN-12 (Compound 6)，一种N-甲基胞氨酸硫代(N-methylcytisine thio)衍生物，主要针对DENV-1和DENV-2病毒展示了抑制效果。特别是对DENV-2，该化合物显示出显著的抗病毒活性，其EC50值在各种细胞系中范围为0.002 - 0.005 μM。