Anti-HSV activity of camptothecin analogues

Abstract

In order to explore the range of biological activities of the camptothecin compound class, the in vitro antiviral efficacies of series I-IV of representative members from camptothecin analogues on herpes simplex virus type 2 (HSV-2) were evaluated on vero cells. Several compounds exhibited similar or better antiviral activity against HSV-2 in vitro than acyclovir. Among them, compound 6 showed the highest anti-HSV-2 activity, with IC(50) values of 1.3 microg mL(-1) and SI values of 27.04, respectively. On the basis of preliminary biological testing results, it is suggested that the intact E lactone ring and 20-hydroxy group should be not a prerequisite for camptothecin-like antiviral activity, and CPT substitution at the C-20 hydroxy group may be optimal for synthesising more potent antiviral compounds, suggesting that CPT has the potential to be a lead structure for semi-synthetic antiviral agents.

Perspectives on Biologically Active Camptothecin Derivatives

“…In ancient China, the crude extract of Camptotheca acuminate containing CPT has been used traditionally to control insect pests for centuries, and it was reported to be a potent chemosterilant against the housefly and cabbage caterpillar. 103,104 It also exhibited significant inhibitory activities against several agricultural pests such as Empoasca vitis, Mythimna separate Walker, Brevicoryne brassicae, Nilaparvata lugens, and Chilo suppressalis, supporting its potential use as a field pesticide. [105][106][107][108] Additionally, a recent study showed that CPT could cause visible changes in the midguts from the lepidopteran pests Trichoplusia ni and Spodoptera exigua, such as losing the single layer of epithelial cells and disrupting the peritrophicmembrane.…”

“…In ancient China, the crude extract of Camptotheca acuminate containing CPT has been used traditionally to control insect pests for centuries, and it was reported to be a potent chemosterilant against the housefly and cabbage caterpillar . It also exhibited significant inhibitory activities against several agricultural pests such as Empoasca vitis, Mythimna separate Walker, Brevicoryne brassicae , Nilaparvata lugens , and Chilo suppressalis , supporting its potential use as a field pesticide .…”

Peptide inhibitors against herpes simplex virus infections

“…Although these agents have proven to be efficacious in the treatment of HSV infections, the risk of adverse effects and the frequent development of drug‐resistant strains of HSV make it imperative to discover new antiviral agents with lower toxicity, more convenient regimens, and less susceptible to resistance emergence. Several viral and cellular products have been investigated in recent years to find different targets with different mechanisms of action, and literature has been filled by scientific reports of the in vitro anti‐herpetic activity of a wide variety of natural products and synthetic compounds .…”

New imidazolidineiminothione derivatives: Synthesis, spectral characterization and evaluation of antitumor, antiviral, antibacterial and antifungal activities

“…Herpes simplex viruses (HSV-1) infection may result several diseases such as genital herpes, labial herpes and chronic mucocutaneous ulceration [12,13]. HSV infections are usually treated with nucleoside analogues such as acyclovir [14]. However, the efficacy of these drugs is limited by the recent increase in the resistance of virus and recurrence of latent virus [15].…”