Abstract
The complexity and multi-target feature of natural compounds have made it difficult to elucidate their mechanism of action (MoA), which hindered the development of lead anticancer compounds to some extent. In this study, we applied RNA-Seq and GSEA transcriptome analysis to rapidly and efficiently evaluate the anticancer mechanisms of neobractatin (NBT), a caged prenylxanthone isolated from the Chinese herb Garcinia bracteata. We found that NBT exerted anti-proliferative effect on various cancer cells and caused both G1/S and G2/M arrest in synchronized cancer cells through its effects on the expression of E2F1 and GADD45α. The in vivo animal study further suggested that NBT could reduce tumor burden in HeLa xenograft model with no apparent toxicity. By demonstrating the biological effect of NBT, we provided evidences for further investigations of this novel natural compound with anticancer potential.
Highlights
Active compounds from traditional Chinese medicine (TCM) have long been recognized as valuable sources of anticancer drugs
Cyclindependent kinase 2 (CDK2) levels showed accelerated decrease after NBT treatment, whereas cyclin B1 protein level was stable after the initial drop within the first 2 h of nocodazole release, in contrast to the sustained decrease seen in DMSO treated cells (Figure 2D)
We found that NBT caused arrest in both G1/S and G2/M synchronized cancer cells by regulating the expression of E2F/DP heterodimeric transcription factor 1 (E2F1) and GADD45α respectively
Summary
Active compounds from traditional Chinese medicine (TCM) have long been recognized as valuable sources of anticancer drugs. Camptothecin, for instance, is one of approved anticancer drugs deprived from TCM [1]. The Garcinia species of Chinese herb has been studied for nearly 80 years. Many compounds isolated from these plants, including benzophenones, caged xanthones, and polycyclic polyprenylated acylphloroglucinol (PPAPs), have been shown to have anticancer potential [2]. For example, is a promising anticancer agent that underwent phase II clinical trials in China in patients with non–small-cell lung, colon, and renal cancers [3]. Our previous study showed that neobractatin (NBT), a caged prenylxanthone isolated from Garcinia bracteata C. The detailed mechanism by which NBT exerts its antiproliferative effect on cancer cells remains largely unknown
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