Cucurbitacin B acts a potential insect growth regulator by antagonizing 20‐hydroxyecdysone activity

Zou, Chuanshan; Liu, Guifen; Liu, Suning; Liu, Shumin; Song, Qisheng; Wang, Jian; Feng, Qili; Yan, Su; Li, Sheng

doi:10.1002/ps.4817

Cited by 22 publications

(22 citation statements)

References 37 publications

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“…Cucurbitacins have been gaining attention of scientists for their potential anti-cancer effects for decades (Lee et al, 2010; Alghasham, 2013; Cai et al, 2015), which process a broad range of pharmacological activities, including anti-inflammatory, antipyretic, and anti-cancer activities (Kaushik et al, 2015). In particular, the anti-cancer activities of cucurbitacins through antiproliferation (Mao et al, 2019; Saeed et al, 2019), inhibition of migration and invasion (Touihri-Barakati et al, 2017; Zou et al, 2018), induction of cell apoptosis (Ding et al, 2017; He et al, 2017; Liu et al, 2018; Mao et al, 2019), autophagy (Ni et al, 2018; Lin et al, 2019), and cell cycle arrest promotion are of great interest (Liu et al, 2018). For instance, cucurbitacins B, D, E, and I are the most wildly studied variants and exhibit general in vitro and in vivo anti-cancer effects.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Antitumor Activity of Cucurbitacin C, a Novel Natural Product From Cucumber

Wang

Lin

et al. 2019

Front. Pharmacol.

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Cucurbitacin C (CuC), a novel analogue of triterpenoids cucurbitacins, confers a bitter taste in cucumber. Genes and signaling pathways responsive for biosynthesis of CuC have been identified in the recent years. In the present study, we explored the anti-cancer effects of CuC against human cancers in vitro and in vivo. CuC inhibited proliferation and clonogenic potential of multiple cancer cells in a dose-dependent manner. Low-dose CuC treatment induced cell cycle arrest at G1 or G2/M stage in different cancer lines, whereas high-dose treatment of CuC caused apoptosis in cancer cells. PI3K-Akt signaling pathway was found to be one of the major pathways involved in CuC-induced cell growth arrest and apoptosis by RNA-Seq and Western blotting. Mechanistic dissection further confirmed that CuC effectively inhibited the Akt signaling by inhibition of Akt phosphorylation at Ser473. In vivo CuC treatment (0.1 mg/kg body weight) effectively inhibited growth of cancer cell-derived xenograft tumors in athymic nude mice and caused significant apoptosis. Our findings for the first time demonstrated the potential therapeutic significance of CuC against human cancers.

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Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Antitumor Activity of Cucurbitacin C, a Novel Natural Product From Cucumber

Wang

Lin

et al. 2019

Front. Pharmacol.

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“…Currently, four insecticides that target the NR gene EcR have been commercialized . However, discovering new eco‐friendly insecticides is urgent because of the rapid development of insecticide resistance and the well‐known negative effects of insecticides to the environment, Targeting insect NRs could block insect metamorphosis effectively and may provide a good direction for biopesticide exploitation . Thus, in the present study, we firstly identified 20 NR genes in Bemisia tabaci Q. Secondly, we investigated their stage‐specific and tissue‐specific expression profiles.…”

Section: Introductionmentioning

confidence: 99%

Genome‐wide identification and analysis of nuclear receptors genes for lethal screening against Bemisia tabaci Q

Liu

Liang

et al. 2020

Pest Management Science

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BACKGROUND: Nuclear receptors (NRs) play an essential role in diverse biological processes, such as insect metamorphosis. Here, transcriptome analysis and functional studies were used to determine whether NRs are involved in metamorphosis of whitefly Bemisia tabaci Q, a serious pest to crops, and to find some potential insecticide targets.RESULTS: Twenty NRs were identified in the Bemisia tabaci Q genome and categorized into the NR0-NR6 subfamilies. The phylogenetic tree of NRs from Bemisia tabaci Q and other representative species was constructed, which provided evolutionary insight into their genetic distances. The results of spatiotemporal gene expression indicated that the majority of NR gene expression was higher in the head than the abdomen and higher in eggs than adults. Further functional analysis using RNA interference (RNAi) showed that NR genes play an important role in Bemisia tabaci Q pupation and eclosion. With respect to high mortality and effects on growth, this was reflected in the unable to become pupa when the third-stage nymph treated with double-stranded RNA (dsRNA) and the developmental time delay (4-7 days) when pupae were treated with dsRNA for the 12 NR genes during molting compared with the development time in the control.CONCLUSION: This study provides insight into NR functions during the metamorphosis stages of Bemisia tabaci Q. Several candidate genes could be potential insecticide targets for whitefly pest control due to their important roles in insect development.

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“…Currently, significant amounts of research are being devoted to developing new types of insecticides that are harmless to the environment. Targeting insect steroid hormones and their nuclear receptors could block insect metamorphosis effectively and provide useful information for biopesticide studies (Zou et al ., ), and are attractive targets for developing new insecticides.…”

Section: Introductionmentioning

confidence: 99%

Nuclear receptor hormone receptor 39 is required for locust moulting by regulating the chitinase and carboxypeptidase genes

Zhao

Qin

Zhang

et al. 2019

Insect Molecular Biology

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The nuclear receptor‐mediated 20‐hydroxyecdysone (20E) signalling pathway plays crucial roles in insects by initiating and regulating moulting and metamorphosis. In the present study, we identified and characterized a cDNA encoding a putative nuclear receptor protein (Locusta migratoria hormone receptor 39, LmHR39) based on L. migratoria transcriptomics data. Reverse‐transcription quantitative PCR (RT‐qPCR) revealed that LmHR39 shows low‐level expression in the early days of fifth‐instar nymphs, and peak expression occurs on day 5, which is followed by a decrease before ecdysis. LmHR39 transcription could be induced by 20E in vivo and was significantly suppressed by knocking down the expression of the L. migratoria ecdysone receptor gene and early‐late gene LmHR3. After RNA interference of LmHR39 with double‐stranded RNA (dsRNA), 85% of the insects showed abnormal morphology, with curly wings after moulting and delayed eclosion time. Haematoxylin and eosin staining indicated that apolysis of the integument and wing pad cuticle in the dsLmHR39‐treated insects was delayed compared to that in the dsRNA for green fluorescent protein‐injected control. Furthermore, RNA‐sequencing and RT‐qPCR analysis showed the expression level of carboxypeptidase genes (Carboxypeptidase A (CPA) and Carboxypeptidase M (CPM)) and chitin degrading genes (LmChitinase5 (LmCHT5) and LmChitinase10 (LmCHT10)) dramatically declined in the dsLmHR39‐treated insects, implying that the LmHR39‐mediated 20E signalling pathway is involved in the regulation of carboxypeptidase genes (CPA and CPM) and chitinase genes (LmCHT5 and LmCHT10), and participated in apolysis of the integument and wing pads during locust moulting.

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Cucurbitacin B acts a potential insect growth regulator by antagonizing 20‐hydroxyecdysone activity

Abstract: In vivo and in vitro experiments demonstrate that CucB acts as a potential insect growth regulator by antagonizing 20E activity and thus blocking molting and metamorphosis induced by 20E signaling. © 2017 Society of Chemical Industry.

Cited by 22 publications

References 37 publications

In Vitro and In Vivo Antitumor Activity of Cucurbitacin C, a Novel Natural Product From Cucumber

In Vitro and In Vivo Antitumor Activity of Cucurbitacin C, a Novel Natural Product From Cucumber

Genome‐wide identification and analysis of nuclear receptors genes for lethal screening against Bemisia tabaci Q

Nuclear receptor hormone receptor 39 is required for locust moulting by regulating the chitinase and carboxypeptidase genes

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