Experimental and In Silico Analysis of Cordycepin and its Derivatives as Endometrial Cancer Treatment

Fong, Pedro; Ao, Cheng N.; Tou, Kai Ip; Huang, Ka M.; Cheong, Chi C.; Meng, Li Rong

doi:10.3727/096504018x15235274183790

Cited by 18 publications

(24 citation statements)

References 44 publications

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“…9 However, ADA inhibitors can cause unacceptable side effects to patients. 8 The nanoscale of Au NS means it can be safely eliminated through the urinary system, thus Au NS is a star-shaped nanomaterial with a coarse surface and high surface-to-volume ratio, which allows it to act as a drug carrier for anticancer drug delivery. 18 Au NS has shown its ability to facilitate and localize drug molecules into tumor cells by the enhanced permeation retention effect.…”

Section: Resultsmentioning

confidence: 99%

Effects of Cordycepin, Gold Nanostar, and Their Combination on Endometrial Cancer Cells

Fong

Cheong

Mak

et al. 2020

Natural Product Communications

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The incidence rate of (EC) has increased significantly in the past 2 decades. The current chemotherapy for this disease can cause intolerable side effects. Recently, both cordycepin and gold nanostars have demonstrated the ability to inhibit the growth and differentiation of cancers. This study aimed to investigate the antiEC effects of cordycepin, gold nanostars (Au NS), and the combination of the two. The gold nanostars were made by seed-mediated reduction, and their morphology was confirmed by laser particle size analysis, spectrophotometry, and electron microscopy. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cytotoxicity assays, clonogenic assays, and flow cytometry were employed to evaluate the inhibition rate, survival fraction, and apoptosis in HEC-1A cells under different concentrations of cordycepin, Au NS, and their combination. This study revealed that both cordycepin and Au NS with 808 nm light exposure could inhibit cell proliferation, cause cell apoptosis, and inhibit the clone ability of EC cells. This study supports further investigations into Au NS-cordycepin in the development of new treatments for EC.

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Section: Resultsmentioning

confidence: 99%

Effects of Cordycepin, Gold Nanostar, and Their Combination on Endometrial Cancer Cells

Fong

Cheong

Mak

et al. 2020

Natural Product Communications

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“…At a dose of 56.50 µg/mL the inhibition rate was 94.39% ± 2.27% for Ishikawa cells and 99.63% ± 0.16% for HEC-1A cells, which showed that MRS5698 is highly effective in inhibiting cell proliferation in both cell lines. According to a previous study, 12 the IC 50 value of cordycepin on Ishikawa cells was 89.03 µg/mL, which is much higher than that of MRS5698 on the same cell line. It indicated that MRS5698 had a better inhibitory effect on Ishikawa cells.…”

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confidence: 79%

“…Interestingly, all of the apoptotic rates in the cisplatin groups did not reach 10% for Ishikawa cell lines. According to Fong et al, 12 cell cycle analysis with cisplatin was conducted on Ishikawa cells, the result of which showed that cisplatin arrested the S-phase in the cell cycle and inhibited the growth of Ishikawa cells. Cisplatin-induced apoptosis is a long and complicated procedure.…”

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confidence: 99%

Antitumor Effects of MRS5698, a Cordycepin Derivative, on Endometrial Cancer Cells

Fong

Loi

Wan-Fong

et al. 2019

Natural Product Communications

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Endometrial cancer drug treatments often produce undesirable effects. Thus, discovering new drugs with fewer side effects is required. Cordycepin is a constituent of Cordyceps sinensis, which has been proven to inhibit tumor growth by stimulating the adenosine A3 receptor (A3R). However, cordycepin is rapidly degraded by adenosine deaminase (ADA) and has a clinically unacceptable short half-life. One of its derivatives, MRS5698, was predicted to exhibit antitumor effects with a poor affinity to ADA by our previous validated in silico experiments. The purpose of this study was to explore the possibilities of using MRS5698 as a novel antitumor agent through experiments on Ishikawa and HEC-1A cells. The detection of inhibition and apoptotic rate of MRS5698 and cisplatin, and their combination, on Ishikawa and HEC-1A cells were performed by MTT assays and flow cytometry, respectively. The inhibition rates of MRS5698 on Ishikawa and HEC-1A cells were both significantly higher than the control groups ( P < 0.05). MRS5698 produced a higher inhibitory effect on HEC-1A cells than on Ishikawa cells with IC50 values of 20.55 and 27.25 μg/mL, respectively. MRS5698 had a stronger inhibitory effect than cisplatin on HEC-1A cells. The Annexin V-FITC/propidium iodide assays demonstrated that the total rate of apoptosis of MRS5698 on HEC-1A cells was higher than that on Ishikawa cells. The results of MTT assay and cellular apoptosis showed that the combined use of MRS5698 and cisplatin produces dose-independent antagonistic effects. MRS5698 produced antitumor effects on both cell lines, which were better than that of cordycepin. However, the combined use of MRS5698 and cisplatin produced an antagonistic effect. A further in vivo study could be considered for investigating the antitumor effects of either MRS5698 monotherapy or MRS5698 in combination with other nonplatinum-based chemotherapeutic drugs in treating endometrial cancer.

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“…In practical research, the molecular docking score is widely used [ 46 ]. Fong P. et al used molecular docking scores to evaluate the possibility of cordycepin and its derivatives as therapeutic agents for endometrial cancer [ 28 ]. In the study of molecular docking evaluation of 31 compounds, the compound numbered MRS5698 was finally successfully screened as a candidate molecule.…”

Section: Virtual Screening Technologymentioning

confidence: 99%

Prediction Methods of Herbal Compounds in Chinese Medicinal Herbs

et al. 2018

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Chinese herbal medicine has recently gained worldwide attention. The curative mechanism of Chinese herbal medicine is compared with that of western medicine at the molecular level. The treatment mechanism of most Chinese herbal medicines is still not clear. How do we integrate Chinese herbal medicine compounds with modern medicine? Chinese herbal medicine drug-like prediction method is particularly important. A growing number of Chinese herbal source compounds are now widely used as drug-like compound candidates. An important way for pharmaceutical companies to develop drugs is to discover potentially active compounds from related herbs in Chinese herbs. The methods for predicting the drug-like properties of Chinese herbal compounds include the virtual screening method, pharmacophore model method and machine learning method. In this paper, we focus on the prediction methods for the medicinal properties of Chinese herbal medicines. We analyze the advantages and disadvantages of the above three methods, and then introduce the specific steps of the virtual screening method. Finally, we present the prospect of the joint application of various methods.

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Experimental and In Silico Analysis of Cordycepin and its Derivatives as Endometrial Cancer Treatment

Cited by 18 publications

References 44 publications

Effects of Cordycepin, Gold Nanostar, and Their Combination on Endometrial Cancer Cells

Effects of Cordycepin, Gold Nanostar, and Their Combination on Endometrial Cancer Cells

Antitumor Effects of MRS5698, a Cordycepin Derivative, on Endometrial Cancer Cells

Prediction Methods of Herbal Compounds in Chinese Medicinal Herbs

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