Synthesis of xanthone derivatives and anti-hepatocellular carcinoma potency evaluation: induced apoptosis
Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique. Their in vitro inhibition potency against the growth of four cancer cell lines was evaluated. XD-1 ∼ [6,9,10-trihydroxy-3,3-dimethyl-5-(2-methylbut-3-en-2-yl)-3 H ,7 H -pyrano[2,3- c ]xanthen-7-one] was confirm...
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| Veröffentlicht in: | RSC advances 2019-12, Vol.9 (7), p.4781-4791 |
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| creator | Liu, Jie Bao, Hui Wang, Huailing Luo, Qiang Zuo, Jianhong Liu, Zhigang Qiu, Shuqi Sun, Xizhuo Liu, Xiaoyu |
| description | Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique. Their
in vitro
inhibition potency against the growth of four cancer cell lines was evaluated. XD-1 ∼ [6,9,10-trihydroxy-3,3-dimethyl-5-(2-methylbut-3-en-2-yl)-3
H
,7
H
-pyrano[2,3-
c
]xanthen-7-one] was confirmed as the most active agent against HepG2 cell line growth with IC
50
of 18.6 ± 2.31 μM. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for XD-1. XD-1 arrested HepG2 cells on the G0/G1 phase, as indicated by the decreased expressions of cyclin D and CDK2 and the increased expressions of p21. Western blot implied that XD-1 regulated p53/MDM2 to a better healthier state. Moreover, XD-1-induced cell apoptosis was mitochondrion-mediated, as evidenced by caspase activation and involved the PI3K/AKT/mTOR signaling pathway. All the evidence supports that XD-1 is a significant anti-cancer agent for HCC.
Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique. |
| doi_str_mv | 10.1039/c9ra06408g |
| format | Article |
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in vitro
inhibition potency against the growth of four cancer cell lines was evaluated. XD-1 ∼ [6,9,10-trihydroxy-3,3-dimethyl-5-(2-methylbut-3-en-2-yl)-3
H
,7
H
-pyrano[2,3-
c
]xanthen-7-one] was confirmed as the most active agent against HepG2 cell line growth with IC
50
of 18.6 ± 2.31 μM. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for XD-1. XD-1 arrested HepG2 cells on the G0/G1 phase, as indicated by the decreased expressions of cyclin D and CDK2 and the increased expressions of p21. Western blot implied that XD-1 regulated p53/MDM2 to a better healthier state. Moreover, XD-1-induced cell apoptosis was mitochondrion-mediated, as evidenced by caspase activation and involved the PI3K/AKT/mTOR signaling pathway. All the evidence supports that XD-1 is a significant anti-cancer agent for HCC.
Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique.</description><identifier>ISSN: 2046-2069</identifier><identifier>EISSN: 2046-2069</identifier><identifier>DOI: 10.1039/c9ra06408g</identifier><language>eng</language><publisher>Cambridge: Royal Society of Chemistry</publisher><subject>Anticancer properties ; Apoptosis ; Biotechnology ; Cell death ; Derivatives ; Necrosis</subject><ispartof>RSC advances, 2019-12, Vol.9 (7), p.4781-4791</ispartof><rights>Copyright Royal Society of Chemistry 2019</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c317t-89ab2a15852f3ef0b3b6e84824f42c22c40f86a530334db82b39616892ff1693</citedby><cites>FETCH-LOGICAL-c317t-89ab2a15852f3ef0b3b6e84824f42c22c40f86a530334db82b39616892ff1693</cites><orcidid>0000-0002-8372-3700 ; 0000-0003-0078-2199</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,864,27924,27925</link.rule.ids></links><search><creatorcontrib>Liu, Jie</creatorcontrib><creatorcontrib>Bao, Hui</creatorcontrib><creatorcontrib>Wang, Huailing</creatorcontrib><creatorcontrib>Luo, Qiang</creatorcontrib><creatorcontrib>Zuo, Jianhong</creatorcontrib><creatorcontrib>Liu, Zhigang</creatorcontrib><creatorcontrib>Qiu, Shuqi</creatorcontrib><creatorcontrib>Sun, Xizhuo</creatorcontrib><creatorcontrib>Liu, Xiaoyu</creatorcontrib><title>Synthesis of xanthone derivatives and anti-hepatocellular carcinoma potency evaluation: induced apoptosis</title><title>RSC advances</title><description>Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique. Their
in vitro
inhibition potency against the growth of four cancer cell lines was evaluated. XD-1 ∼ [6,9,10-trihydroxy-3,3-dimethyl-5-(2-methylbut-3-en-2-yl)-3
H
,7
H
-pyrano[2,3-
c
]xanthen-7-one] was confirmed as the most active agent against HepG2 cell line growth with IC
50
of 18.6 ± 2.31 μM. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for XD-1. XD-1 arrested HepG2 cells on the G0/G1 phase, as indicated by the decreased expressions of cyclin D and CDK2 and the increased expressions of p21. Western blot implied that XD-1 regulated p53/MDM2 to a better healthier state. Moreover, XD-1-induced cell apoptosis was mitochondrion-mediated, as evidenced by caspase activation and involved the PI3K/AKT/mTOR signaling pathway. All the evidence supports that XD-1 is a significant anti-cancer agent for HCC.
Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique.</description><subject>Anticancer properties</subject><subject>Apoptosis</subject><subject>Biotechnology</subject><subject>Cell death</subject><subject>Derivatives</subject><subject>Necrosis</subject><issn>2046-2069</issn><issn>2046-2069</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><recordid>eNpNkM1LAzEQxYMoWGov3oWAN2E1H7sx8VaKVqEgaO9LNpvYlG2yJtni_vdGK-rAMDPwe2_gAXCO0TVGVNwoESRiJeJvR2BCUMkKgpg4_refglmMW5SLVZgwPAH2dXRpo6ON0Bv4IfPhnYatDnYvk93rCKVrcydbbHQvk1e664ZOBqhkUNb5nYS9T9qpEeq97Ias8u4OWtcOSmdl7_vks_8ZODGyi3r2M6dg_XC_XjwWq-fl02K-KhTFt6ngQjZE4opXxFBtUEMbpnnJSWlKoghRJTKcyYoiSsu24aShgmHGBTEGM0Gn4PJg2wf_PuiY6q0fgssfa0IJE6jKbKauDpQKPsagTd0Hu5NhrDGqv8KsF-Jl_h3mMsMXBzhE9cv9hU0_AdzCciE</recordid><startdate>20191209</startdate><enddate>20191209</enddate><creator>Liu, Jie</creator><creator>Bao, Hui</creator><creator>Wang, Huailing</creator><creator>Luo, Qiang</creator><creator>Zuo, Jianhong</creator><creator>Liu, Zhigang</creator><creator>Qiu, Shuqi</creator><creator>Sun, Xizhuo</creator><creator>Liu, Xiaoyu</creator><general>Royal Society of Chemistry</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope><orcidid>https://orcid.org/0000-0002-8372-3700</orcidid><orcidid>https://orcid.org/0000-0003-0078-2199</orcidid></search><sort><creationdate>20191209</creationdate><title>Synthesis of xanthone derivatives and anti-hepatocellular carcinoma potency evaluation: induced apoptosis</title><author>Liu, Jie ; Bao, Hui ; Wang, Huailing ; Luo, Qiang ; Zuo, Jianhong ; Liu, Zhigang ; Qiu, Shuqi ; Sun, Xizhuo ; Liu, Xiaoyu</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c317t-89ab2a15852f3ef0b3b6e84824f42c22c40f86a530334db82b39616892ff1693</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Anticancer properties</topic><topic>Apoptosis</topic><topic>Biotechnology</topic><topic>Cell death</topic><topic>Derivatives</topic><topic>Necrosis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Liu, Jie</creatorcontrib><creatorcontrib>Bao, Hui</creatorcontrib><creatorcontrib>Wang, Huailing</creatorcontrib><creatorcontrib>Luo, Qiang</creatorcontrib><creatorcontrib>Zuo, Jianhong</creatorcontrib><creatorcontrib>Liu, Zhigang</creatorcontrib><creatorcontrib>Qiu, Shuqi</creatorcontrib><creatorcontrib>Sun, Xizhuo</creatorcontrib><creatorcontrib>Liu, Xiaoyu</creatorcontrib><collection>CrossRef</collection><collection>Engineered Materials Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Materials Research Database</collection><jtitle>RSC advances</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Liu, Jie</au><au>Bao, Hui</au><au>Wang, Huailing</au><au>Luo, Qiang</au><au>Zuo, Jianhong</au><au>Liu, Zhigang</au><au>Qiu, Shuqi</au><au>Sun, Xizhuo</au><au>Liu, Xiaoyu</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of xanthone derivatives and anti-hepatocellular carcinoma potency evaluation: induced apoptosis</atitle><jtitle>RSC advances</jtitle><date>2019-12-09</date><risdate>2019</risdate><volume>9</volume><issue>7</issue><spage>4781</spage><epage>4791</epage><pages>4781-4791</pages><issn>2046-2069</issn><eissn>2046-2069</eissn><abstract>Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique. Their
in vitro
inhibition potency against the growth of four cancer cell lines was evaluated. XD-1 ∼ [6,9,10-trihydroxy-3,3-dimethyl-5-(2-methylbut-3-en-2-yl)-3
H
,7
H
-pyrano[2,3-
c
]xanthen-7-one] was confirmed as the most active agent against HepG2 cell line growth with IC
50
of 18.6 ± 2.31 μM. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for XD-1. XD-1 arrested HepG2 cells on the G0/G1 phase, as indicated by the decreased expressions of cyclin D and CDK2 and the increased expressions of p21. Western blot implied that XD-1 regulated p53/MDM2 to a better healthier state. Moreover, XD-1-induced cell apoptosis was mitochondrion-mediated, as evidenced by caspase activation and involved the PI3K/AKT/mTOR signaling pathway. All the evidence supports that XD-1 is a significant anti-cancer agent for HCC.
Twenty-one xanthone derivatives (XDs) were synthesized by a microwave-assisted technique.</abstract><cop>Cambridge</cop><pub>Royal Society of Chemistry</pub><doi>10.1039/c9ra06408g</doi><tpages>11</tpages><orcidid>https://orcid.org/0000-0002-8372-3700</orcidid><orcidid>https://orcid.org/0000-0003-0078-2199</orcidid><oa>free_for_read</oa></addata></record> |
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| source | DOAJ Directory of Open Access Journals; EZB-FREE-00999 freely available EZB journals; PubMed Central; PubMed Central Open Access |
| subjects | Anticancer properties Apoptosis Biotechnology Cell death Derivatives Necrosis |
| title | Synthesis of xanthone derivatives and anti-hepatocellular carcinoma potency evaluation: induced apoptosis |
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