Ai-jun Hou

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Organization: Fudan University

Department: Department of Pharmacognosy, School of Pharmacy

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Chemicals
References

Isoprenylated phenolic compounds with PTP1B inhibition from Morus alba

Co-reporter:Qing-Hua Huang, Chun Lei, Pei-Pei Wang, Jing-Ya Li, Jia Li, Ai-Jun Hou

Fitoterapia 2017 Volume 122(Volume 122) pp:

Publication Date(Web):1 October 2017

DOI:10.1016/j.fitote.2017.09.006

•Four new isoprenylated phenolics and sixteen known compounds were isolated from the root bark of Morus alba.•All the new compounds and most of the known ones showed significant inhibitory effects on PTP1B.•Albasin A is the first Diels-Alder adduct biogenetically derived from a dehydrogeranylated 2-arylbenzofuran as diene.Two new Diels-Alder adducts, albasins A and B (1 and 2), one new isoprenylated 2-arylbenzofuran, albasin C (3), one new isoprenylated flavone, albasin D (4), together with sixteen known phenolic compounds, were isolated from the root bark of Morus alba. Their structures were elucidated by extensive spectroscopic analysis, including NMR, MS, and ECD data. All the new compounds and most of the known ones showed significant inhibitory effects on PTP1B in vitro with IC50 values ranging from 0.57 to 7.49 μM.Download high-res image (155KB)Download full-size image

The total synthesis of (±)-sanggenol F

Co-reporter:Xiao Sheng, Xin-Yu Jia, Fei Tang, Yang Wang, Ai-Jun Hou

Tetrahedron 2017 Volume 73, Issue 25(Issue 25) pp:

Publication Date(Web):22 June 2017

DOI:10.1016/j.tet.2017.05.022

A concise and efficient total synthesis of sanggenol F (1) in racemic form has been completed via a sequence of 15 steps with an overall yield of 3.1%, starting from commercially available 2,4,6-trihydroxyacetophenone. Meanwhile, a semisynthesis of sanggenol F racemate has also been achieved in 11.1% overall yield via 7 steps with naturally-occurring morin (2) as the starting material. One step and a stepwise approach were employed to construct the two prenyl side chains at 2- and 6-positions by Claisen rearrangement reaction.Download high-res image (99KB)Download full-size image

Five Pairs of Meroterpenoid Enantiomers from Rhododendron capitatum

Co-reporter:Hai-Bing Liao, Guang-Hui Huang, Mei-Hua Yu, Chun Lei, and Ai-Jun Hou

The Journal of Organic Chemistry 2017 Volume 82(Issue 3) pp:

Publication Date(Web):December 30, 2016

DOI:10.1021/acs.joc.6b02800

Chemical investigation on the aerial parts of Rhododendron capitatum resulted in the discovery of five enantiomeric pairs of new meroterpenoids, (+)-/(−)-rhodonoids C (1a and 1b), E (3a and 3b), F (4a and 4b), and (−)-/(+)-rhodonoids D (2a and 2b) and G (5a and 5b). These enantiomeric pairs existed as partial racemates in a plant and were obtained by chiral HPLC separation. Their structures with absolute configurations were assigned by spectroscopic data, single-crystal X-ray diffraction, and ECD analysis. Compounds 1a and 1b are the first pair of meromonoterpenes incorporating an unprecedented 6/6/6/5 ring system, and 1a showed antiviral activity against herpes simplex virus type 1 (HSV-1) in vitro. Compounds 2a and 2b are the first examples of meromonoterpenes featuring a unique 6/6/5/5 ring system.

Sanggenol F exerts anti-diabetic effects via promoting adipocyte differentiation and modifying adipokines expression

Co-reporter:Jun-Shang Huang;Ting Wang;Jing-Jie Zhu;Ai-Jun Hou;He-Yao Wang;Jun Ji

Endocrine 2017 Volume 56( Issue 1) pp:73-81

Publication Date(Web):2017/04/01

DOI:10.1007/s12020-016-1203-3

Adipose tissue is not only a lipid storage site, but also a well-known endocrine organ. Dysfunction of adipose tissue is associated with irregular lipid metabolism, ectopic lipid accumulation and insulin resistance. It is proposed that modulating on adipose tissue is a reasonable way to ameliorate glucose and lipid metabolism. (±)-sanggenol F (SGF, purity >98.5%) was synthesized as a racemic mixture of natural (+)-sanggenol F. In this study, SGF was found to promote adipocyte differentiation, enhance insulin sensitivity, and upregulate beneficial adipokines expression in 3T3-L1 cells. Furthermore, in vivo study showed that treatment with SGF for 4 weeks improved glucose metabolism, by decreasing fasting blood glucose and enhancing insulin sensitivity. It also improved lipid metabolism, with reduced serum lipid level and ameliorated hepatic steatosis in db/db mice. During the process of target finding, we found that SGF had multiple activities of protein tyrosine phosphatase 1B inhibition, peroxisome proliferator-activated receptor γ and peroxisome proliferator-activated receptor α agonism. These results showed the potential of SGF as a candidate for the therapy of type 2 diabetes.

Macdentichalcone, a unique polycyclic dimeric chalcone from Macaranga denticulata

Co-reporter:Chun Lei, Lai-Bin Zhang, Jing Yang, Li-Xin Gao, Jing-Ya Li, Jia Li, Ai-Jun Hou

Tetrahedron Letters 2016 Volume 57(Issue 49) pp:5475-5478

Publication Date(Web):7 December 2016

DOI:10.1016/j.tetlet.2016.10.090

•Macdentichalcone (1) is an unprecedented polycyclic dimeric chalcone.•Both 1 and its proposed biosynthetic precursor 2 showed PTP1B inhibition.•The structure of 1 was established by extensive NMR methods and 13C NMR calculation.Macdentichalcone (1), an unprecedented polycyclic dimeric chalcone featuring a unique quinonoid moiety, was isolated from Macaranga denticulata, together with 1-(5,7-dihydroxy-2,2,6-trimethyl-2H-1-benzopyran-8-yl)-3-phenyl-2-propen-1-one (2), a known monomeric chalcone proposed as a biosynthetic precursor of 1. The structure of 1 was elucidated by extensive spectroscopic analysis including NMR and MS data, as well as calculation of 13C NMR chemical shifts. Both compounds 1 and 2 showed inhibitory activity against PTP1B in vitro.

New Alkaloids and -Glucosidase Inhibitory Flavonoids from Ficus hispida

Co-reporter:Zheng-Feng Shi;Chun Lei;Bang-Wei Yu;He-Yao Wang

Chemistry & Biodiversity 2016 Volume 13( Issue 4) pp:445-450

Publication Date(Web):

DOI:10.1002/cbdv.201500142

Two new pyrrolidine alkaloids, ficushispimines A (1) and B (2), a new ω-(dimethylamino)caprophenone alkaloid, ficushispimine C (3), and a new indolizidine alkaloid, ficushispidine (4), together with the known alkaloid 5 and 11 known isoprenylated flavonoids 6 – 16, were isolated from the twigs of Ficus hispida. Their structures were elucidated by spectroscopic methods. Isoderrone (8), 3′-(3-methylbut-2-en-1-yl)biochanin A (11), myrsininone A (12), ficusin A (13), and 4′,5,7-trihydroxy-6-[(1R*,6R*)-3-methyl-6-(1-methylethenyl)cyclohex-2-en-1-yl]isoflavone (14) showed inhibitory effects on α-glucosidase in vitro.

Antiviral clerodane diterpenoids from Dodonaea viscosa

Co-reporter:Lai-Bin Zhang, Hai-Bing Liao, Hai-Yan Zhu, Mei-Hua Yu, Chun Lei, Ai-Jun Hou

Tetrahedron 2016 Volume 72(Issue 49) pp:8036-8041

Publication Date(Web):8 December 2016

DOI:10.1016/j.tet.2016.10.034

Seven new clerodane diterpenoids, dodovisnoids A−G (1–7), were isolated from Dodonaea viscosa. The structures of these compounds were identified by extensive spectroscopic data. The absolute configurations of 1, 2, and 6 were assigned by X-ray crystallographic analysis. Compound 1 is an unprecedented clerodane diterpenoid possessing a new carbon skeleton that could biogenetically derive from 5,10-secoclerodane. Compounds 2–5 are rare cyclopropyl-modified clerodanes and 6 is the first dinor-clerodane featuring an alkynyl moiety. Compounds 4–7 showed antiviral activity against herpes simplex virus type 1 (HSV-1) in vitro.

Isoprenylated Flavonoids with PTP1B Inhibition from Macaranga denticulata

Co-reporter:Lai-Bin Zhang;Chun Lei;Li-Xin Gao;Jing-Ya Li

Natural Products and Bioprospecting 2016 Volume 6( Issue 1) pp:25-30

Publication Date(Web):2016 February

DOI:10.1007/s13659-015-0082-2

Three new C-methylated and isoprenylated chalcone derivatives, dentichalcones A–C (1–3), together with six known compounds (4–9), were isolated from the twigs and leaves of Macaranga denticulata. Their structures were elucidated by spectroscopic analysis, including 1D, 2D NMR, and MS data. The known compounds, (2E)-1-(5,7-dihydroxy-2,2,6-trimethyl-2H-benzopyran-8-yl)-3-(4-methoxyphenyl)-2-propen-1-one (4), (2E)-1-(5,7-dihydroxy-2,2-dimethyl-2H-benzopyran-8-yl)-3-phenyl-2-propen-1-one (5), laxichalcone (6), macarangin (7), bonanniol A (8), and bonannione A (9), showed inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) in vitro.

Two Enantiomeric Pairs of Meroterpenoids from Rhododendron capitatum

Co-reporter:Hai-Bing Liao, Chun Lei, Li-Xin Gao, Jing-Ya Li, Jia Li, and Ai-Jun Hou

Organic Letters 2015 Volume 17(Issue 20) pp:5040-5043

Publication Date(Web):October 1, 2015

DOI:10.1021/acs.orglett.5b02515

Two enantiomeric pairs of meroterpenoids, (−)- and (+)-rhodonoids A (1a and 1b) and B (2a and 2b), were isolated unprecedentedly from partially racemic mixtures that naturally occurred in Rhododendron capitatum. Their structures were fully determined by spectroscopic data, X-ray crystallography, and electronic circular dichroism analysis. Compounds 1a and 1b are the first examples of meromonoterpenes featuring a unique 6/6/6/4 ring system. Compounds 2a and 2b showed PTP1B inhibitory activity.

New Isoprenylated Phenolic Compounds from Morus laevigata

Co-reporter:Meng Wang;Bang-Wei Yu;Mei-Hua Yu;Li-Xin Gao;Jing-Ya Li;He-Yao Wang;Jia Li

Chemistry & Biodiversity 2015 Volume 12( Issue 6) pp:937-945

Publication Date(Web):

DOI:10.1002/cbdv.201400210

Abstract

Two new isoprenylated flavonoids, laevigasins A and B (1 and 2, resp.), and one new isoprenylated 2-arylbenzofuran, leavigasin C (3), together with eight known compounds, 4–11, were isolated from the twigs of Morus laevigata. Their structures were elucidated by spectroscopic methods. Laevigasin A (1) showed significant inhibitory effect on α-glucosidase in vitro. Notabilisin E (5), taxifolin (10), and hultenin (11) inhibited PTP1B phosphatase activity in vitro.

Diels–Alder adducts with PTP1B inhibition from Morus notabilis

Co-reporter:Meng Wang, Li-Xin Gao, Jue Wang, Jing-Ya Li, Mei-Hua Yu, Jia Li, Ai-Jun Hou

Phytochemistry 2015 Volume 109() pp:140-146

Publication Date(Web):January 2015

DOI:10.1016/j.phytochem.2014.10.015

•Eight Diels–Alder adducts were isolated from Morus notabilis.•Some of the Diels–Alder adducts showed inhibition against PTP1B phosphatase.•Ketalized Diels–Alder adducts in this plant were previously unknown.Eight Diels–Alder adducts, morbilisins A–H (1–8), a known analogue, chalcomoracin (9), together with eleven known flavonoids and 2-arylbenzofurans, were isolated from the leaves of Morus notabilis. Their structures were elucidated by extensive spectroscopic analysis, including 1D, 2D NMR, MS, and ECD data. Compounds 1, 5, and 7–9 showed inhibition against PTP1B phosphatase activity in vitro.Eight Diels–Alder adducts and twelve known compounds were isolated from the leaves of Morus notabilis. Some of the compounds showed inhibition against PTP1B phosphatase activity in vitro.

New Isoprenylated Xanthones from Cudrania tricuspidata

Co-reporter:Chun Lei;Chang-Chang Liu;En-Hao Pi

Helvetica Chimica Acta 2014 Volume 97( Issue 12) pp:1683-1688

Publication Date(Web):

DOI:10.1002/hlca.201400096

Abstract

A phytochemical investigation of the roots of Cudrania tricuspidata afforded three new isoprenylated xanthones, cudratricusxanthones N–P (1–3, resp.), together with five known compounds, 4–8. The structures of the new compounds were elucidated by extensive spectroscopic analyses.

Novel grayanane diterpenoids from Rhododendron principis

Co-reporter:Chang-Chang Liu, Chun Lei, Yang Zhong, Li-Xin Gao, Jing-Ya Li, Mei-Hua Yu, Jia Li, Ai-Jun Hou

Tetrahedron 2014 70(29) pp: 4317-4322

Publication Date(Web):

DOI:10.1016/j.tet.2014.05.019

Total syntheses of norartocarpin and artocarpin

Co-reporter:Wen-Jing Zhang, Jing-Fang Wu, Peng-Fei Zhou, Yang Wang, Ai-Jun Hou

Tetrahedron 2013 69(29) pp: 5850-5858

Publication Date(Web):

DOI:10.1016/j.tet.2013.05.024

2-Arylbenzofuran, Flavonoid, and Tyrosinase Inhibitory Constituents of Morus yunnanensis

Co-reporter:Xiao Hu, Jin-Wei Wu, Meng Wang, Mei-Hua Yu, Qin-Shi Zhao, He-Yao Wang, and Ai-Jun Hou

Journal of Natural Products 2012 Volume 75(Issue 1) pp:82-87

Publication Date(Web):December 13, 2011

DOI:10.1021/np2007318

Two novel 2-arylbenzofuran dimers, morusyunnansins A and B (1 and 2), two new biflavonoids, morusyunnansins C and D (3 and 4), two new flavans, morusyunnansins E and F (5 and 6), and four known flavans (7–10) were isolated from the leaves of Morus yunnanensis. Compounds 5–8 showed potent inhibitory effects on mushroom tyrosinase with IC50 values ranging from 0.12 ± 0.02 to 1.43 ± 0.43 μM.

Isoprenylated Flavonoid and Adipogenesis-Promoting Constituents of Dodonaea viscosa

Co-reporter:Lai-Bin Zhang, Jun Ji, Chun Lei, He-Yao Wang, Qin-Shi Zhao, and Ai-Jun Hou

Journal of Natural Products 2012 Volume 75(Issue 4) pp:699-706

Publication Date(Web):April 18, 2012

DOI:10.1021/np2009797

Ten new isoprenylated flavonol derivatives, dodoviscins A–J (1–10), and seven known compounds (11–17) were isolated from the aerial parts of Dodonaea viscosa. Compounds 1, 2, 4, 5, 7–9, 5,7,4′-trihydroxy-3′,5′-bis(3-methyl-2-buten-1-yl)-3-methoxyflavone (11), 5,7,4′-trihydroxy-3′,5′-bis(3-methyl-2-buten-1-yl)-3,6-dimethoxyflavone (12), 5,7,4′-trihydroxy-3′-(4-hydroxy-3-methylbutyl)-5′-(3-methyl-2-buten-1-yl)-3,6-dimethyoxyflavone (13), sakuranetin (14), and blumeatin (15) promoted adipocyte differentiation as characterized by increased triglyceride levels in 3T3L1 cells. Compounds 1, 13, and 15 also enhanced the accumulation of lipid droplets and induced upregulation of the expression of the adipocyte-specific genes aP2 and GLUT4.

New Isoprenylated Flavones and Stilbene Derivative from Artocarpus hypargyreus

Co-reporter:Mei-Hua Yu;Ting Zhao;Gui-Rui Yan;Hong-Xun Yang;He-Yao Wang

Chemistry & Biodiversity 2012 Volume 9( Issue 2) pp:394-402

Publication Date(Web):

DOI:10.1002/cbdv.201100072

Abstract

Three new isoprenylated flavones, hypargyflavones A–C (1–3, resp.), and one novel stilbene derivative, hypargystilbene A (4), together with seven known compounds, 5–11, were isolated from the stems of Artocarpus hypargyreusHance. The structures were elucidated by spectroscopic methods. Hypargyflavone A (1), cudraflavone C (8), brosimone I (10), and norartocarpin (11) showed inhibitory effects on pancreatic lipase.

Isoprenylated Flavonoids and Adipogenesis-Promoting Constituents from Morus nigra

Co-reporter:Xiao Hu, Jin-Wei Wu, Xiao-Dong Zhang, Qin-Shi Zhao, Jian-Ming Huang, He-Yao Wang, and Ai-Jun Hou

Journal of Natural Products 2011 Volume 74(Issue 4) pp:816-824

Publication Date(Web):March 14, 2011

DOI:10.1021/np100907d

Ten new isoprenylated flavonoids, nigrasins A−J (1−10), and three known compounds were isolated from the twigs of Morus nigra. Compounds 8 and 9 promoted adipogenesis, characterized by increased lipid droplet and triglyceride content in 3T3L1 cells, and induced up-regulation of the expression of adipocyte-specific genes, aP2 and GLUT4.

New isoprenylated flavonoids and adipogenesis-promoting constituents from Morus notabilis

Co-reporter:Xiao Hu, Jun Ji, Meng Wang, Jin-Wei Wu, Qin-Shi Zhao, He-Yao Wang, Ai-Jun Hou

Bioorganic & Medicinal Chemistry Letters 2011 Volume 21(Issue 15) pp:4441-4446

Publication Date(Web):1 August 2011

DOI:10.1016/j.bmcl.2011.06.020

Five new isoprenylated flavonoids, notabilisins A–E (1–5), and two known Diels–Alder adducts (6 and 7), were isolated from the twigs of Morus notabilis. Compounds 4 and 5 possess two novel pyran rings, which may be biogenetically derived from 3. Compounds 1 and 3 significantly promoted adipogenesis, characterized by increased lipid droplet and triglyceride content in 3T3L1 cells, and induced up-regulation of the expression of adipocyte-specific genes, aP2 and GLUT4.

A fast and sensitive HPLC–MS/MS analysis and preliminary pharmacokinetic characterization of cudratricusxanthone B in rats

Co-reporter:En-Hao Pi, Jun Chen, Jian-Ming Huang, Ai-Jun Hou

Journal of Chromatography B 2010 Volume 878(Issue 22) pp:1953-1958

Publication Date(Web):15 July 2010

DOI:10.1016/j.jchromb.2010.05.020

New Isoprenylated 2-Arylbenzofurans and Pancreatic Lipase Inhibitory Constituents from Artocarpus nitidus

Co-reporter:Ting Zhao;Gui-Rui Yan;Sheng-Li Pan;He-Yao Wang

Chemistry & Biodiversity 2009 Volume 6( Issue 12) pp:2209-2216

Publication Date(Web):

DOI:10.1002/cbdv.200900130

Abstract

Two new isoprenylated 2-arylbenzofurans, artonitidin A (=(2′R)-2′,3′-dihydro-2′-(1-hydroxy-1-methylethyl)-5′,7-bis(3-methylbut-2-en-1-yl)-2,4′-bi-1-benzofuran-6,6′-diol; 1) and artonitidin B (=5-[6-hydroxy-7-(3-methylbut-2-en-1-yl)-1-benzofuran-2-yl]-4-(3-methylbut-2-en-1-yl)benzene-1,3-diol; 2), together with 14 known compounds, 3–16, were isolated from the stems of Artocarpus nitidusTrec. The structures were elucidated by spectroscopic methods. Norartocarpin (3), cudraflavone C (5), brosimone I (8), artotonkin (11), albanin A (13), and artopetelin M (14) showed inhibitory effects on pancreatic lipase with IC₅₀ values ranging from 1.8±0.1 to 63.8±3.6 μM.

Iridoid Glycosides from Hedyotis corymbosa

Co-reporter:Wei Jiang;Ji-Zong Li;Min Qian;Li-Sha Kuang

Helvetica Chimica Acta 2007 Volume 90(Issue 7) pp:1296-1301

Publication Date(Web):16 JUL 2007

DOI:10.1002/hlca.200790130

Three new iridoid glycosides, hedycorysides A–C (1–3, resp.), were isolated from the whole plant of Hedyotis corymbosa (Linn.) Lam., along with four known compounds. Their structures were elucidated by extensive 1D- and 2D-NMR analysis, as well as by HR-ESI-MS experiments. The three new compounds are the first benzoylated geniposide derivatives from Hedyotis.

Prenylated Stilbenes and Their Novel Biogenetic Derivatives from Artocarpus chama

Co-reporter:Yong-Hong Wang;Dao-Feng Chen;Markus Weiller;Albrecht Wendel;Richard J. Staples

European Journal of Organic Chemistry 2006 Volume 2006(Issue 15) pp:

Publication Date(Web):30 MAY 2006

DOI:10.1002/ejoc.200600278

Two new prenylated stilbenes, artochamins F (1) and G (2), and their four novel derivatives, artochamins H–K (3–6), were isolated from the stems of Artocarpus chama. Their structures were elucidated mainly by NMR spectroscopy and mass spectrometry. The structure of 3 was confirmed by X-ray crystallographic analysis. The origin of 3–6 could be assumed biogenetically from 2. The cytotoxicity of these compounds against HepG2 cells was evaluated. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006)

Novel 2-Arylbenzofuran Derivatives from Artocarpus petelotii

Co-reporter:Lei Chen;Wei Jiang

Helvetica Chimica Acta 2006 Volume 89(Issue 5) pp:1000-1007

Publication Date(Web):24 MAY 2006

DOI:10.1002/hlca.200690076

Further phytochemical investigations on the root barks of Artocarpus petelotiiGagnep afforded four novel isoprenylated 2-arylbenzofuran derivatives, namely artopetelins D–G (1–4). Their structures were elucidated by spectroscopic methods, mainly by 2D-NMR techniques. The biogenetic origins of artopetelins F and G (3 and 4) were also postulated.

Three New Isoprenylated 2-Arylbenzofurans from Artocarpus petelotii

Co-reporter:Lei Chen

Helvetica Chimica Acta 2005 Volume 88(Issue 9) pp:2554-2560

Publication Date(Web):23 SEP 2005

DOI:10.1002/hlca.200590194

Three new isoprenylated 2-arylbenzofurans, artopetelins A–C (1–3), were isolated as minor constituents from the EtOH extract of the root barks of Artocarpus petelotiiGagnep. Their structures were elucidated by spectroscopic methods, including HR-EI-MS and 2D-NMR techniques.

Isoprenylated Xanthones and Flavonoids from Cudrania tricuspidata

Co-reporter:Ying-Shu Zou;Guo-Fu Zhu

Chemistry & Biodiversity 2005 Volume 2(Issue 1) pp:131-138

Publication Date(Web):24 JAN 2005

DOI:10.1002/cbdv.200490164

Further phytochemical investigation on the roots of Cudrania tricuspidata afforded a new isoprenylated xanthone, cudratricusxanthone I (1), two new isoprenylated flavanones, cudraflavanones C and D (2 and 3, resp.), and seven known compounds, 1,7-dihydroxy-3,6-dimethoxyxanthone (4), macluraxanthone C (5), cudraxanthones E, K, and L (6, 7, and 8, resp.), cudraflavanone A (9), and cudraflavone C (10). Their structures were identified by spectroscopic methods. Cudratricusxanthone H (12), macluraxanthone B (13), two xanthones previously isolated from this plant, and 5, showed significant inhibitory effects on four kinds of human digestive apparatus tumor cell lines (HCT-116, SMMC-7721, SGC-7901, and BGC-823) with IC₅₀ values of 2.70–12.66 μM.

Cytotoxic isoprenylated xanthones from Cudrania tricuspidata

Co-reporter:Ying-Shu Zou, Ai-Jun Hou, Guo-Fu Zhu, Yan-Feng Chen, Han-Dong Sun, Qin-Shi Zhao

Bioorganic & Medicinal Chemistry 2004 Volume 12(Issue 8) pp:1947-1953

Publication Date(Web):15 April 2004

DOI:10.1016/j.bmc.2004.01.030

Eight new isoprenylated xanthones, cudratricusxanthones A–H (1–8), were isolated from the roots of Cudrania tricuspidata, together with ten known compounds, cudraxanthones H (9) and M (10), xanthone V1a (11), toxyloxanthone C (12), macluraxanthone B (13), 1-hydroxy-3, 6, 7-trimethoxyxanthone (14), cycloartocarpesin (15), artocarpesin (16), cudraflavone B (17), and kaempferol (18). Their structures were characterized by spectroscopic methods. Xanthones 5, 7, 10, and 12 showed inhibitory effects on four kinds of human digestive apparatus tumor cell lines (HCT-116, SMMC-7721, SGC-7901, and BGC-823) with IC50 values of 1.6–11.8 μg/mL. Xanthones 2, 4, and 11 displayed significant cytotoxicity against HCT-116, SMMC-7721, and SGC-7901 (IC50=1.3–9.8 μg/mL). Flavonoids 15–17 were almost inactive.Eight new xanthones, cudratricusxanthones A–H (1–8), and ten known compounds (9–18) were isolated from the roots of Cudrania tricuspidata. 5, 7, cudraxanthone M (10), and toxyloxanthone C (12) showed inhibitory effects on HCT-116, SMMC-7721, SGC-7901, and BGC-823 cell lines (IC50=1.6–11.8 μg/mL). 2, 4, and xanthone V1a (11) displayed significant cytotoxicity against HCT-116, SMMC-7721, and SGC-7901 (IC50=1.3–9.8 μg/mL).