**1. Introduction**

Natural products offer opportunities for innovation in drug discovery and play a major role for cancer cure. A considerable number of antitumor agents currently used in the clinic are of natural origin. For instance, over half of all anticancer prescription drugs approved internationally between the 1940s and 2006 were natural products or their derivatives. Among

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them, plants have been the chief source of natural compounds used for medicine [1]. Many traditional and folk medicinal plants have been use for cancer therapy throughout the world and they work very well for the prevention of cancers. Phenolic compounds play very important role for the treatment and prevention on different types of cancers which are a major health problem around the world. These secondary metabolites associated with the health benefits of human derived from consuming high levels of fresh and dried fruits and vegetables. These compounds with hydroxyl bearing aromatic ring skeleton exhibit wide range of different biological activities including: anti-inflammatory, antioxidant, cytotoxicity, antimicrobial, anti-allergic. According to WHO, 8.2 million people die each year from cancer and it is estimated 13% of all deaths worldwide [2]. In this chapter, we discuss the most recent literature on phenolic constituents from natural sources and their anticancer activities on different cancer cell lines (**Table 1**).



them, plants have been the chief source of natural compounds used for medicine [1]. Many traditional and folk medicinal plants have been use for cancer therapy throughout the world and they work very well for the prevention of cancers. Phenolic compounds play very important role for the treatment and prevention on different types of cancers which are a major health problem around the world. These secondary metabolites associated with the health benefits of human derived from consuming high levels of fresh and dried fruits and vegetables. These compounds with hydroxyl bearing aromatic ring skeleton exhibit wide range of different biological activities including: anti-inflammatory, antioxidant, cytotoxicity, antimicrobial, anti-allergic. According to WHO, 8.2 million people die each year from cancer and it is estimated 13% of all deaths worldwide [2]. In this chapter, we discuss the most recent literature on phenolic constituents from natural sources and their anticancer activities on dif-

**compounds**

Isoprenoidsubstituted flavonoids

*Dorstenia mannii* Dorsmanin F (**9**) Flavanone LeukaemiaCCRF-CEM, MDA-MB-231-

*Sophora flavescens* Isoxanthohumol (**14**) Flavonoid Breast cancer (MCF-7), ovarian cancer

*Scutellaria barbata* Luteolin (**16**) Flavonoid HepG2 and Bel7402 cells, human

Kaempferol (**8**) Flavonoid p53 or PLK-1, in MCF-7 breast cancer and

**Cytotoxic activity Refernces**

[4]

[5]

[6]

[7]

[8]

[9]

[10–12]

B16 melanoma cells [3]

HeLa cervical cancer cells, U-2 OS human osteosarcoma cell, A549 lung cancer cell, Miapaca-2, Panc-1 and SNU-213 human

pancreatic cancer cells

Flavonoid Induced apoptosis in CCRF-CEM leukemia cells

(CYP1A2).

apoptosis

cells, PC12 cell line

Kushecarpin D (**15**) Novel flavonoid Human umbilical vein endothelial cell

BCRP, CEM/ADR5000 cells

Flavonoid Human tumor (NB4, A549, SHSY5Y, PC3 and MCF7) cell lines

> (A-2780), prostate cancer (DU145 and PC-3) and colon cancer (HT-29 and SW620) cells, human cytochrome P450

line (ECV304), antiangiogenic activity, together with its antiproliferative effect on endothelial cells without causing

hepatocellular carcinoma cells, prostate cancer (PCa), assessing the PC3 and LNCaP cells, MCF-7 human breast cancer

ferent cancer cell lines (**Table 1**).

*Artocarpus heterophyllus*

Apple, grapes, tomato

green tea, pine and many other

Oriental tobacco, *Nicotiana tabacum*

Kushen *Sophora flavescens*

*Morus mesozygia* Artocarpesin (**10**),

cycloartocarpesin (**11**)

6,7-dimethoxy-4′hydroxy-8-formylflavon (**12**), 4′,7-dihydroxy-8-formyl-6 methoxyflavon (**13**)

**Source Compound name Class of** 

30 Phenolic Compounds - Natural Sources, Importance and Applications

Artocarpin (**1**), cudraflavone C (**2**), 6-prenylapigenin (**3**), kuwanon C (**4**), norartocarpin (**5**), albanin A (**6**), cudraflavone B (**7**)



**Source Compound name Class of** 

glucopyranoside (**27**)

32 Phenolic Compounds - Natural Sources, Importance and Applications

Wheat bran Triticuside A (**29**) Flavonoid

Citrus fruits Naringin (**30**) Flavonoid

Quercetin-3-*O*-α-lrhamnopyranosyl- (1→6)-β-d-glucopyranoside

Pectolinarin (**32**) and astragalin (**33**)

Vicenin (**35**) Flavonoid

*Sophora japonica* Troxerutin (**34**) Flavonoid

*Pueraria lobata* Puerarin (**40**) Isoflavone-*C*-

(**31**)

Amplexicaule A (**28**) Flavonoid

*Azadirachta indica* Quercetin-3-*O*-β-d-

*Polygonum amplexicaule*

Filamentous bacterium streptomyces

*Cirsium setidens, Aster scaber*

*Bupleurum flavum, Artemisia capillaris*

*Erythrina stricta, E.* 

*variegata*

*Toxicodendron vernicifluum*

**compounds**

glycoside

glycoside

diglycoside

Flavonoid diglycoside

Flavonoid glycoside

diglycoside

glycoside

Soybean Genistein (**36**) Isoflavone CIP2A in MCF-7-C3 and T47D breast

Soybean Daidzein (**37**) Isoflavone LnCaP, DU145 and PC3 human prostate

*Ateleia glazioviana* Biochanin A (**38**) Isoflavone Pancreatic cancer cells (Panc1 and

glucoside

Flavonoid Protect cells from H<sup>2</sup>

cytotoxicity

and MDA-MB-435

p53 and cytochrome c

cells

& DU-145

cancer cell

AsPC-1)

Alpinum isoflavone (**39**) Isoflavon Leukemia CEM/ADR5000 cells, drug-

Butein (**41**) Chalcone Human colon adenocarcinoma cell line

HER2<sup>+</sup>

line

melanoma cell line

cancer cell lines, MCF-7 breast

colon carcinoma HCT116

cells, colon cancer HT-29 cell

resistant breast adenocarcinoma MDA-MB-231-*BCRP* cells, CEM/ADR5000 cells,

Myeloid leukemia cell lines, U937, Kasumi-1, HL-60 and NB4 cells, breast cancer MCF-7/adriamycin (MCF-7/adr)

220.1, human leukemia cells HL-60,

 HCC-1419, HCC-2218 and SKBR-3 breast cancer cells, human PCa (LNCaP, CWR22Rν1 and PC-3), human uveal melanoma cell lines (M17, SP6.5 and C918), HeLa human cervical cancer cell

MDA-MB-231)

**Cytotoxic activity Refernces**

[27]

[28]

[29]

[32]

[33]

[34]

[35, 36]

[37, 38]

[39]

[40]

[41]

[42]

[43–47]

[30, 31]

O2 -induced

Human breast cancer cell lines MCF-7

Human breast cancer cells (MCF-7 and

Breast cancer (TNBC), MDA-MB-231, MDA-MB-468 and BT-549 cells, K562 (human leukemia cell line), Raji (human Burkitt's lymphoma cell line) and NK-92MI

Human lung cancer A549 cells through

Human brain neuroblastoma SK-N-SH

Human prostate cancer radioresistant (DU145) and radiosensitive (PC3) cells

Hepatocellular carcinoma HEP-G2 cells, human prostate carcinoma LNCaP, PC- 3

cancer cells, human prostate cancer cell PC3-M, PC3 and DU-145 human PCa cell lines, sarcomatoid mammary carcinoma cell line F3II, B16F0



**Table 1.** Cytotoxic phenolics from different natural source.

**Source Compound name Class of** 

34 Phenolic Compounds - Natural Sources, Importance and Applications

9,10-anthraquinone (**63**), 2-hydroxy-9,10 anthraquinone (**64**), 2,3-dihydroxy-9,10 anthraquinone (**65**)

glucopyranoside **(66)**

8-hydroxycudraxanthone G (**71**), cudraxanthone

1,6,8-trihydroxy-2,3,4,5 tetramethoxyxanthone (**73**), 1,6-dihydroxy-

pentamethoxyxanthone (**74**)

*Garcinia hunburyi* Desoxymorellin (**75**) Xanthone HEL (human embryonic lung fibroblasts)

*Garcinia lateriflora* Lateriflorone (**77**) Xanthone P388 cancer cell line [78] *Garcinia morella* Gambogic acid (**78**) Xanthone T47D and DLD-1 breast cancer cells [79]

*Garcinia cowa* Cowaxanthones G (**80**) Xanthone Human cancer cell lines (HeLa, PANC-1

Gaudichaudione (**79**) Xanthone Parental murine leukemia P388 and

*Garcinia cantleyana* Cantleyanone (**76**) Xanthone Breast cancer (MDA-MB-231 and

*Rheum palmatum* Chrysophanol 8-*O*-beta- (6′-acetyl)

*Garcinia nobilis* Morusignin I (**70**),

I (**72**)

2,3,4,5,8-

*Streptomyces* sp. ERINLG-26

*Cratoxylum maingayi* and *C. cochinchinense*

*Garcinia mangostana*

*Securidaca longepedunculata*

*Garcinia gaudichaudii*

Mangrove fungus *Phomopsis longicolla*, Fungus *Phomopsis longicolla, Rhizhopora mucronata*

**compounds**

Anthraquinone glucoside

Formoxanthone C (**67**) Xanthone Human lung cancer (NCI-H187), MCF-7

Phomoxanthone A (**68**) Xanthone Tumour cell lines or of blood cancer cell lines

Garcinone C (**69**) Xanthone MCF-7, A549, Hep-G2 and CNE cell lines [73]

Xanthone Breast cancer cells transduced with

and normal AML12

Xanthone Human pancreatic cancer cell line, PANC-1

cancer)

HeLa cells

and A549)

*Rumex dentatus* Chrysophanol (**62**) Anthraquinone MCF-7 breast cancer cell line, gastric

**Cytotoxic activity Refernces**

[65]

[66–68]

[69]

[70, 71]

[72]

[74]

[75]

[76]

[77]

[80]

[81]

cancer 7901 cells, Melanoma A375 cells and oophoroma SKOV-3 cells

Human oral squamous cell carcinoma (HSC-2) and salivary gland tumor (HSG) cell lines than against normal human

(breast adenocarcinoma), KB (human oral cancer), HeLa (human cervical cancer)

control vector (MDA-MB-231-pcDNA3), Human wild-type HCT116 (p53+/+) colon cancer cells, Human glioblastoma multiforme U87MG cells, Human HepG2 hepatocellular carcinoma cells

and HeLa (Henrietta Lacks cervical

MCF-7), ovarian cancer (CaOV-3) and

P388/doxorubicin-resistant cell lines

Anthraquinone A549 lung adenocarcinoma and

COLO320 cancer cell line

gingival fibroblasts (HGF)

and HT-29 (colon cancer)
