Rhubarb is a Chinese traditional medicine. Ninety-four compounds belonging to five different classes of compounds (anthraquinone, anthrones, stilbenes, flavonoids and acylglucosides) have so far been identified in rhubarb. These constituents are effective in purgative, clearing heat-fire, removing toxic materials from the body, cooling blood and promoting blood circulation. Recent studies have shown that the appropriate processing methods may directly impact on its remedial activities and chemical compositions. Here, we provide a comprehensive review of the chemical compositions, pharmacological activities and processing methods of rhubarb.
Aburjai, T.A. (2000). Anti-platelet stilbenes from aerial parts of Rheum palaestinum. Phytochemistry 55(5): 407–410.
Cha, T. -L., Qiu, L., Chen, C. -T., Wen, Y., and Hung, M. -C. (2005). Emodin down-regulates androgen receptor and inhibits prostate cancer cell growth. Cancer Res. 65(6): 2287–2295.
Chan, T., Chang, C., Koonchanok, N., and Geahlen, R. (1993). Selective inhibition of the growth of ras-transformed human bronchial epithelial cells by emodin, a protein-tyrosine kinase inhibitor. Biochem. Biophys. Res. Commun. 193(3): 1152–1158.
Chang, C., Ashendel, C., Geahlen, R., McLaughlin, J., and Waters, D. (1996). Oncogene signal transduction inhibitors from medicinal plants. In Vivo 10(2): 185–190.
Chen, H., Hsieh, W., Chang, W., and Chung, J. (2004). Aloe-emodin induced in vitro G2/M arrest of cell cycle in human promyelocytic leukemia HL-60 cells. Food Chem. Toxicol. 42(8): 1251–1257.
Chen, Y. -Y., Chiang, S. -Y., Lin, J. -G., Ma, Y. -S., Liao, C. -L., Weng, S. -W., Lai, T. -Y., and Chung, J. -G. (2010). Emodin, aloe-emodin and rhein inhibit migration and invasion in human tongue cancer SCC-4 cells through the inhibition of gene expression of matrix metalloproteinase-9. Int. J. Oncol. 36(5): 1113–1120.
Cichewicz, R.H., Zhang, Y., Seeram, N.P., and Nair, M.G. (2004). Inhibition of human tumor cell proliferation by novel anthraquinones from daylilies. Life Sci. 74(14): 1791–1799.
Cun, Z., Li, L., Yong-Qing, X., Guo-Fang, T., Dong-Dong, C., Yun, W., Yu-Tian, L., and Wen-Qian, H. (2010). Two new anthraquinone glycosides from the roots of Rheum palmatum. J. Asian Nat. Prod. Res. 12(12): 1026–1032.
Darias, V. (1987). Analgesic activity of some phenolic components in rhubarb. Farmaco (Ed Sci) 33: 460–465.
Dequeker, R., Lemli, J., and Cuveele, J. (1964). Anthraquinone drugs. Ⅶ. Densitometric determination of the sennidins, rheidins and rhein in the root of rhubarb. Planta Med. 12(1): 51–56.
Ejderhamn, J., Finkel, Y., and Strandvik, B. (1989). Na, K-ATPase activity in rectal mucosa of children with ulcerative colitis and Crohn's disease. Scand. J. Gastroenterol. 24(9): 1121–1125.
Gao, L, Xu, X, and Yang, J (2013). Chemical constituents of the roots of Rheum officinale. Chem. Nat. Compd. 49(4): 603–605.
Gao, L., Xu, X., and Yang, J. (2013). Chemical constituents of the roots of Rheum officinale. Chem. Nat. Compd. 49(4): 603–605.
Ham, I. -H., Oh, I. -S., Whang, W. -K., and Kim, I. -H. (1994). Pharmaco-constituents of Korean cultivated Rhubarb leaves-the flavonoids from leaves. Yakhak Hoeji 38(4): 410–417.
Hanessian, S., Simard, D., Bayrakdarian, M., Therrien, E., Nilsson, I., and Fjellström, O. (2008). Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs. Bioorg. Med. Chem. Lett. 18(6): 1972–1976.
HARIMA, S., MATSUDA, H., and KUBo, M. (1994). Study of various rhubarbs regarding the cathartic effect and endotoxin-induced disseminated intravascular coagulation. Biol. Pharm. Bull. 17(11): 1522–1525.
Hesse, O. (1908). Rhapontic root and Austrian rhubarb. J fuer Praktische Chemie (Leipzig) 77: 321–352.
Holzschuh, L., Kopp, B., and Kubelka, W. (1982). Physcion-8-O-beta-D-gentiobioside, a new anthraquinone glycoside from rhubarb roots. Planta Med. 46(3): 159–161.
Huang, Q., Lu, G., Shen, H.M., Chung, M.C., and Ong, C.N. (2007). Anti-cancer properties of anthraquinones from rhubarb. Med. Res. Rev. 27(5): 609–630.
Huang, Z., Dong, Y., and Ye, W. (1997). Clinical observation on treatment of infantile cholestatic hepatitis syndrome by rhubarb. Chinese journal of integrated traditional and Western medicine 17(8): 459–461.
Huiyan, X., Xiaofeng, Z., Huan, W., and Li, P.A.N. (2003). HPLC determination of anthraquinones from various parts of R. T anguticum, R. undulatum and R. spiciforme. Acta Bot. Boreali-Occidential Sinica 23(2): 328–331.
Jin, W., Ge, R. -L., Wei, Q. -J., Bao, T. -Y., Shi, H. -M., and Tu, P. -F. (2006). Development of high-performance liquid chromatographic fingerprint for the quality control of Rheum tanguticum Maxim. ex Balf. J. Chromatogr. 1132(1-2): 320–324.
Jong-Chol, C., Tsukasa, M., Kazuo, A., Hiroaki, K., Haruki, Y., and Yasuo, O. (1987). Anti-Bacteroides fragilis substance from rhubarb. J. Ethnopharmacol. 19(3): 279–283.
Kashiwada, Y., Nonaka, G., and Nishioka, I. (1986). Tannins and related compounds. XLⅧ. Rhubarb. (7). Isolation and characterization of new dimeric and trimeric procyanidins. Chem. Pharm. Bull. (Tokyo) 34(10): 4083–4091.
Kashiwada, Y., Nonaka, G. -i., and Nishioka, I. (1988). Galloylsucroses from rhubarbs. Phytochemistry 27(5): 1469–1472.
Kashiwada, Y., Nonake, G., and Nishioka, I. (1984). Studies on Rhubarb (Rhei Rhizoma). Ⅵ. Isolation and characterization of stilbenes. Chem. Pharm. Bull. 32(9): 3501–3517.
Ko, S.K. (2000). A new stilbene diglycoside from Rheum undulatum. Arch. Pharmacal Res. 23(2): 159–162.
Ko, S.K., Lee, S.M., and Whang, W.K. (1999). Anti-platelet aggregation activity of stilbene derivatives from Rheum undulatum. Arch. Pharmacal Res. 22(4): 401–403.
Komatsu, K., Nagayama, Y., Tanaka, K., Ling, Y., Cai, S.Q., Omote, T., and Meselhy, M.R. (2006). Comparative study of chemical constituents of rhubarb from different origins. Chem. Pharm. Bull. (Tokyo) 54(11): 1491–1499.
Krenn, L., Pradhan, R., Presser, A., Reznicek, G., and Kopp, B. (2004). Anthrone C-glucosides from Rheum emodi. Chem. Pharm. Bull. 52(4): 391–393.
Kuo, P. -L., Lin, T. -C., and Lin, C. -C. (2002). The antiproliferative activity of aloe-emodin is through p53-dependent and p21-dependent apoptotic pathway in human hepatoma cell lines. Life Sci. 71(16): 1879–1892.
Kuo, Y. -C., Sun, C. -M., Ou, J. -C., and Tsai, W. -J. (1997). A tumor cell growth inhibitor from Polygonum hypoleucum Ohwi. Life Sci. 61(23): 2335–2344.
Lee, H. -Z., Hsu, S. -L., Liu, M. -C., and Wu, C. -H. (2001). Effects and mechanisms of aloe-emodin on cell death in human lung squamous cell carcinoma. Eur. J. Pharmacol. 431(3): 287–295.
LEMLI, J., Bequeker, R., and Cuveele, J. (1964). SENNIDIN C, REIDIN B AND REIDIN C, HETERODIANTHRONES OF THE FRESH ROOTS OF RHUBARB. Pharm. Weekbl. 99: 613.
Li, F., Wang, S., Wang, X., Ren, Q., Wang, W., Shang, G., Zhang, L., and Zhang, S. (2008). Novel exploration of cathartic pharmacology induced by rhubarb. China J. Chin. Mater. Med. 33(4): 481–484.
Li, J., Li, J., and He, W. (1998). Studies on the non-anthraquinones of Hotao rhubarb (Rheum hotaoense). Chinese Traditional and Herbal Drugs 29: 721–722.
Li, Y., Miao, X., Wu, P., Li, Y., Liu, F., and Wei, S. (2011). Influences of different initial processing methods on Rheum palmatum. J. Chin. Med. Mater. 34(8): 1196–1199.
Liselotte, K., Riddhi, P., Armin, P., Gottfried, R., and Brigitte, K. (2004). Anthrone C-glucosides from Rheum emodi. Cheminform 35(37): 391.
Lu, K., Tong, W., and Hu, R. (1998). Studies on the chemical constituents of rheum's Callus. Chin. Tradit. Herb. Drugs 29: 438–440.
Mase, A., Makino, B., Tsuchiya, N., Yamamoto, M., Kase, Y., Takeda, S., and Hasegawa, T. (2010). Active ingredients of traditional Japanese (kampo) medicine, inchinkoto, in murine concanavalin A-induced hepatitis. J. Ethnopharmacol. 127(3): 742–749.
Matsuda, H., Shimoda, H., Morikawa, T., and Yoshikawa, M. (2001). Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity. Bioorg. Med. Chem. Lett. 11(14): 1839–1842.
Matsuda, H., Tomohiro, N., Hiraba, K., Harima, S., Ko, S., Matsuo, K., Yoshikawa, M., and Kubo, M. (2001). Study on anti-Oketsu activity of rhubarb Ⅱ. Anti-allergic effects of stilbene components from Rhei undulati Rhizoma (dried rhizome of Rheum undulatum cultivated in Korea). Biol. Pharm. Bull. 24(3): 264–267.
Moon, M.K., Kang, D.G., Lee, J.K., Kim, J.S., and Lee, H.S. (2006). Vasodilatory and anti-inflammatory effects of the aqueous extract of rhubarb via a NO-cGMP pathway. Life Sci. 78(14): 1550–1557.
Nonaka, G., Minami, M., and Nishioka, I. (1977). Studies on rhubarb (Rhei rhizoma). Ⅲ. Stilbene glycosides. Chem. Pharm. Bull. (Tokyo) 25(9): 2300–2305.
Nonaka, G., NISHIOKA, I., NAGASAWA, T., and OURA, H. (1981). Tannins and related compounds. I. Rhubarb (1). Chem. Pharm. Bull. 29(10): 2862–2870.
Oshio, H., IMAI, S., FUJIOKA, S., SUGAWARA, T., MIYAMOTO, M., and TSUKUI, M. (1974). Investigation of Rhubarbs. Ⅲ. New purgative constituents, sennosides E and F. Chem. Pharm. Bull. 22(4): 823–831.
Park, E. -K., Choo, M. -K., Yoon, H. -K., and Kim, D. -H. (2002). Antithrombotic and antiallergic activities of rhaponticin from Rhei Rhizoma are activated by human intestinal bacteria. Arch. Pharmacal Res. 25(4): 528–533.
Pecere, T., Gazzola, M.V., Mucignat, C., Parolin, C., Dalla Vecchia, F., Cavaggioni, A., Basso, G., Diaspro, A., Salvato, B., and Carli, M. (2000). Aloe-emodin is a new type of anticancer agent with selective activity against neuroectodermal tumors. Cancer Res. 60(11): 2800–2804.
Pecere, T., Sarinella, F., Salata, C., Gatto, B., Bet, A., Dalla Vecchia, F., Diaspro, A., Carli, M., Palumbo, M., and Palù, G. (2003). Involvement of p53 in specific anti-neuroectodermal tumor activity of aloe-emodin. Int. J. Cancer 106(6): 836–847.
Seo, E.J., Ngoc, T.M., Lee, S. -M., Kim, Y.S., and Jung, Y. -S. (2012). Chrysophanol-8-O-glucoside, an anthraquinone derivative in rhubarb, has antiplatelet and anticoagulant activities. J. Pharmacol. Sci. 118(2): 245–254.
Shi, Y. -Q., Fukai, T., Sakagami, H., Kuroda, J., Miyaoka, R., Tamura, M., Yoshida, N., and Nomura, T. (2001). Cytotoxic and DNA damageinducing activities of low molecular weight phenols from rhubarb. Anticancer Res. 21(4A): 2847–2853.
Shieh, D. -E., Chen, Y. -Y., Yen, M. -H., Chiang, L. -C., and Lin, C. -C. (2004). Emodin-induced apoptosis through p53-dependent pathway in human hepatoma cells. Life Sci. 74(18): 2279–2290.
Shikishima, Y., Takaishi, Y., Honda, G., Ito, M., Takeda, Y., Kodzhimatov, O.K., and Ashurmetov, O. (2001). Phenylbutanoids and stilbene derivatives of Rheum maximowiczⅡ. Phytochemistry 56(4): 377–381.
Siegers, C., von Hertzberg-Lottin, E., Otte, M., and Schneider, B. (1993). Anthranoid laxative abuse--a risk for colorectal cancer? Gut 34(8): 1099–1101.
Singh, P., Pant, G.J.N., and Rawat, M. (2016). Phytochemistry and Biological Activity Perspectives of Rheum Species. Natural Products Journal 6(2): 84–93.
Singh, S.S., Pandy, S.C., Singh, R., and Agarwal, S.K. (2005). 1,8-Dihydroxyanthraquinone derivatives from rhizomes of Wall. Indian J. Chem. 43B: 1494–1496.
Sun, J., Wu, Y., Dong, S., Li, X., and Gao, W. (2018). Influence of the drying method on the bioactive compounds and pharmacological activities of rhubarb. J. Sci. Food Agric. 98(9): 3551–3562.
Suresh Babu, K., Tiwari, A.K., Srinivas, P.V., Ali, A.Z., China Raju, B., and Rao, J.M. (2004). Yeast and mammalian α-glucosidase inhibitory constituents from Himalayan rhubarb Rheum emodi Wall. ex Meisson. Bioorg. Med. Chem. Lett. 14(14): 3841–3845.
Wang, A., Li, J., and Li, J. (2010). Chemical constituents of Rheum emodi. Chin. Tradit. Herb. Drugs 41(3): 343–347.
Wang, C. -C., Huang, Y. -J., Chen, L. -G., Lee, L. -T., and Yang, L. -L. (2002). Inducible nitric oxide synthase inhibitors of Chinese herbs Ⅲ. Rheum palmatum. Planta Med. 68(10): 869–874.
Wang, J. -b., Kong, W. -j., Wang, H. -j., Zhao, H. -p., Xiao, H. -y., Dai, C. -m., Xiao, X. -h., Zhao, Y. -l., Jin, C., and Zhang, L. (2011). Toxic effects caused by rhubarb (Rheum palmatum L. ) are reversed on immature and aged rats. J. Ethnopharmacol. 134(2): 216–220.
Wei, Y.H., Zhang, C.Z., Chong, L.I., and Tao, B.Q. (2004). Chemical constituents of Rheum glabricaule (Ⅰ). Chin. Tradit. Herb. Drugs 35(7): 732–734.
Weitz, J.I. (2003). A novel approach to thrombin inhibition. Thromb. Res. 109: S17–S22.
Xiang, L., Liu, X., and Fan, G. (2005). Chemical constituents from Rheum nanum Siev. ex Pall. (Ⅱ). Chin Tradit Herb Drugs 36: 1306–1309.
Xing-Sheng, F.U., Chen, F., Liu, X.H., Hu, X.U., and Zhou, Y.Z. (2011). Progress in research of chemical constituents and pharmacological actions of Rhubarb. Chin. J. New Drugs 20(16): 1534–1538+1568.
Xiuwei, Y., Jing, Z., and Yan, Z. (1998). Studies on Rhubarb I. A New Malonylanthraquinone Glycoside from the Rhizomes of Qinling Rhubarb (Rheum qinlingense). Chin. Tradit. Herb. Drugs 5: .
Xu Qing, Q.Y., Su, X.J., and Luo, W.S. (2009). Chemical constituents in Rheum palmatum. Chin. Tradit. Herb. Drugs 40(04): 533–536.
Yakubu, M., and Salimon, S. (2015). Antidiarrhoeal activity of aqueous extract of Mangifera indica L. leaves in female albino rats. J. Ethnopharmacol. 163: 135–141.
Yamagishi, T., Nishizawa, M., Ikura, M., Hikichi, K., Nonaka, G. -I., and Nishioka, I. (1987). New Laxative Constituents of Rhubarb. Isolation and Characterization of Rheinosides A, B, C and D. Chem. Pharm. Bull. (Tokyo) 35(8): 3132–3138.
Wei, Y, Wu, X, Zhang, C., and Li, C. (2005). Studies on Chemical Constituents of Rheum glabricaule Sam. J. Chin. Med. Mater. 28(8): 658–660.
Zhang, L., Chang, C. -j., Bacus, S.S., and Hung, M. -C. (1995). Suppressed transformation and induced differentiation of HER-2/neu-overexpressing breast cancer cells by emodin. Cancer Res. 55(17): 3890–3896.
Zhang, X. -P., Li, Z. -F., Liu, X. -G., Wu, Y. -T., Wang, J. -X., Wang, K. -M., and Zhou, Y. -F. (2005). Effects of emodin and baicalein on rats with severe acute pancreatitis. World Journal of Gastroenterology: WJG 11(14): 2095.
Zhao, Y.L., Wang, J.B., Zhou, G.D., Shan, L.M., and Xiao, X.H. (2009). Investigations of Free Anthraquinones from Rhubarb Against α-Naphthylisothiocyanate-induced Cholestatic Liver Injury in Rats. Basic Clin. Pharmacol. Toxicol. 104(6): 463–469.
Zhou, X., Song, B., Jin, L., Hu, D., Diao, C., Xu, G., Zou, Z., and Yang, S. (2006). Isolation and inhibitory activity against ERK phosphorylation of hydroxyanthraquinones from rhubarb. Bioorg. Med. Chem. Lett. 16(3): 563–568.
Zhu, B., Lin, Y., Zhu, C. -F., Zhu, X. -L., Huang, C. -Z., Lu, Y., Cheng, X. -X., and Wang, Y. -J. (2011). Emodin inhibits extracellular matrix synthesis by suppressing p38 and ERK1/2 pathways in TGF-β1-stimulated NRK-49F cells. Mol. Med. Report. 4(3): 505–509.
Zhu, T., Liu, X., Wang, X., Cao, G., Qin, K., Pei, K., Zhu, H., Cai, H., Niu, M., and Cai, B. (2016). Profiling and analysis of multiple compounds in rhubarb decoction after processing by wine steaming using UHPLC-Q-TOF-MS coupled with multiple statistical strategies. J. Sep. Sci. 39(15): 3081–3090.
Zhu, Y., Pu, B. -Q., Xie, G. -Y., Tian, M., Xu, F. -Y., and Qin, M. -J. (2014). Dynamic changes of flavonoids contents in the different parts of rhizome of Belamcanda chinensis during the thermal drying process. Molecules 19(7): 10440–10454.
Zwaving, J. (1965). Separation and isolation of anthraquinone glycosides of Rheum palmatum. Planta Med. 13(4): 474–484.