Botany, traditional use, phytochemistry, pharmacology and toxicology of Sigesbeckiae Herba (Xixiancao): a review Hong Xun Tao . Guan Ding Zhao . Ke Gang Linghu . Wei Xiong . Wei Sang . Yu Peng . Yitao Wang . Hua Yu Received: 28 February 2019 / Accepted: 6 January 2020 Ó Springer Nature B.V. 2020 Abstract Sigesbeckiae Herba is a traditional Chi- nese herbal medicine and has been used for inflam- matory diseases with a long history. The current official plant origins of Sigesbeckiae Herba include Sigesbeckia orientalis L. (SO), S. pubescens Markino (SP) and S. glabrescens Markino (SG). In this work, a systemic review about the scientific work for medic- inal Sigesbeckiae Herba regarding their botanical descriptions, reported bioactive components, pharma- cological activities and toxicities was performed. The results indicate that a total of 251 compounds includ- ing flavonoids, diterpenoids, sesquiterpenoids, triter- penoids, and sterols have been isolated from Sigesbeckia plants and reported to be characteristically distributed in SO, SP and SG. The extracts and pure compounds derived from Sigesbeck- iae Herba are reported to present various pharmaco- logical activities including anti-inflammation, immunomodulation, anti-cancer, and others. Although no significant side-effects and toxicities for Siges- beckiae Herba have been reported in clinics, the potential pulmonary toxicity for the water extracts of SH are reported in experimental animals. In conclu- sion, Sigesbeckiae Herba is a valuable Chinese herbal medicine and has been investigated to present multiple pharmacological activities. The main pharmacological investigations support its traditional use for treating chronic inflammatory diseases. The available litera- ture shows that much of the activity of Sigesbeckiae Herba can be attributed to diterpenoids, sesquiter- penoids and flavonoids. However, further investiga- tions on the molecular mechanisms to pharmacological activities and the potential toxicities is recommended. Moreover, further investigations on the comparative comprehension among the three medicinal Sigesbeckia plants (SO, SP and SG) both in chemistry and pharmacology are also recommended for their precise applications in clinics. Keywords Sigesbeckiae Herba Á Traditional use Á Phytochemistry Á Pharmacology Á Toxicology Electronic supplementary material The online version of this article (https://doi.org/10.1007/s11101-020-09714-4) con- tains supplementary material, which is available to authorized users. H. X. Tao Á G. D. Zhao Á K. G. Linghu Á W. Xiong Á W. Sang Á Y. Peng Á Y. Wang Á H. Yu (&) Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Macao, SAR, China e-mail: yuhuayu@vip.sina.com H. Yu HKBU Shenzhen Research Center, Shenzhen, Guangdong, China H. Yu School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong SAR, China 123 Phytochem Rev https://doi.org/10.1007/s11101-020-09714-4