The Hedyotis diffusa Willd. (Rubiaceae): A Review on Phytochemistry, Pharmacology, Quality Control and Pharmacokinetics

Abstract

Hedyotis diffusa Willd (H. diffusa) is a well-known Chinese medicine with a variety of activities, especially its anti-cancer effect in the clinic. Up to now, 171 compounds have been reported from H. diffusa, including 32 iridoids, 26 flavonoids, 24 anthraquinones, 26 phenolics and their derivatives, 50 volatile oils and 13 miscellaneous compounds. In vitro and in vivo studies show these phytochemicals and plant extracts to exhibit a range of pharmacological activities of anti-cancer, antioxidant, anti-inflammatory, anti-fibroblast, immunomodulatory and neuroprotective effects. Although a series of methods have been established for the quality control of H. diffusa, a feasible and reliable approach is still needed in consideration of its botanical origin, collecting time and bioactive effects. Meanwhile, more pharmacokinetics researches are needed to illustrate the characteristics of H. diffusa in vivo. The present review aims to provide up-to-date and comprehensive information on the phytochemistry, pharmacology, quality control and pharmacokinetic characteristics of H. diffusa for its clinical use and further development.

Scandoside Exerts Anti-Inflammatory Effect via Suppressing NF-κB and MAPK Signaling Pathways in LPS-Induced RAW 264.7 Macrophages

“…Traditionally, it is used for the treatment of bronchitis, arthritis, rheumatism, urethral infection, appendicitis, sore throat, contusions, ulcerations and extension of malignancies [10]. Modern pharmacological studies have proved that H. diffusa have multiple effects, such as anti-inflammatory, anti-cancer, immunemodulating, neuroprotective and hepatoprotective activities [11]. It was found that the iridoid compounds possibly attributed to anti-inflammatory effect of H. diffusa [12][13].…”

The Antitumor Constituents from Hedyotis Diffusa Willd

“…The components of iridoids, triterpenes, flavonoids, lignans, anthraquinones, alkaloids, cerebrosides, coumarins, and sterols were discovered during the chemical studies of H. diffusa Willd. [ 2 , 6 , 7 , 8 ]. There are some differences of the chemical constituents if the H. diffusa Willd.…”

“…These include 2,7-dihydroxy-3-methyl anthraquinone, 2-hydroxy-3-methyl-1-methoxy anthraquinone, 2-hydroxy-3-methoxy-7-methoxy anthraquinone, 2-methyl-3-hydroxy anthraquinone, 2-methyl-3-hydroxy-4-methoxy anthraquinone, deacetyl asperulosidic acid, scandoside, E -6- O - p -coumaroyl scandoside methyl ester [ 9 ]. Various hepatoprotective, immunoloregulation, anti-tumor, anti-inflammatory, antibacterial, analgesia, sedative, and anti-oxidant activities can be found in pharmacological studies of H. diffusa Willd [ 3 , 6 , 10 , 11 , 12 , 13 ], but more studies found that the extracts from H. diffusa Willd. possessed evident anticancer activities [ 1 , 2 , 14 , 15 , 16 , 17 , 18 , 19 , 20 ].…”

An update on Chinese herbal medicines as adjuvant treatment of anticancer therapeutics

“…Recently, Hedyotis diffusa willd and some of its active constituents have gained increasing attention as an antitumor herb. Clinically, this herb has often been applied as a critical element in many TCM formulae for the treatment of various cancers, including gastric cancer (GC) and colorectal cancer (61)(62)(63)(64). A latest retrospective matched-cohort study presented that Hedyotis diffusa willd was the most commonly prescribed single herb for treating GC patients and complementary TCM therapy enhanced the overall survival of patients with GC in Taiwan (62).…”

“…A latest retrospective matched-cohort study presented that Hedyotis diffusa willd was the most commonly prescribed single herb for treating GC patients and complementary TCM therapy enhanced the overall survival of patients with GC in Taiwan (62). It probably produced the therapeutic effects against GC by synergistically regulating many biological pathways, such as nucleotide excision repair, apoptosis, cell cycle, PI3K/AKT/mTOR signaling pathway, VEGF signaling pathway, and Ras signaling pathway (61). Hedyotis diffusa willd could suppress colorectal cancer growth through multiple cellular pathways including MAPK, STAT3, AKT and ERK signaling (63).…”