Rehmanniae Radix in osteoporosis: A review of traditional Chinese medicinal uses, phytochemistry, pharmacokinetics and pharmacology. (23rd February 2017)

• Record Type: Journal Article
• Authors: Liu, Chenyue; Ma, Rufeng; Wang, Lili; Zhu, Ruyuan; Liu, Haixia; Guo, Yubo; Zhao, Baosheng; Zhao, Shangang; Tang, Jinfa; Li, Yu; Niu, Jianzhao; Fu, Min; Zhang, Dongwei; Gao, Sihua
• Is Part Of: Journal of ethnopharmacology. Volume 198(2017)
• Page Start: 351
• Page End: 362
• Publication Date: 2017-02-23
• Subjects: ALP alkalinephosphatase -- BBB blood–brain barrier -- BMC bone mineral content -- BMD bone mineral density -- BW body weight -- CKD chronic kidney disease -- Col collagen -- CSF cerebrospinal fluid -- CT calcitonin -- DREE dried Rehmanniae Radix alcohol extraction refluxing extracted by 95% ethanol -- DREW dried Rehmanniae Radix by aqueous extracted -- E2 estradiol -- FREE fresh Rehmanniae Radix alcohol extraction refluxing extracted by 95% ethanol -- FREW fresh Rehmanniae Radix by aqueous extracted -- p.o. gavage -- H/C hydroxyproline/creatinine -- IL interleukin -- i.m. intramuscular administration -- Itg β1 integrin beta 1 -- i.v. intravenous injection -- NRS numerical rating scale -- OC osteocalcin -- OPG osteoprotegerin -- OPN osteopontin -- OVX ovariectomized -- PPRE peroxisome proliferator response element -- PTH parathyroid hormone -- RANKL receptor activator of nuclear factor kappa-B ligand -- Runx2 Runt-related transcription factor 2 -- TCM traditional Chinese medicine -- TRAP tartrate-resistant acid phosphatase -- UHP urine hydroxyproline -- VAS visual analogue scale; Catalpol, CID 91520 -- Rehmannioside A, CID 78407230 -- Rehmannioside B, CID 101654196 -- Rehmannioside C, CID 101654197 -- Rehmaionoside A, CID 10023290 -- Rehmaionoside B, CID 10430488 -- Rehmaionoside C, CID 11740990 -- Rehmaglutin A, CID 5320903 -- Rehmaglutin B, CID 14413769 -- Rehmaglutin D, CID 5320906 -- Rehmaglutin C, CID 21637649 -- Ajugol, CID 6325127 -- Rehmannioside D, CID 92044472 -- and geniposide, CID 107848 -- Gentisic acid, CID 3469 -- Versulin, CID 5280443 -- Oleanolic acid, CID 10494; Rehmanniae Radix -- Osteoporosis -- Clinical trial -- Phytochemistry -- Pharmacokinetics -- Pharmacology; Ethnopharmacology -- Periodicals; Pharmacognosy -- Periodicals; Herbs -- Periodicals; Herbs -- Periodicals; Pharmacognosy -- Periodicals; Pharmacognosie -- Périodiques; Herbes -- Périodiques; 615.1
• DOI: 10.1016/j.jep.2017.01.021
• Languages: English
• ISSNs: 0378-8741

Abstract

Abstract: Ethnopharmacological relevance: Emerging clinical usage and pharmacological effects have been achieved in using Rehmanniae Radix either singly or in combination with other herbs to treat skeletal diseases in traditional Chinese medicine (TCM) in the recent years. This study is aimed to provide a comprehensive review about the historical TCM interpretation of the action of Rehmanniae Radix in osteoporosis, its usage in clinical trials and osteoporotic models, its main phytochemical constituents, and its pharmacokinetics. Materials and methods: Several databases included PubMed, China Knowledge Resource Integrated Database, China Science and Technology Journal Database, National Science and Technology Library and the Web of Science Database were consulted to locate the publications pertaining to Rehmanniae Radix . The initial inquiry was conducted for the presence of the following terms combinations in the abstracts: Rehmanniae Radix, Dihuang, phytochemistry, pharmacokinetics, osteoporosis, bone, osteoclast and osteoblast. About 330 research papers and reviews were consulted. Results: In TCM, Rehmanniae Radix exerts the anti-osteoporotic effect via regulating the functions of kidney and liver as well as improving blood circulation. 107 clinical trials are identified that used Rehmanniae Radix in combination with other herbs to treat post-menopausal, senile and secondary osteoporosis. Most of the clinical trials are characterized by high efficacy and no obvious adverse effects. However, the efficacies of these clinical trials are limited because of small patient sample size, short treatment duration and poor clinical design. In addition, TCM herbs under the clinical study are not clear because of a lack of standardization and authentication. The pharmacokinetics data demonstrate that the ingredients of Rehmanniae Radix are widely distributed after administration, and that catalpol and ajugol as well as acetoside are supposed to be the active constituents. More than 140 individual compounds have been currently isolated from this plant and reported to show pleiotropic effects on various diseases. Rehmanniae Radix displays bone protecting features in the osteoporosis models via the delicate balance between osteoclastogenesis and osteoblastogenesis through single herb extracts and its isolated compounds. Conclusions: The successful inclusion of Rehmanniae Radix in clinical trials and preclinical studies for the management of osteoporosis has attracted rising attentions for identifying potential anti-osteoporotic candidates from this plant and clinical existing TCM formulas, which will further speed up anti-osteoporosis drug discovery processes. Properly designed and well controlled prospective studies are still needed to further demonstrate bone protective actions and safe use of this herb and its ingredients Graphical abstract: