Efficacy and Safety of Echinacoside in a Rat Osteopenia Model

Abstract

This study aimed to investigate the efficacy and safety of echinacoside (ECH) using an osteopenia rat model. Forty-eight 6-month-old female Sprague-Dawley rats were randomly divided into one sham-operated group (SHAM) and five OVX (ovariectomized) subgroups: SHAM with vehicle 0.5% carboxymethylcellulose sodium (0.5% CMC-Na) and OVX with vehicle (OVX), OVX with 17β-estradiol (E2), and OVX with ECH of graded doses (ECH-L, ECH-M, and ECH-H). The effects of ECH and E2 on serum biochemical parameters, bone mineral density (BMD), bone biomechanical properties, bone microarchitecture, and immunohistochemistry were examined, and safety assessments were also evaluated. The results showed that ECH treatments improved total femur BMD, bone microarchitecture, and biomechanical properties and decreased serum marker levels in comparison to OVX group. Moreover, ECH administration significantly increased osteoprotegerin (OPG) level, and decreased receptor activator of nuclear factor-κB ligand (RANKL) level in serum, as well as in proximal femur. Importantly, ECH treatment ameliorated the lipid parameters without the overall incidences of adverse events of uterus and mammary gland compared to OVX and SHAM groups. This study demonstrated that administration of ECH for 12 weeks can effectively and safely prevent OVX-induced osteoporosis in rats via increasing the OPG/RANKL ratio.

Echinacoside induces rat pulmonary artery vasorelaxation by opening the NO-cGMP-PKG-BKCa channels and reducing intracellular Ca2+ levels

“…Lagotis brevituba Maxim is a species of Lagotis spp belonging to the Scrophulariaceae and grows widely at an altitude over 3000 meter in the Qinghai-Tibet Plateau. ECH has various desirable pharmacological characteristics, such as antioxidative, anti-inflammatory, neuroprotective, hepatoprotective, and nitric oxide (NO) radical-scavenging properties [6] . It can also elicit endothelium-dependent relaxation in rat thoracic aortic rings and cure cardiovascular diseases [7] .…”

Therapeutic potential of phenylethanoid glycosides: A systematic review

“…166 Compared to OVX group, 270 mg/kg/day echinacoside treatment caused the highest levels of OPG and OPG/RANKL ratios (150.14% and 197.64%). 166 After 12 weeks' daily orally administration of echinacoside (30, 90, 270 mg/kg/day) in OVX rats, the urine concentration of calcium, inorganic phosphorus, and hydroxyproline was increased by 92.23%, 66.67%, and 36.41%, respectively, in 270 mg/kg/day group. 167 Cistanoside A (po, 20, 40, and 80 mg/kg/day for 12 weeks) was found to promote bone formation and prevent bone resorption in OVX rats by downregulating TRAF6, coordinating the inhibition of NF-kB pathway and stimulating PI3K/Akt pathway.…”

Echinacoside Induces Apoptosis in Human SW480 Colorectal Cancer Cells by Induction of Oxidative DNA Damages

“…It is a hydrophilic polyphenol glycoside consisting of a phenylpropanoid and a phenylethanoid glycosidically linked to a trisaccharide moiety ( Figure 1 A). Many biological effects have been ascribed to Echinacoside, including neuroprotection [ 5 ], hepatoprotection [ 6 ], anti-apoptosis [ 7 ], anti-senescence [ 8 ], immunomodulation [ 9 ], aperient [ 10 ], anti-diabetes [ 11 ] and promotion of bone formation [ 12 ], but detailed molecular mechanisms behind these effects remain unclear. Perhaps the most extensively studied and accepted bioactivity of Echinacoside is its anti-oxidative and reactive oxygen species (ROS)-scavenging function [ 13 , 14 ], which may also explain its neuroprotective and anti-aging effects.…”