Osteoprotective Effect of Echinocystic Acid, a Triterpone Component from Eclipta prostrata, in Ovariectomy-Induced Osteoporotic Rats

Abstract

Echinocystic acid (EA) is a natural triterpone enriched in various herbs and has been used for medicinal purposes in China. In the present study, we systematically examined the effects of EA on ovariectomy-induced osteoporosis in rats for the first time. Three-month-old female ovariectomy (OVX) Sprague–Dawley rats were used to evaluate the osteoprotective effect of EA. Results showed that administration of EA (5 or 15 mg/kg/day) for 12 weeks prevented lower levels of maximum stress and Young’s modulus of femur induced by OVX. EA also recovered bone metabolic biomarkers levels in OVX rats, including osteocalcin, alkaline phosphatese, deoxypyridinoline, and urinary calcium and phosphorus. EA (5 and 15 mg/kg/day) could prevent the alteration of total bone mineral density in the femur caused by OVX. However, only high dose (15 mg/kg/day) of EA significantly improved trabecular architecture, as evidenced by higher levels of bone volume/tissue volume, trabecula number, and trabecula thickness, and lower levels of trabecula separation and structure model index compared with OVX rats. In addition, EA treatment decresed the serum levels of IL-1β and TNF-α in OVX rats. In conclusion, EA could prevent reduction of bone mass and strength and improve the cancellous bone structure and biochemical properties in OVX rats. Hence, EA may serve as a new candidate or a leading compound for anti-osteoporosis.

The triterpene echinocystic acid and its 3-O-glucoside derivative are revealed as potent and selective glucocorticoid receptor agonists

“…Certain echinocystic acids exert anti-inflammatory, anti-apoptotic, antidepression, osteoprotective and anti-diabetic activities (Kumar et al, 2012;Deng et al, 2015;Yang et al, 2016). The molecular mechanisms of these actions are not clearly defined.…”

“…Apoptotic activities of certain EAs derivatives are attributed to activation of JNK-and p38 kinase-mediated mitochondrial pathways and to regulation of protein expression of proapoptotic and antiapoptotic molecules (Tong et al, 2004a(Tong et al, , 2004bLee et al, 2005, Cho et al, 2016. Recently, the anti-depression, osteoprotective and anti-diabetic activities of EAs have also been proposed (Kumar et al, 2012;Deng et al, 2015;Yang et al, 2016).…”

Validated UPLC‐MS/MS method for quantification of seven compounds in rat plasma and tissues: Application to pharmacokinetic and tissue distribution studies in rats after oral administration of extract of Eclipta prostrata L.

“…The distribution order of the other tissues was as follows: spleen > lung > kidney > heart for ecliptasaponin IV, ecliptasaponin A, apigenin, luteolin and luteolin‐7‐ O ‐glucoside; kidney > spleen > lung > heart for 3′‐hydroxybiochanin A and wedelolactone. In total, all of the analytes could be detected in the selected organs, supporting the possibility that E. prostrata may have various activities (Chung et al, ; Deng et al, ; Lee et al, ; Liu et al, ; Tewtrakul et al, ).…”

“…Modern pharmacological studies have shown that E. prostrata possesses anti‐oxidant, anti‐inflammatory, anti‐proliferative and anti‐tumor effects (Lee et al, ; Liu et al, ; Pukumpuang et al, ; Tewtrakul, Subhadhirasakul, Tansakul, Cheenpracha, & Karalai, ). Chemical studies reveal that it contains various constituents, such as triterpenoid saponins, flavonoids, coumarins, steroids, thiophenes, alkaloids and essential oils (Chung, Rajakumar, Lee, Kim, & Thiruvengadam, ; Deng, Kang, Zhao, Liu, & Zhao, ; Han et al, ; Lee et al, ; Ogunbinu, Flamini, Cioni, Ogunwande, & Okeniyi, ; Pukumpuang et al, ; Tabata, Taniguchi, & Shibano, ; Xi et al, ; Xi, Li, Mi, Wu, & Chen, ; Zhang, Sun, Zhang, & Zhang, ).…”

A brief lightening on medicinal activity and Pharmacological profile of plant Eclipta prostrata: A Review

“…Flowers throughout the year, a quantitative short-day plant abundant seeders. [12] Leaves are inverse, basic, harsh, dull green, praise to elliptical lanceolate, 2-10 cm long, 1-3 cm wide, zenith intense or gruff, base lessen, edge whole or somewhat serrate, pubescent, for the most part sessile, the lower leaves once in a while short-petioled, basally swollen hairs on the two surfaces, veins noticeable. Inflorescence: blossom goes to 1 cm in distance across, a group of sessile white blooms, in upper axils or terminal, lone or two heads together.…”