Abstract

Blainvillea acmella (L.) Philipson [Asteraceae] (B. acmella) is an important medicinal plant native to Brazil, and it is widely known as a toothache plant. A plethora of studies have demonstrated the antioxidant activities of B. acmella and few studies on the stimulatory effects on alkaline phosphatase (ALP) secretion from bone cells; however, there is no study on its antioxidant and anabolic activity on bone cells. The study aimed to evaluate the phytochemical contents of aqueous and ethanol extracts of B. acmella using gas chromatography mass spectrometry (GCMS) and liquid chromatography time of flight mass spectrometry (LCTOFMS) along with the total phenolic (TPC) and flavonoid (TFC) contents using Folin-Ciocalteu and aluminum colorimetric methods. The extracts of B. acmella leaves were used to scavenge synthetic-free radicals such as 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. The bone anabolic effects of B. acmella extracts on MC3T3-E1 cells were measured with 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazoium bromide (MTT) at 1, 3, 5, and 7 days, Sirius-red and ALP at 7 and 14 days, and Alizarin Red S at 14 and 21 days. Comparatively, ethanol extract of B. acmella (BaE) contributed higher antioxidant activities (IC50 of 476.71 µg/ml and 56.01 ± 6.46 mg L-ascorbic acid/g against DPPH and FRAP, respectively). Anabolic activities in bone proliferation, differentiation, and mineralization were also higher in B. acmella of ethanol (BaE) than aqueous (BaA) extracts. Positive correlations were observed between phenolic content (TPC and TFC) to antioxidant (ABTS and FRAP) and anabolic activities. Conversely, negative correlations were present between phenolic content to antioxidant (DPPH) activity. These potential antioxidant and bone anabolic activities in BaE might be due to the phytochemicals confirmed through GCMS and LCTOFMS, revealed that terpenoids of α-cubebene, cryophyllene, cryophyllene oxide, phytol and flavonoids of pinostrobin and apigenin were the compounds contributing to both antioxidant and anabolic effects in BaE. Thus, B. acmella may be a valuable antioxidant and anti-osteoporosis agent. Further study is needed to isolate, characterize and elucidate the underlying mechanisms responsible for the antioxidant and bone anabolic effects.

Highlights

  • According to the World Health Organization (WHO) Global Atlas of Traditional, Complementary, and Alternative Medicine (Bodeker et al, 2005), traditional medicine has been used widely by the world population to treat diseases

  • These findings indicated that the osteoprotective effect of B. acmella extracts were via amplification of osteoblast proliferation

  • These results revealed that 2.93 μg/ml was the most compatible concentration of B. acmella followed by others B. acmella (BaE_23.44, BaA_5.86 and BaA_11.72) to provoke a significant proliferation of MC3T3-E1 cells compared to control

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Summary

Introduction

According to the World Health Organization (WHO) Global Atlas of Traditional, Complementary, and Alternative Medicine (Bodeker et al, 2005), traditional medicine has been used widely by the world population to treat diseases. 70–95% of the population in the developing world uses traditional medicine as primary care (Robinson and Zhang, 2011). The use of medicinal plants or isolated active compounds from plants has gained attention due to their perceived lower toxicity. Reactive oxygen species (ROS) may inhibit the function of osteoblast cells in bone formation. This would lead to imbalances between bone formation and bone resorption, contributing to osteoporosis (Domazetovic et al, 2017). Current treatments such as calcitonin, estrogen, and bisphosphonates are anti-bone resorptive drugs that inhibit osteoclast activity (Yang et al, 2018). Long-term use of these treatments is associated with several side effects, such as cancer, femur fractures, osteonecrosis of the jaw, myocardial infarction, thromboembolic events, and skin reaction (DRESS syndrome) (Khosla and Hofbauer, 2017; Pherwani and Sathaye, 2020)

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