Abstract

Osteoporosis is a serious health problem characterized by decreased bone mineral density and deterioration of bone microarchitecture. Current antiosteoporotic agents exhibit a wide range of adverse effects; meanwhile, phytochemicals are effective and safer alternatives. In the current work, nine compounds belonging to hydroxyphenylalkane and diarylheptanoid groups were isolated from Aframomum meleguea seeds and identified as 6-gingerol (1), 6-paradol (2), 8-dehydrogingerdione (3), 8-gingerol (4), dihydro-6-paradol (5), dihydrogingerenone A (6), dihydrogingerenone C (7), 1,7-bis(3,4-dihydroxy-5-methoxyphenyl)heptane-3,5-diyl diacetate (8), and 1-(3,4-dihydroxy-5-methoxyphenyl)-7-(3,4-dihydroxyphenyl)heptane-3,5-diyl diacetate (9). The structures of isolated compounds were established by NMR and mass spectral data, in addition to referring to literature data. Exposure of MCF-7, MG-63, and SAOS-2 cells to subcytotoxic concentrations of the compounds under investigation resulted in accelerated proliferation. Among them, paradol was selected for further detailed biochemical analysis in SAOS-2 cells. DNA flowcytometric analysis of cell cycle distribution revealed that paradol did not induce any significant change in the proliferation index of SAOS-2 cells. Assessment of osteogenic gene expression revealed that paradol enhanced the expression of osteocyte and osteoblast-related genes and inhibited osteoclast and RUNX suppressor genes. Biochemically, paradol enhanced alkaline phosphatase activity and vitamin D content and decreased the osteoporotic marker acid phosphatase. In conclusion, paradol, which is a major constituents of A. melegueta seeds, exhibited potent proliferative and ossification characteristics in bone cells.

Highlights

  • Osteoporosis is a serious health problem that affects more than 200 million people worldwide [1].Osteoporosis is characterized by a decrease in bone mineral density (BMD) and the deterioration of bone microarchitecture

  • Current antiosteoporotic agents health are not problem devoid of adverse effects, which range from gastrointestinal burden

  • Current antiosteoporotic agents are not devoid of adverse effects, which range from irritation to carcinogenesis [7,29]

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Summary

Introduction

Osteoporosis is a serious health problem that affects more than 200 million people worldwide [1]. Osteoporosis is characterized by a decrease in bone mineral density (BMD) and the deterioration of bone microarchitecture. It affects postmenopausal women, leading to a significant loss of bone mineralized mass and leading to increased bone fragility and susceptibility to fracture [2]. The disease is sometimes described as a “silent disease”, as it is usually asymptomatic until a fracture ensues [3]. It causes significant morbidity, mortality, and a socioeconomic burden. Post-menopausal women are at a high risk, especially with the adoption of the Western sedentary lifestyle [5]

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