Molecules
2016,
21(3),
239;
doi:10.3390/molecules21030239
Review
1
Department of Medicinal Chemistry and
Pharmacognosy, College of Pharmacy, The University of Illinois at
Chicago, Chicago, IL 60612, USA
2
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China
3
State Key Laboratory of Quality Research
in Chinese Medicine, Macau Institute for Applied Research in Medicine
and Health, Macau University of Science and Technology, Macau, China
*
Correspondence: Tel.: +1-312-996-5234; Fax: +1-312-996-7107
Academic Editor:
Derek J. McPhee
Received: 9 December 2015 / Accepted: 12 February 2016 / Published: 27 February 2016
Abstract
: Osteoporosis is a progressive, systemic bone disorder characterized by loss of bone mass and microstructure, leading to reduced bone strength and increased risk of fracture. It is often associated with reduced quality of life and other medical complications. The disease is common in the aging population, particularly among postmenopausal women and patients who receive long-term steroidal therapy. Given the rapid growth of the aging population, increasing life expectancy, the prevalence of bone loss, and financial burden to the healthcare system and individuals, demand for new therapeutic agents and nutritional supplements for the management and promotion of bone health is pressing. With the advent of global interest in complementary and alternative medicine and natural products, Chinese medicine serves as a viable source to offer benefits for the improvement and maintenance of bone health. This review summarizes the scientific information obtained from recent literatures on the chemical ingredients of Chinese medicinal plants that have been reported to possess osteoprotective and related properties in cell-based and/or animal models. Some of these natural products (or their derivatives) may become promising leads for development into dietary supplements or therapeutic drugs.
Keywords:
anti-osteoporosis; osteoprotection; bone health; natural product; Chinese medicine1. Introduction
Osteopenia
(low bone density) and osteoporosis (“porous bone”) are progressive
metabolic bone disorders occurring in aging populations, especially
postmenopausal women and patients who undergo long-term steroid therapy.
While postmenopausal women are at greater risk, osteopenia/osteoporosis
can strike at any age of both genders. The disease is characterized by
thinning of bones, with reduction in bone mass and bone mineral density,
as well as micro-architectural deterioration of the bone tissue due to
depletion of calcium and bone protein. The clinical manifestation is
loss of bone strength, thus making the bones fragile and vulnerable to
fractures, which often happens in the hip, spine, and wrist. The disease
is often associated with reduced quality of life and other medical
complications such as disability and depression. Worldwide, osteoporosis
is estimated to affect 200 million women, approximately one-tenth of
women aged 60 and one-fifth of women aged 70 [1].
Although the overall prevalence of fragility fractures is higher in
women, osteoporosis is a significant health issue in men [2].
The U.S. National Osteoporosis Foundation projected that by 2020,
fourteen million Americans over the age of 50 are expected to have
osteoporosis and another 47 million to have low bone mass, accounting
for 55% of the population 50 years of age and older [3].
In
comprehensive bone health management plans, both pharmacologic therapy
and non-pharmacologic measures (such as balanced diet, adequate calcium
and vitamin D intake, exercise and fall prevention) are usually included
[4,5,6].
Currently there are less than ten FDA-approved drugs for osteoporosis
prevention and treatment. They fall into two classes, the
anti-resorptive and the anabolic drugs. Anti-resorptive drugs include
bisphosphonates (alendronate, ibandronate, risedronate, and zoledronic
acid), calcitonin, denosumab (an inhibitor of receptor activator of
nuclear factor-κB ligand [RANKL]), and raloxifene (a selective estrogen
receptor modulator). These compounds slow down the process of bone loss.
On the other hand, anabolic drug such as the recombinant form of
parathyroid hormone (teriparatide) enhances new bone formation [7,8,9].
Nevertheless, the efficacy of these drugs varies in patients and the
long-term safety has posted some concerns; for example, potentially
serious adverse effects of bisphosphonate therapy have been reported [10,11,12,13,14,15]. Only a small number of investigational drugs are currently in the pipeline of development [16,17], and new targets such as c-Src kinase, cathepsin K, and chloride channel are being investigated [18,19,20].
Estrogen
(with or without progesterone) has been used in hormone replacement
therapy. It is effective to increase bone density and reduce the risk of
fracture. Nevertheless, the use of estrogens has been restrained due to
concerns of risk of cancer (such as breast, endometrial and ovarian
cancers), heart attack and stroke [21].
Dietary supplementation of calcium and vitamin D is often included as
part of the treatment plan, yet calcium and vitamin D alone or in
combination are ineffective in reducing fractures in the absence of
pharmacologic agents [22,23].
Given
the rapid growth of the aging population, increasing life expectancy,
the prevalence of bone loss, and financial burden to the healthcare
system and individuals, demand for new therapeutic agents and
nutritional supplements for the management and promotion of bone health
is pressing. With the advent of general interest in alternative medicine
and natural products, Chinese medicine can serve as a viable source to
offer benefits for the improvement and maintenance of bone health. This
review intends to highlight scientific information on
naturally-occurring chemical compounds derived from Chinese medicinal
plants which have been documented to possess protective properties
against osteoporosis or osteonecrosis. Focus has been put on worldwide
literature available in the last ten years. Due to the vast volume of
literature information readily obtainable for the soybean phytoestrogens
(such as daidzein, genistein and equol) [24,25,26,27,28,29,30],
this class of compounds is not included in the present review. In
addition, this review covers only natural molecules derived from Chinese
medicinal plants; and it does not include herbal extracts and medicinal
formulas from which the active compounds are unidentified. Readers are
referred to a number of recent review articles on the topics of
medicinal herbs and/or Chinese medicines for bone disorders and for
maintenance of bone health [31,32,33,34,35,36,37,38,39,40,41,42].
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