Small molecules of herbal origin for osteoarthritis treatment: in vitro and in vivo evidence

Abstract

Osteoarthritis (OA) is one of the most common musculoskeletal degenerative diseases and contributes to heavy socioeconomic burden. Current pharmacological and conventional non-pharmacological therapies aim at relieving the symptoms like pain and disability rather than modifying the underlying disease. Surgical treatment and ultimately joint replacement arthroplasty are indicated in advanced stages of OA. Since the underlying mechanisms of OA onset and progression have not been fully elucidated yet, the development of novel therapeutics to prevent, halt, or reverse the disease is laborious. Recently, small molecules of herbal origin have been reported to show potent anti-inflammatory, anti-catabolic, and anabolic effects, implying their potential for treatment of OA. Herein, the molecular mechanisms of these small molecules, their effect on physiological or pathological signaling pathways, the advancement of the extraction methods, and their potential clinical translation based on in vitro and in vivo evidence are comprehensively reviewed.

Emerging Roles of Macrophage Polarization in Osteoarthritis: Mechanisms and Therapeutic Strategies

“…In addition, a number of extractions, including frugoside from Calotropis gigante and quercetin, a naturally occurring flavonoid present in a large variety of fruits and vegetables, have been shown to retard the degradation of cartilage and extracellular matrix as well as chondrocyte hypertrophy by inhibiting M1 polarization or inducing M2 polarization 124,153 . Nevertheless, the translation of herbal substances into clinics has a number of challenges, including potential liver and kidney toxicity, the difficulty of standardization, and the low stability or solubility of tiny molecules in serum or synovial fluid 196,202 . The efficacy of TCM herbs for the treatment of OA patients cannot be adequately evaluated 203 .…”

“…The formulations used in traditional Chinese medicine (TCM) are very intricate and include a wide range of effective substances. 196 It is crucial to separate the components and purify them to create powerful single compounds that can be used to increase medicine efficacy, lessen adverse effects, and study the pharmacological process. As a result, numerous researchers have investigated and analyzed tiny compounds derived from TCM to prevent inflammation and degeneration against OA.…”

In Vitro and In vivo approaches to evaluate Uncaria tomentosa bark extract loaded FDOFs on Osteoarthritis models

“…Calf thymus DNA was used as standard. The measurement was performed according to the protocol of the instrument and DNA concentrations were measured as (µg) [20].…”

Notopterol mitigates IL-1β-triggered pyroptosis by blocking NLRP3 inflammasome via the JAK2/NF-kB/hsa-miR-4282 route in osteoarthritis

“…The role of natural compounds in protecting OA has gained significant attention in recent years. These compounds, derived from various natural sources such as plants, herbs, and fruits, have shown promising potential in mitigating OA progression and providing therapeutic benefits [ 27 , 28 ]. Notopterygium incisum is a species of Notopterygium, a traditional Chinese medicinal plant that is used to make the Juanbi pill, which is used for the treatment of rheumatism in conjunction with other herbs.…”