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Herbal Drug Discovery Against Inflammation: From Traditional Wisdom to Modern Therapeutics
Published in Amit Baran Sharangi, K. V. Peter, Medicinal Plants, 2023
Shalini Dixit, Karuna Shanker, Madhumita Srivastava, Priyanka Maurya, Nupur Srivastava, Jyotshna, Dnyaneshwar U. Bawankule
The isolation of salicin derivatives from the twigs of Salix glandulosa Seemen (Figure 3.9) is reported for their NO inhibitory efficacy in lipo-polysaccharide (LPS)-activated microglial cell (BV-2). The results show that salicin derivatives from Salix glandulosa might have potent effect as anti-neuroinflammatory agents (Kim et al., 2015). Salicin derivatives (1–14) where A, B, C, D are H, Ac, benzoyl, etc., groups.
Nonopioid and Adjuvant Analgesic Agents
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
The analgesic and anti-inflammatory properties of the bark of the willow and other plants have been known for centuries. The active ingredient in willow bark is salicin, and it was first described in the nineteenth century (Wick, 2012). Subsequently, the chemist Hoffmann, trying to improve the gastric tolerability of salicylic acid for his father, synthesized acetylsalicylic acid, the well-known aspirin. Aspirin became the prototype NSAID, and attempts to improve on this compound resulted in the many different NSAIDs now available worldwide.
The Americas
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
Viburnum opulus, cramp bark, or guelder rose, and the related V. prunifolium, contain scopoletin, a coumarin which has a sedative effect on the uterus. Useful for dysmenorrhea and threatened miscarriage, Viburnum was listed in all the major pharmacopoeias in the early pan of this century (Squire, 1908) and remained in the American National Formulary until 1960. V. prunifolium contains salicin which also occurs in the willow, Salix alba, and from which salicylic acid was derived. Both salicin and salicylic acid are analgesic chemicals and were first synthetically prepared in 1852, but were found to cause marked gastric irritation. In 1899 the Bayer Company produced acetylsalicylic acid, known better by its proprietary name, aspirin (Griggs, 1997).
Vascular protection of salicin on IL-1β-induced endothelial inflammatory response and damages in retinal endothelial cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Yu Song, Xia Tian, Xuehong Wang, Hui Feng
Willow bark is a commonly used traditional medicine. Known for its alleviating effect on fever, pain, and inflammation, willow bark has been referred to as “nature’s Aspirin.” In preclinical and clinical studies, willow bark has been reported to be effective in pain management and anti-inflammation [8,9]. Salicin is the major component of willow bark extract. Salicin is metabolized to salicylic acid in vivo and then plays a major role in anti-inflammatory and anti-analgesic effects. For example, it has been recently reported that salicin displays an anti-inflammatory effect against lipopolysaccharides (LPS) in RAW264.7 cells in mouse models by suppressing the expression of pro-inflammatory cytokines such as TNF-α, IL-1β, IL-6, and IL-10 and the activation of NF-κB [10]. Another study reported that administration of salicin could ameliorate inflammatory response, suppress edema and mucosal damage in a dextran sulfate sodium (DSS)-induced colitis in mouse models [11]. We have been motivated by willow bark’s healing effects and previous studies to investigate whether salicin plays a beneficial role in retinal vascular cells. In this study, we applied salicin to cultured retinal endothelial cells and revealed its protective role and the molecular mechanism involved.
Salicin prevents TNF-α-induced cellular senescence in human umbilical vein endothelial cells (HUVECs)
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Salicin is a plant-based derivative that can be found in willow bark or in the stems and roots of Alangium chinense, an east and southeast Asian shrub [10,11]. It is a precursor to acetylsalicylic acid and has documented anti-inflammatory properties [12], including an inhibitory effect on TNF-α [13]. Whereas TNF-α inhibitors are typically administered via injection, salicin is ingested [14] and has no noted serious side effects [15,16], fewer even than its synthetic counterpart, aspirin, and other non-steroidal anti-inflammatory drugs (NSAIDs), all of which can damage the gastrointestinal mucosa [17].
Salicin inhibits AGE-induced degradation of type II collagen and aggrecan in human SW1353 chondrocytes: therapeutic potential in osteoarthritis
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Salicin is a prodrug of acetylsalicylic acid, a main constituent of aspirin and can be derived from the stems and roots of Alangium chinense (Lour.) Harms. (Alangiaceae), a common evergreen shrub native to east and southeast Asia [1]. Alangium chinense has long been used in traditional Chinese medicine (TCM) to treat rheumatic disease, snake bites, circulatory issues, hemostasis, and toxicity, it is also used as a contraceptive or analgesic and to promote wound healing [2,3]. Records of the use of willow bark, another common source of salicylic acid, have been found dating back to the 3rd century B.C. [4]. Numerous substances can be derived from the rhizome, roots, stems, leaves, or flowers of Alangium chinense such as alkaloids, sugars, saponins, steroids, triterpenes, anthraquinones, and glycosides including salicin [2,5,6] Recently, research has focused on methods of extraction of salicin and its potential therapeutic applications [6–8] As a prodrug, salicin is hydrolyzed to salicyl alcohol and then oxidized to salicylic acid in the gut [9]. As a metabolite of salicin, salicylic acid inhibits the activity of cyclo-oxygenase (COX), which plays a major role in regulating pain, fever, and inflammation by metabolizing arachidonic acid, a prostaglandin precursor [10]. However, to the best of our knowledge, this is the first time that the potential effects of salicin have been explored in osteoarthritis (OA). OA is characterized by chronic inflammation and irreversible cartilage destruction, which takes a massive toll on patients’ quality of life and mobility. The main risk factor for OA is age, in part due to the accumulation of advanced glycation end-products (AGEs). AGEs came to exist in the body as a byproduct of the innate process of non-enzymatic glycation as well as via dietary intake, as AGEs are used as a food preservative owing to their high resilience to degradation [11,12]. Some of the factors involved in the development and progression of OA include oxidative stress, secretion of proinflammatory cytokines, recruitment of immune cells, degradation of cartilage and activation of proinflammatory signaling pathways, all of which are demonstrated to be triggered by exposure to AGEs.