Inhibition of Trypsin and Chymotrypsin by Anti-Inflammatory Triterpenoids from Compositae Flowers

Rajic, Antonio; Akihisa, Toshihiro; Ukiya, Motohiko; Yasukawa, Ken; Sandeman, R.M.; Chandler, David; Polya, Gideon M.

doi:10.1055/s-2001-17350

Cited by 35 publications

(23 citation statements)

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“…Future studies should examine the efficacy of a,bamyrin in mitigating pancreatic pain in animal models of acute pancreatitis. Many plant-derived anti-inflammatory triterpenoids, including oleanone and ursane derivatives, have been previously described to act as competitive and non-competitive inhibitors of the serine proteases trypsin and chymotrypsin, which have a key role in the development of acute pancreatitis [46,47]. Such an antiprotease effect of a,b-amyrin is quite likely, due to its structural resemblance to ursane and oleanone series of triterpenes.…”

Section: Discussionmentioning

confidence: 99%

Anti-inflammatory effect of α,β-amyrin, a triterpene from Protium heptaphyllum, on cerulein-induced acute pancreatitis in mice

et al. 2011

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Section: Discussionmentioning

confidence: 99%

Anti-inflammatory effect of α,β-amyrin, a triterpene from Protium heptaphyllum, on cerulein-induced acute pancreatitis in mice

et al. 2011

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“…Chrysanthemum is an important medicinal plant that has various pharmacological effects. Among other things, it functions as an antibacterial, anti-inflammatory, vasodilatory, and antitumor agent, as well as reducing blood pressure and acting as an antioxidant [21]. Teas made from the buds of the camellia plant contain many bioactive compounds, including polyphenols, tea polysaccharides, alkaloids, vitamins, and amino acids, as well as various essential metal ions.…”

Section: Introductionmentioning

confidence: 99%

Clearance of Free Silica in Rat Lungs by Spraying with Chinese Herbal Kombucha

ChangHui

et al. 2013

Evidence-Based Complementary and Alternative Medicine

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The effects of spraying with kombucha and Chinese herbal kombucha were compared with treatments with tetrandrine in a rat silicosis model. Silica dust (50 mg) was injected into the lungs of rats, which were then treated with one of the experimental treatments for a month. The rats were then killed and the effects of the treatments were evaluated by examining the extent and severity of the histopathological lesions in the animals' lungs, measuring their organ coefficients and lung collagen contents, determining the dry and wet weights of their lungs, and measuring the free silica content of the dried lungs. In addition, lavage was performed on whole lungs taken from selected rats, and the numbers and types of cells in the lavage fluid were counted. The most effective treatment in terms of the ability to reduce lung collagen content and minimize the formation of pulmonary histopathological lesions was tetrandrine treatment, followed by Chinese herbal kombucha and non-Chinese herbal kombucha. However, the lavage fluid cell counts indicated that tetrandrine treatment had severe adverse effects on macrophage viability. This effect was much less pronounced for the kombucha and Chinese herbal kombucha treatments. Moreover, the free silica levels in the lungs of animals treated with Chinese herbal kombucha were significantly lower than those for any other silica-exposed group. These preliminary results indicate that spraying with Chinese herbal kombucha preparations can effectively promote the discharge of silica dust from lung tissues. Chinese herbal kombucha inhalation may thus be a useful new treatment for silicosis and other pneumoconiosis diseases.

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“…The side-chain double bond has also a great effect on anti-inflammatory activity 19) : most of active tirucallane triterpenoids reported had this characteristic. [17][18][19][20][21][23][24][25] Therefore, compounds 3 and 7, not surprisingly, had good anti-inflammatory activity.…”

Section: Resultsmentioning

confidence: 99%

“…3,[15][16][17][18] In recent years, there have been ever increasing reports concerning the anti-inflammatory activity of tirucallane triterpenoids. [19][20][21][22][23][24][25][26] Herein, we reported the evaluation of the anti-inflammatory activity of a series of tirucallane triterpenoids isolated from the stem barks of Aphanamixis grandifolia and their structure and activity relationship (SAR).…”

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Relationship of Chemical Structure to <i>in Vitro</i> Anti-inflammatory Activity of Tirucallane Triterpenoids from the Stem Barks of <i>Aphanamixis grandifolia</i>

Guo

Wang

Zhang

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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A series of tirucallane triterpenoids isolated from the stem barks of Aphanamixis grandifolia were assessed for their anti-inflammatory activity, exhibiting from weak to strong anti-inflammatory activity, by testing their inhibitory effects on nitric oxide (NO) production and tumor necrosis factor-α (TNF-α) level in lipopolysaccharide (LPS) induced RAW264.7 murine macrophages. To explore the relationship between the structures and anti-inflammatory activity, a vast pool of molecular descriptors for each isolate were calculated. Genetic algorithms (GA) or simulated annealing (SA) based partial least squares (GA-PLS and SA-PLS) algorithms identified some important descriptor combinations, which were correlated with both sets of the anti-inflammatory data by partial least squares 2 (PLS2) method. S-Plot was used to visualize the descriptor influence in the PLS2 model, disclosed five most important molecular descriptors, nOHt, RDF150m, lip_vio-lation, Mor32m and JhetZ.Key words Aphanamixis grandifolia; tirucallane triterpenoid; anti-inflammatory activity; nitric oxide; tumor necrosis factor-α; structure-activity relationship Inflammation is a normal and crucial response of the organism to various stimuli including physical damage, ultra violet irradiation, microbial invasion and immune reactions, playing a pivotal role in host defense.1,2) While inflammatory cascades may cause pain, tissue damage, and a wide range of human acute and chronic inflammatory diseases, such as chronic asthma, rheumatoid arthritis and multiple sclerosis, and psoriasis.3) Many of these diseases with increasing incidence rate are particularly debilitating to the patient's functional capacity and quality of life.Macrophages have vital functions in maintaining body homeostasis, as well as in inflammatory processes, which are endowed with the ability to release a variety of mediators including the free radical nitric oxide (NO), 4) one of the most versatile regulator in the immune system. 5) Overproduction of NO can exacerbate inflammation, playing an important role in the pathogenesis of several chronic and systemic inflammation diseases, such as rheumatoid arthritis. 6,7)Tumor necrosis factor-α (TNF-α), one of the most important pro-inflammatory cytokines, is also massively produced by the activated macrophages and monocytes at local sites of inflammation.8) Its excessive production further triggers the secretion of other inflammatory cytokines such as interleukin-1β (IL-1β), interleukin-6 (IL-6) and granulocyte-macrophage colony-stimulating factor (GM-CSF) and thereby aggravates the inflammation in many autoimmune/inflammatory diseases. 9-11)Exposure to major anti-inflammatory agents, such as corticosteroids, non-steroidal anti-inflammatory drugs (NSAIDs), is known to increase substantially the risk of serious side effects.3,12) Therefore, there is an unmet medical need for new treatment strategies, which could be possibly filled by rational phytopharmaceuticals with a favorable benefit/risk ratio. Recent investigations into the anti-inflamm...

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Inhibition of Trypsin and Chymotrypsin by Anti-Inflammatory Triterpenoids from Compositae Flowers

Cited by 35 publications

References 0 publications

Anti-inflammatory effect of α,β-amyrin, a triterpene from Protium heptaphyllum, on cerulein-induced acute pancreatitis in mice

Anti-inflammatory effect of α,β-amyrin, a triterpene from Protium heptaphyllum, on cerulein-induced acute pancreatitis in mice

Clearance of Free Silica in Rat Lungs by Spraying with Chinese Herbal Kombucha

Relationship of Chemical Structure to <i>in Vitro</i> Anti-inflammatory Activity of Tirucallane Triterpenoids from the Stem Barks of <i>Aphanamixis grandifolia</i>

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