Advances on the Anti-inflammatory Activity of Oleanolic Acid and Derivatives

: Oleanolic acid can inhibit edema and exhibit obvious inhibitory activity to inflammatory by activating of the pituitary-adrenal cortical system, inhibiting the synthesis or release of PGs, inhibiting endotoxin-mediated release of HMGB1 by endothelial cells or regulating MAPK, PI3K/Akt/NF-κB/ICAM-1/JAK/STAT signaling pathways, etc. In recent years, an increased number of interesting research work has been carried out on the anti-inflammatory activity and mechanisms of OA derivatives, such as acyloxyimino derivative, 3-acetylated derivatives, novel 3,5-disubstituted isoxazoles derivatives, acetate, ester derivatives and oximes derivatives. The review summaries and highlights the update advances on the anti-inflammatory activity and mechanism of OA and its derivatives.

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Sparassis crispa exerts anti-inflammatory activity via suppression of TLR-mediated NF-κB and MAPK signaling pathways in LPS-induced RAW264.7 macrophage cells

Journal of Ethnopharmacology ◽

10.1016/j.jep.2018.11.003 ◽

2019 ◽

Vol 231 ◽

pp. 10-18 ◽

Cited By ~ 17

Author(s):

Jang Mi Han ◽

Eun Kyeong Lee ◽

So Youn Gong ◽

Jae Kyung Sohng ◽

Yue Jai Kang ◽

...

Keyword(s):

Signaling Pathways ◽

Mapk Signaling ◽

Inflammatory Activity ◽

Macrophage Cells ◽

Sparassis Crispa ◽

Anti Inflammatory ◽

Raw264.7 Macrophage ◽

Mapk Signaling Pathways

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Anti-inflammatory activity of Eupatorium perfoliatum L. extracts, eupafolin, and dimeric guaianolide via iNOS inhibitory activity and modulation of inflammation-related cytokines and chemokines

Journal of Ethnopharmacology ◽

10.1016/j.jep.2011.05.040 ◽

2011 ◽

Vol 137 (1) ◽

pp. 371-381 ◽

Cited By ~ 31

Author(s):

Mareike Maas ◽

Alexandra M. Deters ◽

Andreas Hensel

Keyword(s):

Inhibitory Activity ◽

Inflammatory Activity ◽

Cytokines And Chemokines ◽

Anti Inflammatory ◽

Eupatorium Perfoliatum

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Development, Optimisation and Evaluation of Ketoprofen Lipospheres

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4389 ◽

2020 ◽

Vol 11 (SPL4) ◽

pp. 1853-1863

Author(s):

Shubhra Rai ◽

Gopal Rai ◽

Ashish Budhrani

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Research Work ◽

Extended Period ◽

Entrapment Efficiency ◽

Inflammatory Activity ◽

Scanning Calorimetry ◽

Anti Inflammatory

Lipospheres represent a novel type of fat-based encapsulation system produced for the topical drug delivery of bioactive compounds. The goal of this research work was to develop lipospheres, including ketoprofen applied for topical skin drug delivery. Ketoprofen lipospheres were formulated by melt emulsification method using stearic acid and Phospholipon® 90G. The lipospheres were analysed in terms of particle size and morphology, entrapment efficiency, Differential scanning calorimetry, In-vitro drug release, In-vivo (Anti-inflammatory activity). Outcomes of research revealed that particle size was found to be 9.66 µm and entrapment efficiency 86.21 ± 5.79 %. In-vivo, the study of ketoprofen loaded lipospheres formulation shows a higher plain formulation concentration in plasma (5.61 mg/mL). For dermis, ketoprofen retention was 27.02 ± 5.4 mg/mL for the lipospheres formulation, in contrast to that of the plain formulation group (10.05 ± 2.8 mg/mL). The anti-inflammatory effect of liposphere drug delivery systems was assessed by the xylene induced ear oedema technique and compared with marketed products. Finally, it seems that the liposphere drug delivery system possesses superior anti-inflammatory activity as compared to the marketed product gel consistencies. Liposphere may be capable of entrapping the medicament at very high levels and controlling its release over an extended period. Liposphere furnishes a proper size for topical delivery as well as is based on non-irritating and non-toxic lipids; it’s a better option for application on damaged or inflamed skin.

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Demonstration of Phytochemicals and In-vitro Antioxidant and Anti-inflammatory activity by methanolic extract of Elettaria cardamomum

Pharmaceutics and Pharmacology Research ◽

10.31579/2693-7247/023 ◽

2020 ◽

Vol 3 (3) ◽

pp. 01-04

Author(s):

Md. Shahidul Islam

Keyword(s):

Methanolic Extract ◽

Research Work ◽

Inflammatory Activity ◽

Pharmacological Activities ◽

Elettaria Cardamomum ◽

Ic50 Values ◽

Phytochemical Profile ◽

Anti Inflammatory ◽

Dpph Scavenging

The existing research study attempts to untie novel avenues for development of the medicinal exercises of Elettaria cardamomum, fashionable known as the “Queen of Spices” and locally recognized as “elaichi”. Its seeds are utilized as abortifacient, acrid, alexiteric, aromatic, sweet, cardiac tonic, cooling, carminative, digestive, diuretic, expectorant, stimulant and also tonic beneficial in the asthma, haemorrhoids, bronchitis, strangury, renal in addition to vesical calculi, anorexia, halitosis, gastropathy dyspepsia as well as burning sensation. The prime goal of this research work is to evaluate antioxidant as well as anti-inflammatory properties of the traditional Bangladeshi medicinal extracts in addition to examine these activities. The aim in present work was to screen the phytochemical profile as well as pharmacological activities of the methanolic extract of this plant’s leaves. To explore pharmacological actions DPPH scavenging test and the HRBC membrane stabilization techniques were done for the antioxidant and also anti-inflammatory test respectively. The pharmacological works revealed that plant extracts might have noteworthy antioxidant effect which is possibly mediated by the inhibition of DPPH free radical which is accountable for oxidation. The IC50 values by the DPPH scavenging test observed for the standard and the leaves were 106.38µg/ml & 594.47µg/ml respectively. There is also moderate anti-inflammatory activity. The IC50 values for anti-inflammatory activity by standard & leaves were 35.04µg/ml and 944.0 µg/ml respectively.

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Anti-Cancer Potential of Synthetic Oleanolic Acid Derivatives and Their Conjugates with NSAIDs

Molecules ◽

10.3390/molecules26164957 ◽

2021 ◽

Vol 26 (16) ◽

pp. 4957

Author(s):

Wanda Baer-Dubowska ◽

Maria Narożna ◽

Violetta Krajka-Kuźniak

Keyword(s):

Signaling Pathways ◽

Oleanolic Acid ◽

Short Review ◽

Therapeutic Effects ◽

Pentacyclic Triterpenoid ◽

Anti Cancer ◽

Inflammatory Drugs ◽

Anti Inflammatory ◽

Synthetic Derivatives ◽

Cancer Activity

Naturally occurring pentacyclic triterpenoid oleanolic acid (OA) serves as a good scaffold for additional modifications to achieve synthetic derivatives. Therefore, a large number of triterpenoids have been synthetically modified in order to increase their bioactivity and their protective or therapeutic effects. Moreover, attempts were performed to conjugate synthetic triterpenoids with non-steroidal anti-inflammatory drugs (NSAIDs) or other functional groups. Among hundreds of synthesized triterpenoids, still the most promising is 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which reached clinical trials level of investigations. The new group of synthetic triterpenoids are OA oximes. The most active among them is 3-hydroxyiminoolean-12-en-28-oic acid morpholide, which additionally improves the anti-cancer activity of standard NSAIDs. While targeting the Nrf2 and NF-κB signaling pathways is the main mechanism of synthetic OA derivatives′ anti-inflammatory and anti-cancer activity, most of these compounds exhibit multifunctional activity, and affect cross-talk within the cellular signaling network. This short review updates the earlier data and describes the new OA derivatives and their conjugates in the context of modification of signaling pathways involved in inflammation and cell survival and subsequently in cancer development.

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