Evaluation of anti-inflammatory and immunomodulatory effects of Premna integrifolia extracts and assay-guided isolation of a COX-2/5-LOX dual inhibitor

Azad, Rajaram; Babu, Neela Kishore; Gupta, Atul; Reddanna, Pallu

doi:10.1016/j.fitote.2018.10.016

Cited by 21 publications

(10 citation statements)

References 31 publications

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“…43 Our studies in this direction have resulted in the isolation of a natural product, chebulagic acid isolated from Terminalia chebula and 6-hydroxy salvinolone isolated from the roots of Premna integrifolia with COX-2/5-LOX dual inhibition and with potent anti-inflammatory and anticancer effects. [44][45][46] However, further welldesigned pre-clinical and clinical trials are required for evaluation of their efficacy and safety and further development.…”

Section: Cox-2/5-lox Dual Inhibitors Spare Gastrointestinal and Cardiac Side-effects?mentioning

confidence: 99%

Overview on the Discovery and Development of Anti-Inflammatory Drugs: Should the Focus Be on Synthesis or Degradation of PGE2?

Mahesh¹,

Kumar²,

Reddanna³

2021

JIR

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Inflammation is a protective response that develops against tissue injury and infection. Chronic inflammation, on the other hand, is the key player in the pathogenesis of many inflammatory disorders including cancer. The cytokine storm, an inflammatory response flaring out of control, is mostly responsible for the mortality in COVID-19 patients. Anti-inflammatory drugs inhibit cyclooxygenases (COX), which are involved in the biosynthesis of prostaglandins that promote inflammation. The conventional non-steroidal anti-inflammatory drugs (NSAIDs) are associated with gastric and renal side-effects, as they inhibit both the constitutive COX-1 and the inducible COX-2. The majority of selective COX-2 inhibitors (COXIBs) are without gastric side-effects but are associated with cardiac side-effects on long-term use. The search for anti-inflammatory drugs without side-effects, therefore, has become a dream and ongoing effort of the Pharma companies. As PGE 2 is the key mediator of inflammatory disorders, coming up with a strategy to reduce the levels of PGE 2 alone without affecting other metabolites may form a better choice for the development of next generation anti-inflammatory drugs. In this direction the options being explored are on synthesis of PGE 2 -mPGES-1; PGE 2 degradation through a specific PG dehydrogenase, 15-PGDH, and by blocking its activity mediated through a specific PGE receptor, EP4. As leukotrienes formed via the 5-lipoxygenase (5-LOX) pathway also play an important role in the mediation of inflammation, efforts are also being made to target both COX and LOX pathways. This review focuses on addressing the following three points: 1) How NSAIDs and COXIBs are associated with gastric, renal and cardiac side-effects; 2) Should the focus be on the targets upstream or downstream of PGE 2 ; and 3) the status of alternative targets being explored for the discovery and development of anti-inflammatory drugs without side-effects.

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Section: Cox-2/5-lox Dual Inhibitors Spare Gastrointestinal and Cardiac Side-effects?mentioning

confidence: 99%

Overview on the Discovery and Development of Anti-Inflammatory Drugs: Should the Focus Be on Synthesis or Degradation of PGE2?

Mahesh¹,

Kumar²,

Reddanna³

2021

JIR

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“…The petroleum ether extract of the leaves of Premna integrifolia Linn (Another congeneric plant of Premna Puberula Pamp.) decreased the formation of nitric oxide (NO), reduced pro-inflammatory cytokines (IL-1β, IL-6) and prostaglandin E2 (PGE2), induced anti-inflammatory cytokine (IL-2) and down-regulated COX-2, 5-LOX, TNF-α, IL-1β and iNOS [ 9 ]. Furthermore, in an in vivo study, the petroleum ether extracts significantly reduced paw edema in a carrageenan-induced inflammation model in mice [ 9 ].…”

Section: Discussionmentioning

confidence: 99%

“…have focused on the anti-inflammatory effects. The examples included Premna microphylla Turcz., Premna fulva Craib., and Premna integrifolia Linn [ 1 , 8 , 9 ]. However, little studies have been reported for P. Puberula , its chemical compounds, preparation, quality control, effects and toxicity.…”

Section: Introductionmentioning

confidence: 99%

Quality control, preparation process optimizing and anti-inflammatory effects of Premna Puberula Pamp. Pectin

Liu

Guo²,

Chen³

et al. 2022

Heliyon

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“…Indomethacin was used as a standard reference enzyme inhibitor in the COX assay. The results were measured at 405 nm, with reference wavelengths of 570 nm and 590 nm, and were expressed as IC 50 (μg/mL) [ 25 , 60 ]. Furthermore, 5-LOX enzyme was extracted from potato tubers as described previously [ 61 ].…”

Section: Methodsmentioning

confidence: 99%

Quercetin-3-Glucoside Extracted from Apple Pomace Induces Cell Cycle Arrest and Apoptosis by Increasing Intracellular ROS Levels

Nile

Shin

et al. 2021

IJMS

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Cervical cancer is a life-threatening disease and the fourth most common cancer among women worldwide. Apple pomace is a multifunctional phenolic compound possessing effective biological activity against cervical cancer cells. This study aimed to investigate the anticancer effects of quercetin-3-glucoside (Q3G) extracted from apple pomace in HeLa cell lines and analyze its molecular mechanisms. High-performance liquid chromatography revealed that Q3G, coumaric acid, phloridzin, quercetin, and phloretin are the major polyphenolic compounds constituting apple pomace. Among them, Q3G possessed the greatest antioxidant and anti-inflammatory effects in vitro and exhibited significant cytotoxic effects in HeLa cells in a dose-and time-dependent manner. Flow cytometric analysis indicated that Q3G induced cell cycle arrest at the S phase in a time-dependent manner by altering cyclin-dependent kinase 2. Moreover, it induced apoptosis via chromosomal DNA degradation and increased reactive oxygen species generation. Furthermore, Q3G treatment altered the apoptosis-associated protein expression in the cells by activating caspase-9/-3, downregulating anti-apoptosis protein B-cell lymphoma (Bcl)-2 expressions and up regulating the pro-apoptotic Bcl-2-associated X protein. BH3-interacting domain death agonist cleavage occurred prior to the degradation of an anti-apoptotic Mu-2-related death-inducing gene involved in cell death signaling. Consequently, apple pomace Q3G holds promise as an anti-inflammatory and anticancer agent for treating cervical cancer.

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Evaluation of anti-inflammatory and immunomodulatory effects of Premna integrifolia extracts and assay-guided isolation of a COX-2/5-LOX dual inhibitor

Cited by 21 publications

References 31 publications

Overview on the Discovery and Development of Anti-Inflammatory Drugs: Should the Focus Be on Synthesis or Degradation of PGE2?

Overview on the Discovery and Development of Anti-Inflammatory Drugs: Should the Focus Be on Synthesis or Degradation of PGE2?

Quality control, preparation process optimizing and anti-inflammatory effects of Premna Puberula Pamp. Pectin

Quercetin-3-Glucoside Extracted from Apple Pomace Induces Cell Cycle Arrest and Apoptosis by Increasing Intracellular ROS Levels

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