Design and synthesis of novel magnolol derivatives as potential antimicrobial and antiproliferative compounds

Srinivas, Jada; Doma, Mahendhar Reddy; Singh, Parvinder Pal; Kumar, Suresh; Malik, Fayaz; Sharma, Akash; Khan, Inshad Ali; Qazi, G. N.; Kumar, Halmuthur M. Sampath

doi:10.1016/j.ejmech.2011.12.039

Cited by 32 publications

(21 citation statements)

References 23 publications

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“…Recently, we reported the cell growth inhibitory effect of Ery5 in different cell lines including PC-3. 29, 32 In PC-3, Ery5 treatment significantly inhibited colony formation at 1 μ M concentration and was more prominent with increasing doses of Ery5 (Figures 1b and c). While examining the anti-angiogenic effect in HUVECs and PC-3 cells, it was found that Ery5 significantly inhibited the tube formation in HUVECs in a dose-dependent manner.…”

Section: Resultsmentioning

confidence: 94%

Autophagy triggered by magnolol derivative negatively regulates angiogenesis

et al. 2013

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Angiogenesis has a key role in the tumor progression and metastasis; targeting endothelial cell proliferation has emerged as a promising therapeutic strategy for the prevention of cancer. Previous studies have revealed a complex association between the process of angiogenesis and autophagy and its outcome on tumorigenesis. Autophagy, also known as type-II cell death, has been identified as an alternative way of cell killing in apoptotic-resistant cancer cells. However, its involvement in chemoresistance and tumor promotion is also well known. In this study, we used a derivate of natural product magnolol (Ery5), a potent autophagy inducer, to study the association between the autophagy and angiogenesis in both in vitro and in vivo model system. We found that the robust autophagy triggered by Ery5, inhibited angiogenesis and caused cell death independent of the apoptosis in human umbilical cord vein endothelial cells and PC-3 cells. Ery5 induced autophagy effectively inhibited cell proliferation, migration, invasion and tube formation. We further demonstrated that Ery5-mediated autophagy and subsequent inhibition of angiogenesis was reversed when autophagy was inhibited through 3-methyl adenine and knocking down of key autophagy proteins ATG7 and microtubule-associated protein light chain 3. While evaluating the negative regulation of autophagy on angiogenesis, it was interesting to find that angiogenic environment produced by the treatment of VEGF and CoCl2 remarkably downregulated the autophagy and autophagic cell death induced by Ery5. These studies, while disclosing the vital role of autophagy in the regulation of angiogenesis, also suggest that the potent modulators of autophagy can lead to the development of effective therapeutics in apoptosis-resistant cancer.

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Section: Resultsmentioning

confidence: 94%

Autophagy triggered by magnolol derivative negatively regulates angiogenesis

et al. 2013

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“…The hydroxyl group on biphenolic moiety results in magnolol/honokiol against reactive oxygen species, inhibiting cell proliferation and antimicrobial activity [3,6,14]. It has been reported that most of allylated biphenolic magnolol/honokiol analogues possessed anti-proliferative activity and anti-MRSA capacity while magnolol analogues with flexible allylated biphenolic structure showed a better anti-virus activity than simple allylated ones [4,5]. In addition, the derivatives of honokiol with the biaryl structure bearing a hydroxyl and a allyl groups at the 4'-hydroxyl shown to be essential for neurite outgrowth-promoting activity [15].…”

Section: Reviewmentioning

confidence: 99%

Cardiovascular protection of magnolol: cell-type specificity and dose-related effects

Hong

2012

J Biomed Sci

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Magnolia officinalis has been widely used in traditional Chinese medicine. Magnolol, an active component isolated from Magnolia officinalis, is known to be a cardiovascular protector since 1994. The multiplex mechanisms of magnolol on cardiovascular protection depends on cell types and dosages, and will be reviewed and discussed in this article. Magnolol under low and moderate dosage possesses the ability to protect heart from ischemic/reperfusion injury, reduces atherosclerotic change, protects endothelial cell against apoptosis and inhibits neutrophil-endothelial adhesion. The moderate to high concentration of magnolol mainly acts on smooth muscle cells and platelets. Magnolol induces apoptosis in vascular smooth muscle cells at moderate concentration and inhibits proliferation at moderate and high concentration. High concentration of magnolol also abrogates platelet activation, aggregation and thrombus formation. Magnolol also serves as an smooth muscle relaxant only upon the high concentration. Oral intake of magnolol to reach the therapeutic level for cardiovascular protection is applicable, thus makes magnolol an agent of great potential for preventing cardiovascular diseases in high-risk patients.

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“…Numerous preclinical studies have established that MAG exerts its effect on different types of human cancers such as those of lung, prostate, breast, gall bladder, colon, skin and hepatocellular carcinoma [50,51,52,53,54,55,56,57]. The plausible molecular mechanisms liable for the anti-cancer potential of MAG are reduced cell proliferation or cell cytotoxicity, induction of apoptosis, accumulation of reactive oxygen species (ROS), induction of autophagy and activation/inactivation of various cellular signaling pathways [46].…”

Section: Introductionmentioning

confidence: 99%

Magnolol: A Neolignan from the Magnolia Family for the Prevention and Treatment of Cancer

Ranaware¹,

Banik

Deshpande³

et al. 2018

IJMS

128

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The past few decades have witnessed widespread research to challenge carcinogenesis; however, it remains one of the most important health concerns with the worst prognosis and diagnosis. Increasing lines of evidence clearly show that the rate of cancer incidence will increase in future and will create global havoc, designating it as an epidemic. Conventional chemotherapeutics and treatment with synthetic disciplines are often associated with adverse side effects and development of chemoresistance. Thus, discovering novel economic and patient friendly drugs that are safe and efficacious is warranted. Several natural compounds have proved their potential against this dreadful disease so far. Magnolol is a hydroxylated biphenyl isolated from the root and stem bark of Magnolia tree. Magnolol can efficiently prevent or inhibit the growth of various cancers originating from different organs such as brain, breast, cervical, colon, liver, lung, prostate, skin, etc. Considering these perspectives, the current review primarily focuses on the fascinating role of magnolol against various types of cancers, and the source and chemistry of magnolol and the molecular mechanism underlying the targets of magnolol are discussed. This review proposes magnolol as a suitable candidate that can be appropriately designed and established into a potent anti-cancer drug.

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Design and synthesis of novel magnolol derivatives as potential antimicrobial and antiproliferative compounds

Cited by 32 publications

References 23 publications

Autophagy triggered by magnolol derivative negatively regulates angiogenesis

Autophagy triggered by magnolol derivative negatively regulates angiogenesis

Cardiovascular protection of magnolol: cell-type specificity and dose-related effects

Magnolol: A Neolignan from the Magnolia Family for the Prevention and Treatment of Cancer

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