Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-α

Shah, Muhammad Raza; Arfan, Muhammad; Amin, Hazrat; Hussain, Zahid; Qadir, Muhammad Irfan; Choudhary, M. Iqbal; VanDerveer, Donald G.; Mesaik, M. Ahmed; Soomro, Samreen; Jabeen, Almas; Khan, Inam Ullah

doi:10.1016/j.bmcl.2012.02.096

Cited by 34 publications

(21 citation statements)

References 26 publications

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“…A previous study showed that bergenin is a potent inhibitor of the inflammatory mediators, NO and TNF-α [21]. In the present study, NO, TNF-α, IL-1β, and IL-6 were analyzed.…”

Section: Discussionmentioning

confidence: 99%

“…Studies report that it has multiple biological activities, such as anti-oxidant [16], antiinflammatory [17], anti-malarial [18], neuroprotective [19], and immunomodulatory [20] properties. The antiinflammatory action of bergenin is associated with potent inhibition of the inflammatory mediators, NO and TNF-a, as demonstrated in macrophages stimulated with LPS [21]. The exact molecular mechanism of bergenin's antiinflammatory effects remains unclear, and there is little data about the anti-inflammatory effect of bergenin on mastitis.…”

Section: Introductionmentioning

confidence: 96%

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Bergenin Plays an Anti-Inflammatory Role via the Modulation of MAPK and NF-κB Signaling Pathways in a Mouse Model of LPS-Induced Mastitis

et al. 2014

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Mastitis is a major disease in humans and other animals and is characterized by mammary gland inflammation. It is a major disease of the dairy industry. Bergenin is an active constituent of the plants of genus Bergenia. Research indicates that bergenin has multiple biological activities, including anti-inflammatory and immunomodulatory properties. The objective of this study was to evaluate the protective effects and mechanism of bergenin on the mammary glands during lipopolysaccharide (LPS)-induced mastitis. In this study, mice were treated with LPS to induce mammary gland mastitis as a model for the disease. Bergenin treatment was initiated after LPS stimulation for 24 h. The results indicated that bergenin attenuated inflammatory cell infiltration and decreased the concentration of NO, TNF-α, IL-1β, and IL-6, which were increased in LPS-induced mouse mastitis. Furthermore, bergenin downregulated the phosphorylation of nuclear factor-kappaB (NF-κB) and mitogen-activated protein kinases (MAPK) signaling pathway proteins in mammary glands with mastitis. In conclusion, bergenin reduced the expression of NO, TNF-α, IL-1β, and IL-6 proinflammatory cytokines by inhibiting the activation of the NF-κB and MAPKs signaling pathways, and it may represent a novel treatment strategy for mastitis.

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“…A previous study showed that bergenin is a potent inhibitor of the inflammatory mediators, NO and TNF-α [21]. In the present study, NO, TNF-α, IL-1β, and IL-6 were analyzed.…”

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 96%

Bergenin Plays an Anti-Inflammatory Role via the Modulation of MAPK and NF-κB Signaling Pathways in a Mouse Model of LPS-Induced Mastitis

et al. 2014

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“…Furthermore, it has a range of pharmacologic activities such as neuroprotective (Takahashi et al, 2003), antitussive, hypolipidemic, anti-HIV, anti-inflammatory, PTP1B inhibitory and gastroprotective effects (Li et al, 2005). Its free-radical scavenging ability is well established, while its hepatoprotective activity has been reported in various in-vitro and in-vivo models (Shah et al, 2012). Being with a safe pharmacological profile and reactive multiple sides in its structure, it offers good possibilities for the derivatization of sugar-based nonionic surfactants.…”

Section: Introductionmentioning

confidence: 99%

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

et al. 2016

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Context: Vesicular systems have attracted great attention in drug delivery because of their amphiphilicity, biodegradability, non-toxicity and potential for increasing drug bioavailability. Objective: A novel sugar-based double-tailed surfactant containing renewable block was synthesized for preparing niosomal vesicles that could be exploited for Levofloxacin encapsulation, aiming to increase its oral bioavailability. Materials and methods: The surfactant was characterized by 1 H NMR, mass spectroscopy and Fourier transform infrared spectroscopy (FT-IR). Its biocompatibility was studied against cell cultures and human blood hemolysis. In vivo acute toxicity was evaluated in mice. The vesicle morphology, size, drug-excipients interaction and entrapment efficiency (EE) were examined using atomic force microscope (AFM), dynamic light scattering (DLS), FT-IR and HPLC. Oral bioavailability studies of Levofloxacin in surfactant-based niosomal formulation were carried out using rabbits and plasma samples were analyzed using HPLC. Results and discussion: Vesicles were spherical in shape and the size was 190.31 ± 4.51 nm with a polydispersity index (PDI) of 0.29 ± 0.03. The drug EE in niosomes was 68.28 ± 3.45%. When applied on cell lines, high cell viability was observed even after prolonged exposure at high concentrations. It caused 5.77 ± 1.34% hemolysis at 1000 mg/mL and was found to be safe up to 2000 mg/kg. Elevated Levofloxacin plasma concentration was achieved when delivered with novel vesicles. Conclusion:The surfactant was demonstrated to be safe and effective as carrier of Levofloxacin. The study suggests that this sugar-based double-tailed nonionic surfactant could be promising nano-vesicular system for delivery and enhancing oral bioavailability of the hydrophobic Levofloxacin.

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“…8,10-Di-O-methylbergenin (7) was synthesized by methylation of bergenin (1) and norbergenin (2) with diazomethane [97,139]. Shah et al have prepared the alkyl derivatives of bergenin (7,(37)(38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50) by treating alkyl halides with bergenin (1) under mild basic conditions [107] (Fig. 3).…”

Section: Alkylationmentioning

confidence: 99%

Diversity, pharmacology and synthesis of bergenin and its derivatives: Potential materials for therapeutic usages

Bajracharya

2015

Fitoterapia

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Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-α

Cited by 34 publications

References 26 publications

Bergenin Plays an Anti-Inflammatory Role via the Modulation of MAPK and NF-κB Signaling Pathways in a Mouse Model of LPS-Induced Mastitis

Bergenin Plays an Anti-Inflammatory Role via the Modulation of MAPK and NF-κB Signaling Pathways in a Mouse Model of LPS-Induced Mastitis

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

Diversity, pharmacology and synthesis of bergenin and its derivatives: Potential materials for therapeutic usages

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