Synthesis and evaluation of antibacterial activities of andrographolide analogues

Jiang, Xiaojian; Yu, Pei; Jiang, Jie; Zhang, Zaijun; Wang, Zhongli; Yang, Zhaoqi; Tian, Zhimei; Wright, Susan C.; Larrick, James W.; Wang, Yuqiang

doi:10.1016/j.ejmech.2008.12.014

Cited by 87 publications

(61 citation statements)

References 44 publications

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“…The antibacterial and anti-inflammatory effects have been attributed related to the immune system. Previous studies showed that Andrographis paniculata has been recently identified as a potent inhibitor of NF-kB [19][20][21]. Andrograpanin not block the activation of ERK1/2, JNK MAPKs and NF-κB activation but it only inhibited p38 MAPKs activation [22].…”

Section: Discussionmentioning

confidence: 99%

Andrographis Paniculata (Burm. F.) Nees Induces Clinical and Sputum Conversion in Pulmonary Tuberculosis Patients

Widhawati¹,

Hanani²,

Zaini³

2015

Med-Science

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Section: Discussionmentioning

confidence: 99%

Andrographis Paniculata (Burm. F.) Nees Induces Clinical and Sputum Conversion in Pulmonary Tuberculosis Patients

Widhawati¹,

Hanani²,

Zaini³

2015

Med-Science

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“…TBN was synthesized and purified in our laboratory. 26,28) All other reagents were purchased from Sigma-Aldrich unless stated otherwise.…”

Section: Methodsmentioning

confidence: 99%

Therapeutic Effects of Multifunctional Tetramethylpyrazine Nitrone on Models of Parkinson’s Disease <i>in Vitro</i> and <i>in Vivo</i>

Guo¹,

Duan³

et al. 2014

Biological & Pharmaceutical Bulletin

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“…1) significantly protected β-cells in diabetic rats and the finding that NO offered protection to β-cells, we wanted to know if andrographolide derivatives bearing NO-donating moieties could release NO to offer additional protective effects to β-cells. 2) We herein reported synthesis of several novel andrographolide derivatives with NO-releasing capability. The target compounds were evaluated for their in vitro protective effects against tertbutyl hydroperoxide (t-BHP) induced cell damage.…”

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confidence: 99%

“…1), the main bioactive component of the medicinal plant Andrographis paniculata, has a variety of biological activities including anti-inflammation, 1) anti-bacteria, [2][3][4] anti-malaria, 5) hepatoprotection, 6,7) immunomodulation, 8) and anti-cancer. 9,10) In addition, previous studies showed that andrographolide lowered blood glucose levels and possessed anti-diabetic properties.…”

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confidence: 99%

Synthesis and Preliminary Biologic Activity Evaluation of Nitric Oxide-Releasing Andrographolide Derivatives in RIN-m Cells

Liang¹,

Du²,

Xu³

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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Pancreatic β-cell dysfunction and death are important feature of diabetes mellitus. Beta-cell protection has demonstrated clinical benefits in the treatment of this disease. In the present study, andrographolide derivatives with nitric oxide (NO)-releasing capability were synthesized and their protective effects against tert-butyl hydroperoxide (t-BHP) induced cell damage were investigated in RIN-m cells. Compound 6b was found to release a moderate amount of NO and was more potent than its natural parent andrographolide in inhibiting cell apoptosis. These findings suggested that andrographolide derivatives with NO-releasing capacity may be a potential therapy for diabetes.Key words andrographolide; synthesis; nitric oxide (NO) donor; β cell protection Andrographolide ( Fig. 1), the main bioactive component of the medicinal plant Andrographis paniculata, has a variety of biological activities including anti-inflammation, 1) anti-bacteria, 2-4) anti-malaria, 5) hepatoprotection, 6,7) immunomodulation, 8) and anti-cancer. 9,10) In addition, previous studies showed that andrographolide lowered blood glucose levels and possessed anti-diabetic properties.11) It was reported that the anti-diabetic effects of andrographolide were attributed to its anti-inflammation and hypoglycemic effects.12) It has been documented that andrographolide attenuated inflammation primarily through inhibition of the nuclear factor-kappa B (NF-κB) signalling pathway. 13,14) Jin et al. reported that andrographolide inhibited tumor necrosis factor-alpha (TNF-α) induced insulin resistance and improved insulin sensitivity through inhibition of the NF-κB pathway. 15) In an effort to find more effective therapies for diabetes, we have recently synthesized numerous andrographolide derivatives, investigated their antidiabetic activities and their potential mechanisms of action. 16) Nitric oxide (NO) is a small, diffusible and highly reactive molecule with many important biological and physiological functions. The role NO plays in insulin secretion has been controversial. 17) Although excessive NO production within β-cells may trigger oxidative/nitrosative stress leading to cell death, NO also served as an important β-cell stimulus-secretion coupling factor. [18][19][20] Evidence suggested that exogenous NO and endogenous glucose-stimulated β-cell NO augmented insulin release. 21) In addition, studies had demonstrated that NO stimulated insulin secretion by stimulating calcium release from mitochondria. 22) A recent report also suggested that low levels of NO protected β-cells from thapsigargin-induced apoptosis. 23)Building on our previous discovery that andrographolide and its lipoic acid conjugate AL-1 (Fig. 1) significantly protected β-cells in diabetic rats and the finding that NO offered protection to β-cells, we wanted to know if andrographolide derivatives bearing NO-donating moieties could release NO to offer additional protective effects to β-cells.2) We herein reported synthesis of several novel andrographolide derivatives with NO-releasin...

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Synthesis and evaluation of antibacterial activities of andrographolide analogues

Cited by 87 publications

References 44 publications

Andrographis Paniculata (Burm. F.) Nees Induces Clinical and Sputum Conversion in Pulmonary Tuberculosis Patients

Andrographis Paniculata (Burm. F.) Nees Induces Clinical and Sputum Conversion in Pulmonary Tuberculosis Patients

Therapeutic Effects of Multifunctional Tetramethylpyrazine Nitrone on Models of Parkinson’s Disease <i>in Vitro</i> and <i>in Vivo</i>

Synthesis and Preliminary Biologic Activity Evaluation of Nitric Oxide-Releasing Andrographolide Derivatives in RIN-m Cells

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