• Microbiology and Biotechnology Letters
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• v.44 no.2
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• pp.218-226
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• 2016

Helicobacter pylori primarily colonizes the human stomach. Infection by this bacterium is associated with various gastric diseases, including inflammation, peptic ulcer, and gastric cancer. Although there are antibiotic regimens for the eradication of H. pylori, the resistance of this species against antibiotics has been continuously increasing. The natural compound plumbagin has been reported as an antimicrobial and anticancer molecule. In this study, we analyzed the inhibitory effect of plumbagin on H. pylori strain ATCC 49503 as well as the expression of various molecules associated with H. pylori growth or virulence by immunoblotting and reverse transcription polymerase chain reaction (RT-PCR) analyses. We demonstrated the minimal inhibitory concentration of plumbagin on H. pylori through the agar dilution and broth dilution methods. Furthermore, we investigated the effect of plumbagin treatment on the expression of the RNA polymerase subunits and various virulence factors of H. pylori. Plumbagin treatment decreased the expression of RNA polymerase subunit alpha (rpoA), which is closely associated with bacterial survival. Moreover, the mRNA and protein levels of the major CagA and VacA toxins were decreased in plumbagintreated H. pylori cells. Likewise, the expression levels of urease subunit alpha (ureA) and an adhesin (alpA) were decreased by plumbagin treatment. Collectively, these results suggest that plumbagin may inhibit the growth, colonization, and pathogenesis of H. pylori by the mechanism demonstrated in this study.

• Journal of Plant Biotechnology
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• v.5 no.3
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• pp.181-185
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• 2003

Callus and suspension cultures derived from leaf explants of Plumbago rosea were established on Murashige and Skoog's medium containing 1 mg/L IAA, 0.5 mg/L NAA and 0.3 mg/L BAP. Callus cultures were tested for their growth and accumulation of plumbagin, a naphthoquinone and was identified by $^1H$ NMR and electron ionization mass spectroscopy. While auxins (not 2,4-D) influenced growth and plumbagin accumulation, cytokinins did not influence them much. Increasing concentrations of IAA in presence of NAA and BAP increased plumbagin in suspensions only up to 1 mg/L. Growth of callus was optimum (8.3 g DCW/I) at a hormonal combination of 1.5 mg/L IAA, 0.5 mg/L NAA and 0.3 mg/L BAP, but high plumbagin accumulation (4.9 mg/g DCW) was recorded at 1.0 mg/L IAA plus 0.3 mg/L BAP. Since instability in growth and secondary metabolite accumulation was noticed, several cell lines/clumps of callus were screened for plumbagin accumulation by visual and analytical methods. Biomass and accumulation of plumbagin showed a negative correlation in several cell lines. But one cell line showed stability both in terms of biomass and plumbagin accumulation over a period of 6 months.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.6
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• pp.687-694
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• 2017

Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats. Although plumbagin alone had no effect on the isometric tone of DFA, $1{\mu}M$ phenylephrine (PhE)-induced partial contraction was largely augmented by plumbagin (${\Delta}T_{Plum}$, 125% of 80 mM KCl-induced contraction at $1{\mu}M$). With relatively higher concentrations (>$5{\mu}M$), plumbagin induced a transient contraction followed by tonic relaxation of DFA. Similar biphasic augmentation of the PhE-induced contraction was observed in MA and RA. VAS2870 and GKT137831, specific NOX4 inhibitors, neither mimicked nor inhibited ${\Delta}T_{Plum}$ in DFA. Also, pretreatment with tiron or catalase did not affect ${\Delta}T_{Plum}$ of DFA. Under the inhibition of PhE-contraction with L-type $Ca^{2+}$ channel blocker (nifedipine, $1{\mu}M$), plumbagin still induced tonic contraction, suggesting $Ca^{2+}$-sensitization mechanism of smooth muscle. Although ${\Delta}T_{Plum}$ was consistently observed under pretreatment with Rho A-kinase inhibitor (Y27632, $1{\mu}M$), a PKC inhibitor (GF 109203X, $10{\mu}M$) largely suppressed ${\Delta}T_{Plum}$. Taken together, it is suggested that plumbagin facilitates the PKC activation in the presence of vasoactive agonists in skeletal arteries. The biphasic contractile effects on the systemic arteries should be considered in the pharmacological studies of plumbagin and 1,4-naphthoquinones.

• Natural Product Sciences
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• v.12 no.1
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• pp.50-54
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• 2006

The wound healing activity of plumbagin and the chloroform extract of Plumbago rosea Linn. (Yoot), incorporated into ointments with yellow soft paraffin, have been investigated on rats. Wound healing activity was studied using excision and incision wound models in rats following topical application. Both plumbagin and the Plumbago rosea root extract produced a significant response in both of the wound models studied. The wound contracted in 14 days in the case of plumbagin (0.1%) and 16 days in case of Plumbago rosea root extract (0.5%), as against in 22 days in the case of control animals. The results were also comparable to those of a standard drug, framycetin sulphate cream (1% w/w) in terms of wound contracting ability, wound closure time, tensile strength of wound and regeneration of tissues at the wound site. Histological studies revealed evidences for the healing process by formation of fibrovascular tissue, epithelization and increased collagenization when compared to control.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.4
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• pp.2325-2331
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• 2013

Objective: To detect effects of plumbagin on proliferation and apoptosis in non-small cell lung cancer cell lines, and investigate the underlying mechanisms. Materials and Methods: Human non-small cell lung cancer cell lines A549, H292 and H460 were treated with various concentrations of plumbagin. Cell proliferation rates was determined using both cell counting kit-8 (CCK-8) and clonogenic assays. Apoptosis was detected by annexin V/propidium iodide double-labeled flow cytometry and TUNEL assay. The levels of reactive oxygen species (ROS) were detected by flow cytometry. Activity of NF-${\kappa}B$ was examined by electrophoretic mobility shift assay (EMSA) and luciferase reporter assay. Western blotting was used to assess the expression of both NF-${\kappa}B$ regulated apoptotic-related gene and activation of p65 and $I{\kappa}B{\kappa}$. Results: Plumbagin dose-dependently inhibited proliferation of the lung cancer cells. The IC50 values of plumbagin in A549, H292, and H460 cells were 10.3 ${\mu}mol/L$, 7.3 ${\mu}mol/L$, and 6.1 ${\mu}mol/L$ for 12 hours, respectively. The compound concentration-dependently induced apoptosis of the three cell lines. Treatment with plumbagin increased the intracellular level of ROS, and inhibited the activation of NK-${\kappa}B$. In addition to inhibition of NF-${\kappa}B$/p65 nuclear translocation, the compound also suppressed the degradation of $I{\kappa}B{\kappa}$. ROS scavenger NAC highly reversed the effect of plumbagin on apoptosis and inactivation of NK-${\kappa}B$ in H460 cell line. Treatment with plumbagin also increased the activity of caspase-9 and caspase-3, downregulated the expression of Bcl-2, upregulated the expression of Bax, Bak, and CytC. Conclusions: Plumbagin inhibits cell growth and induces apoptosis in human lung cancer cells through an NF-${\kappa}B$-regulated mitochondrial-mediated pathway, involving activation of ROS.

• Journal of Microbiology and Biotechnology
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• v.18 no.2
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• pp.314-321
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• 2008

Acaricidal effects of materials derived from Diospyros kaki roots against Dermatophagoides farinae and D. pteronyssinus were assessed using impregnated fabric disk bioassay and compared with that of the commercial benzyl benzoate. The observed responses varied according to dosage and mite species. The $LD_{50}$ values of the chloroform extract of Diospyros kaki roots were 1.66 and $0.96{\mu}g/cm^2$ against D. farinae and D. pteronyssinus. The chloroform extract of Diospyros kaki roots was approximately 15.2 more toxic than benzyl benzoate against D. farinae, and 7.6 times more toxic against D. pteronyssinus. Purification of the biologically active constituent from D. kaki roots was done by using silica gel chromatography and high-performance liquid chromatography. The structure of the acaricidal component was analyzed by GC-MS, $^1H-NMR,\;^{13}C-NMR,\;^1H-^{13}C$ COSY-NMR, and DEPT-NMR spectra, and identified as plumbagin. The acaricidal activity of plumbagin and its derivatives (naphthazarin, dichlon, 2,3-dibromo-1,4-naphthoquinone, and 2-bromo-1,4-naphthoquinone) was examined. On the basis of $LD_{50}$ values, the most toxic compound against D. farinae was naphthazarin $(0.011{\mu}g/cm^2)$ followed by plumbagin $(0.019{\mu}g/cm^2),$ 2-bromo-1,4-naphthoquinone $(0.079{\mu}g/cm^2)$, dichlon $(0.422{\mu}g/cm^2)$, and benzyl benzoate $(9.14{\mu}g/cm^2)$. Additionally, the skin color of the dust mites was changed from colorless-transparent to dark brown-black by the treatment of plumbagin. Similar results have been exhibited in its derivatives (naphthazarin, dichlon, and 2-bromo-1,4-naphthoquinone). In contrast, little or no discoloration was observed for benzyl benzoate. From this point of view, plumbagin and its derivatives can be very useful for the potential control agents, lead compounds, and indicator of house dust mites.

• Journal of Life Science
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• v.27 no.3
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• pp.325-333
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• 2017

High level of plasma cholesterol is strongly associated with the development of atherosclerosis and coronary heart disease. Clinical trials designed to reduce plasma cholesterol level by diet or pharmacological intervention have resulted in marked reduction of disease incidence. The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which reduces cholesterol biosynthesis in the liver is the key enzyme of the mevalonate pathway that produces cholesterol. In this study, 71 naturally occurring phenolic compounds were tested for inhibitory activities against HMG-CoA reductase. Eleven compounds out of 71 showed inhibitory activities: three hydrolyzable tannin (geraniin, acetonyl geraniin and pentagalloyl ${\beta}-D-glucose$), four benzoic acid derivatives (benzoic acid, trans-cinnamic acid, 2,4-dihydroxybenzoic acid and 2,5-dihydroxybenzoic acid), and four naphthoquinone derivatives (1,2-naphthoquinone, 1,4-naphthoquinone, plumbagin and shikonin). At the concentration of $10{\mu}g/ml$, 1,4-naphthoquinone inhibited HMG-CoA reductase by 99.4%, and then plumbagin 91.4%, pentagalloyl ${\beta}-D-glucose$ 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonyl geraniin 30.2%, benzoic acid 28.5%, geraniin 28.3% and 2,5-dihydroxybenzoic acid 22.3%, respectively. $IC_{50}$ values of 1,4-naphthoquinone and plumbagin was $2.1{\mu}g/ml$ and $5.8{\mu}g/ml$, respectively.

• The Plant Pathology Journal
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• v.23 no.2
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• pp.113-115
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• 2007

A kind of naphthoquinone, plumbagin was purified and identified from the leaves of Nepenthes $ventricosa\;{\times}\;maxima$ through solvent extraction, silica gel column chromatography, and recrystallization. The yield (0.51%) was higher than that of the root of Plumbago scandens (0.26%), P. capensis (0.15%), and N. thorelii (0.092%). It exhibited antifungal activity against all plant pathogenic fungi tested, Alternaria alternata, Aspergillus niger, Bipolaris oryzae, Fusarium oxysporum, Phytophthora capsici, Rhizoctonia solani, Rhizopus stolonifer var. stolonifer and Sclerotinia sclerotiorum. The minimum inhibitory concentration values ranged from about 4.8 to $56.6\;{\mu}g/ml$ against the above eight fungi and R. solani was the most sensitive.

• 한국약용작물학회:학술대회논문집
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• 2011.04a
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• pp.106-107
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• 2011

• Microbiology and Biotechnology Letters
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• v.28 no.1
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• pp.1-7
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• 2000

The bacterial strain JW-2 which conferred resistance against paraquat (1,1'-dimethyl-4,4'-bipyridinium dichloride) was isolated from soil. The strain was identified as an Ochrobactrum anthropi based on its morphological, physiological, biological and fatty acid composition, and was designated as Ochrobactrum anthropi JW-2. We compard paraquat resistance of O. anthropi JW-2 with Escherichia coli J105. In the presence of 100mM paraquat, E. coli JM105 was not grown whereas the growth rate of O. anthropi was about 70% of control. We compared the sensitivity of O. anthropi JW-2 and E. coli J105 to redox-cycling compounds such as paraquat, plumbagin or menadione, which are known to exacebate wuperoxide generation. O. anthropi JW-2 did not show cross-resistance to plumbagin or menadione. superoxide dismutase activity was increased in paraqunt-treated E. coli JM105 while it was not increased in O.anthropi JW-2. These results suggest that the mechanism of paraquat resistance in O.anthropi JW-2 is probably due to selectively decreased permeability toward paraquat by membrane protein.