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Research regarding the anti-microbial activity of Hydrastis canadensis (goldenseal) and/or its active compounds berberine and hydrastine
This information has been complied in order to facilitate the research efforts of health care professionals and others. These statements have not been evaluated by the Food and Drug Administration and are not intended diagnose, treat, cure, prevent, mitigate, or prevent any disease. The information is presented with the latest publications first. This is an ongoing work so check back often as we will update these pages as more information becomes available. Also see the anti-parasitic and anti-diarrhea pages. Last Updated : 08/25/2008
Potent In Vitro Synergism of Fluconazole and Berberine Chloride against
Clinical Isolates of Candida albicans Resistant to Fluconazole.
Quan H, Cao YY, Xu Z, Zhao JX, Gao PH, Qin XF, Jiang YY.
Antimicrob Agents Chemother. 2006 Mar;50(3):1096-9
In vitro interaction of fluconazole and berberine chloride was investigated
against 40 fluconazole-resistant clinical isolates of Candida albicans.
Synergism in fungistatic activity was found with the checkerboard
microdilution assay. The findings of agar diffusion tests and time-kill
curves confirmed the synergistic interaction, but no antagonistic action was
observed.
Antimicrobial Activity of Berberine Alone and in Combination with Ampicillin
or Oxacillin Against Methicillin-Resistant Staphylococcus aureus.
Yu HH, Kim KJ, Cha JD, Kim HK, Lee YE,
Choi NY, You YO.
J Med Food. 2005
Winter;8(4):454-61.
Methicillin-resistant Staphylococcus aureus (MRSA) bacteria have been
responsible for substantial morbidity and mortality in hospitals because
they usually have multidrug resistance. Some natural products are candidates
as new antibiotic substances. In the present study, we investigated the
antimicrobial activity of berberine, the main antibacterial substance of
Coptidis rhizoma (Coptis chinensis Franch) and Phellodendri cortex (Phellodendron
amurense Ruprecht), against clinical isolates of MRSA, and the effects of
berberine on the adhesion to MRSA and intracellular invasion into human
gingival fibroblasts (HGFs). Berberine showed antimicrobial activity against
all tested strains of MRSA. Minimum inhibition concentrations (MICs) of
berberine against MRSA ranged from 32 to 128 microg/mL. Ninety percent
inhibition of MRSA was obtained with 64 microg/mL or less of berberine. In
the checkerboard dilution test, berberine markedly lowered the MICs of
ampicillin and oxacillin against MRSA. An additive effect was found between
berberine and ampicillin, and a synergistic effect was found between
berberine and oxacillin against MRSA. In the presence of 1-50 microg/mL
berberine, MRSA adhesion and intracellular invasion were notably decreased
compared with the vehicle-treated control group. These results suggest that
berberine may have antimicrobial activity and the potential to restore the
effectiveness of beta-lactam antibiotics against MRSA, and inhibit the MRSA
adhesion and intracellular invasion in HGFs.
Berberine Inhibits Arylamine N-Acetyltransferase Activity
and Gene Expression in Salmonella Typhi.
Wu LT, Tsou MF, Ho CC, Chuang JY, Kuo HM, Chung JG
Curr Microbiol.
2005 Aug 2;
The effects of berberine on growth, arylamine N-acetyltransferase (NAT)
activity, and gene expression in Salmonella Typhi (Typhi) were described.
The growth inhibition of Typhi was determined by measuring absorbance by
optical density (OD at 650 nm). The NAT activity was determined by measuring
the levels of 2-aminofluorene (AF) and N-acetyl-2-aminofluorene (AAF) by
high-performance liquid chromatography. The results demonstrated that 24-h
berberine treatment decreased bacteria growth and amounts of AAF in Typhi.
Western blotting and flow cytometry were used for examining the levels of
NAT after bacteria were cotreated with or without various concentrations of
berberine, and results indicated that berberine decreased the levels of NAT
in Typhi. Polymerase chain reaction was used for examining the gene
expression of NAT (mRNA NAT), and results indicated that berberine affects
mRNA NAT1 expression in Typhi.
Inhibition of sortase-mediated Staphylococcus aureus
adhesion to fibronectin via fibronectin-binding protein by sortase
inhibitors.
Oh KB, Oh MN, Kim JG, Shin DS, Shin J
Appl
Microbiol Biotechnol. 2005 Jul 12;:1-5
The sortase enzymes are a family of Gram-positive transpeptidases
responsible for anchoring surface protein virulence factors to the
peptidoglycan cell wall layer. In Staphylococcus aureus, deletion of the
sortase isoforms results in marked reduction in virulence and infection
potential, making it an important antivirulence target. Recombinant sortase
A (SrtA) and sortase B (SrtB) were incubated with peptide substrate
containing either the LPETG or NPQTN motifs.
(Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile,
beta-sitosterol-3-O-glucopyranoside, berberine chloride, and psammaplin A1
showed potent inhibitory activity against SrtA and SrtB. These compounds
also exhibited potent inhibitory activity against S. aureus cell adhesion to
fibronectin. The fibronectin-binding activity data highlight the potential
of these compounds for the treatment of S. aureus infections via inhibition
of sortase activity.
Berberine Synergy with Amphotericin B against
Disseminated Candidiasis in Mice.
Han Y, Lee JH.
Biol Pharm Bull. 2005
Mar;28(3):541-4.
In present study, we investigated the synergic effect of berberine against
disseminated candidiasis caused by the pathogenic fungus, Candida albicans.
Berberine inhibited the growth of C. albicans under in-vitro condition. The
broth susceptibility revealed the synergic effect of berberine with
amphotericin B (Amp B). To confirm these results under the in-vivo
condition, the effect was examined in mice against disseminated candidiasis.
Results showed mice that were given diluent (negative control), Amp B (0.5
mg/kg of body weight), or berberine (1 mg/kg of body weight) had mean
survival times (MST) of approximately 12, 14, and 17 d, respectively. On the
contrary, mice that were treated using a combination of the two agents at
the same concentrations resulted in a MST value of 36 d, surviving at an
average of 22 d longer than the mice group treated only with the Amp B. This
MST value was almost same as MST value from the mice that were given four
times the Amp B dose. These data indicate that the combination of Amp B
and berberine could reduce approximately 75% of the Amp B dose, implying
that berberine indeed has synergy with Amp B against the disseminated
disease.
Inhibition of the bacterial surface protein anchoring transpeptidase sortase by isoquinoline alkaloids.
Kim SH, Shin DS, Oh MN, Chung SC, Lee JS, Oh KB.
Biosci Biotechnol Biochem. 2004 Feb;68(2):421-4.
The inhibitory activity of Coptis chinensis rhizome-derived material was evaluated against sortase, a bacterial surface protein anchoring transpeptidase, from Staphylococcus aureus ATCC 6538p and compared to that of four commercially available isoquinoline alkaloids. The biologically active constituent of C. chinensis extract was characterized as the isoquinoline alkaloid, berberine chloride, by spectral analysis. The isolate was a potent inhibitor of sortase, with an IC50 value of 8.7 microg/ml and had antibacterial activity against Gram-positive bacteria with a minimum inhibitory concentration (MIC) in the range of 50-400 microg/ml. Among the four isoquinoline alkaloids tested, berberine chloride had strong inhibitory activity. These results indicate that berberine is a possible candidate for the development of a bacterial sortase inhibitor.
Isoflavones as potentiators of antibacterial activity.
Morel C, Stermitz FR, Tegos G, Lewis K.
J Agric Food Chem. 2003 Sep 10;51(19):5677-9.
Isoflavones isolated from Lupinus argenteus were found to potentiate the antibacterial activity of alpha-linolenic acid, also found in the same plant. The isoflavones also potentiated the activity of the natural plant antibiotic berberine and the synthetic fluoroquinoline antibiotic norfloxacin. The isoflavones increased the uptake of berberine into Staphylococcus aureus cells, indicating that they may be inhibiting a multidrug resistance pump (MDR). Thus, L. argenteus contains a weak antibacterial and also MDR pump inhibitors, which increase its potency.
Antimicrobial constituents from goldenseal (the Rhizomes
of Hydrastis canadensis) against selected oral pathogens.
Hwang BY, Roberts SK, Chadwick LR, Wu CD, Kinghorn AD.
Planta Med. 2003 Jul;69(7):623-7.
Two new C-methyl flavonoids, 6,8-di- C-methylluteolin 7-methyl ether (1) and
6- C-methylluteolin 7-methyl ether (2), were isolated from a commercially
available sample of the roots of Hydrastis canadensis, along with seven
known compounds, berberine (3), beta-hydrastine (4), canadine (5),
canadaline (6), isocorypalmine (7), canadinic acid (8), and beta-sitosterol
3- O-beta- D-glucoside (9). The structures of the new compounds 1 and 2 were
elucidated on the basis of their spectral data including 1D and 2D NMR
techniques. Of these isolates, berberine (3) and, to a lesser extent, 1 and
2, showed antimicrobial activity when evaluated against the oral pathogens
Streptococcus mutans and Fusobacterium nucleatum. Berberine (3) exhibited an
additive antimicrobial effect when tested against S. mutans in combination
with 1.
Berberis aetnensis C. Presl. extracts: antimicrobial properties and interaction with ciprofloxacin.
Musumeci R, Speciale A, Costanzo R, Annino A, Ragusa S, Rapisarda A, Pappalardo MS, Iauk L.
Int J Antimicrob Agents. 2003 Jul;22(1):48-53.
Previous research showed that berberine-containing Berberis species synthesise the substances 5'-methoxyhydnocarpin-D (5'-MHC-D) and pheophorbide a, which have no antimicrobial activity but inhibit the expression of multidrug resistant efflux pumps (MDRs) in Staphylococcus aureus and potentiate the action of berberine. The MDR pumps extrude synthetic and natural antimicrobials from bacterial cells. We searched for these compounds in Berberis aetnensis C. Presl. (Berberidaceae), an endemic plant of the volcano Mount Etna. This work confirms the presence of pheophorbide a and permits us to hypothesise the presence of 5'-MHC-D in leaf extracts. In fact, the activity of ciprofloxacin was improved when two chromatographic fractions isolated from leaf extracts were added. These results are indicative of the presence of MDR pump inhibitors. Moreover, crude extracts were tested on several micro-organisms and showed antimicrobial activity mainly against Gram-positive bacteria and yeasts.
Giardiasis: pathophysiology and management.
Hawrelak, J.
Altern Med Rev. 2003 May;8(2):129-42.
Giardia, a common human parasite, can cause significant morbidity; however, natural medicine has great potential to influence the course of Giardia infection. The most beneficial way to treat giardiasis naturally may be through a combination approach, utilizing both nutritional interventions and phytotherapeutic agents. Nutritional intervention aims to reduce the acute symptoms of Giardia and help clear the infection. This can best be achieved by consuming a whole-food based, high-fiber, diet that is low in fat, lactose, and refined sugars. Additionally, ingestion of probiotics and wheat germ assists in parasite clearance. Numerous medicinal herbs show promise in the treatment of giardiasis. Berberine-containing herbs, garlic, and the Ayurvedic formulation Pippali rasayana currently have the most clinical evidence supporting their use. Blending the nutritional interventions and phytotherapeutic agents outlined in this article can minimize Giardia symptomatology and aid clearance of the parasite, without significant ill effects. As such, this therapeutic strategy should be considered the first-line approach. Antibiotic use may best be reserved for cases that fail to respond to initial treatment with natural measures.
In vitro antiplasmodial activity of antimalarial medicinal plants used in Vietnamese traditional medicine.
Tran QL, Tezuka Y, Ueda JY, Nguyen NT, Maruyama Y, Begum K, Kim HS, Wataya Y, Tran QK, Kadota S.
J Ethnopharmacol. 2003 Jun;86(2-3):249-52.
Among 42 extracts, prepared from 14 medicinal plants used in Vietnamese traditional medicine to treat malaria, 24 were found to have antiplasmodial activity by inhibiting the growth of the chloroquine-resistant Plasmodium falciparum strain FCR-3 with EC(50) values less than 10 microg/ml. Each medicinal plant possessed at least one active extract. The methanol extract of Coscinium fenestratum had the strongest antiplasmodial activity with EC(50) value of 0.5 microg/ml. Activity-guided fractionation led to identification of berberine as the major active constituent.
In vitro susceptibility of Helicobacter pylori to
isoquinoline alkaloids from Sanguinaria canadensis and Hydrastis canadensis.
Mahady GB, Pendland SL, Stoia A, Chadwick LR.
Phytother Res. 2003 Mar;17(3):217-21.
Methanol extracts of the rhizomes of Sanguinaria canadensis, and the roots
and rhizomes of Hydrastis canadensis, two plants used traditionally for the
treatment of gastrointestinal ailments, were screened for in vitro
antibacterial activity against 15 strains of Helicobacter pylori. The
rhizome extracts, as well as a methanol extract of S. canadensis
suspension-cell cultures inhibited the growth of H. pylori in vitro, with a
MIC50 range of 12.5-50.0 microg/ml. Three isoquinoline alkaloids were
identified in the active fraction. Sanguinarine and chelerythrine, two
benzophenanthridine alkaloids, inhibited the growth of the bacterium, with
an MIC50 of 50.0 and 100.0 microg/ml, respectively. Protopine, a protopine
alkaloid, also inhibited the growth of the bacterium, with a MIC50 of 100
microg/ml. The crude methanol extract of H. canadensis rhizomes was very
active, with an MIC50 of 12.5 microg/ml. Two isoquinoline alkaloids,
berberine and beta-hydrastine, were identified as the active constituents,
and having an MIC50 of 12.5 and 100.0 microg/ml, respectively.
Antimicrobial activity of berberine--a constituent of
Mahonia aquifolium.
Cernakova M, Kostalova D.
Folia Microbiol (Praha). 2002;47(4):375-8.
The antimicrobial activity of the protoberberine alkaloid, berberine, isolated from Mahonia aquifolium, was evaluated against 17 microorganisms including two Gram-negative bacteria--Pseudomonas aeruginosa and Escherichia coli (both resistant and sensitive), two Gram-positive bacteria--Bacillus subtilis and Staphylococcus aureus, Zoogloea ramigera, six filamentous fungi--Penicilium chrysogenum, Aspergillus niger, Aureobasidium pullulans (black and white strain), Trichoderma viride (original green strain and brown mutant), Fusarium nivale, Mycrosporum gypseum and two yeasts--Candida albicans and Saccharomyces cerevisiae. The IC50, minimum inhibitory concentration (MIC), minimum microbicidal concentration (MMC) and minimum microbistatic concentration (MMS) varied considerably depending on the microorganism tested, the sensitivity decreasing as follows: S. aureus > P. aeruginosa S (sensitive) > E. coli S > P. aeruginosa R (resistant) > E. coli R > B. subtilis > Z. ramigera > C. albicans > S. cerevisiae > A. pullulans B (black) > A. pullulans W (white) > T. viride Br (brown) > M. gypseum > A. niger > F. nivale > P. chrysogenum > T. viride G (green).
Multidrug Pump Inhibitors Uncover Remarkable Activity of Plant Antimicrobials
George Tegos, Frank R. Stermitz, Olga Lomovskaya, and Kim Lewis
Antimicro Agents and Chemo, Oct 2002, p. 3133-3141, Vol. 46, No. 10
Plant antimicrobials are not used as systemic antibiotics at present. The main reason for this is their low level of activity, especially against gram-negative bacteria. The reported MIC is often in the range of 100 to 1,000 µg/ml, orders of magnitude higher than those of common broad-spectrum antibiotics from bacteria or fungi. Major plant pathogens belong to the gram-negative bacteria, which makes the low level of activity of plant antimicrobials against this group of microorganisms puzzling. Gram-negative bacteria have an effective permeability barrier, comprised of the outer membrane, which restricts the penetration of amphipathic compounds, and multidrug resistance pumps (MDRs), which extrude toxins across this barrier. It is possible that the apparent ineffectiveness of plant antimicrobials is largely due to the permeability barrier. We tested this hypothesis in the present study by applying a combination of MDR mutants and MDR inhibitors. A panel of plant antimicrobials was tested by using a set of bacteria representing the main groups of plant pathogens. The human pathogens Pseudomonas aeruginosa, Escherichia coli, and Salmonella enterica serovar Typhimurium were also tested. The results show that the activities of the majority of plant antimicrobials were considerably greater against the gram-positive bacteria Staphylococcus aureus and Bacillus megaterium and that disabling of the MDRs in gram-negative species leads to a striking increase in antimicrobial activity. Thus, the activity of rhein, the principal antimicrobial from rhubarb, was potentiated 100- to 2,000-fold (depending on the bacterial species) by disabling the MDRs. Comparable potentiation of activity was observed with plumbagin, resveratrol, gossypol, coumestrol, and berberine. Direct measurement of the uptake of berberine, a model plant antimicrobial, confirmed that disabling of the MDRs strongly increases the level of penetration of berberine into the cells of gram-negative bacteria. These results suggest that plants might have developed means of delivering their antimicrobials into bacterial cells. These findings also suggest that plant antimicrobials might be developed into effective, broad-spectrum antibiotics in combination with inhibitors of MDRs.
Antibacterial activity of Hydrastis canadensis extract
and its major isolated alkaloids.
Scazzocchio F, Cometa MF, Tomassini L, Palmery M.
Planta Med. 2001 Aug;67(6):561-4.
The antibacterial activity of extract and isolated major alkaloids (berberine,
beta-hydrastine, canadine and canadaline) of Hydrastis canadensis L. (Ranunculaceae)
was evaluated against 6 strains of microorganism: Staphylococcus aureus (ATCC
25 993 and ATCC 6538P), Streptococcus sanguis (ATCC 10 556), Escherichia
coli (ATCC 25 922), Pseudomonas aeruginosa (ATCC 27 853). Bactericidal
activity was evaluated by contact test by measuring the "killing time" on a
low density bacterial inoculum, and bacteriostatic activity in liquid medium
by M.I.C. values. The results provide a rational basis for the
traditional antibacterial use of Hydrastis canadensis.
In search of natural substrates and inhibitors of MDR pumps.
Lewis K.
J Mol Microbiol Biotechnol. 2001 Apr;3(2):247-54.
The function of microbial MDRs remains a hotly debated
subject. Given the very broad substrate specificities of some MDRs, like the
RND pumps that can extrude all classes of amphipathic compounds (cationic,
neutral, and anionic), it seems difficult to develop a rationale for
pinpointing possible natural substrates of these translocases. At the same
time, several clues can be used to guide our search for natural MDR
substrates. One is the fact that amphipathic cations appear to be the
preferred substrates of MDRs. These substances are extruded by MDRs of all 5
known families and are the almost exclusive substrates of SMR and MF family
MDRs. The universal nature of amphipathic cations as MDR substrates suggests
that these were the substances that fueled the evolution of MDR pumps. Two
factors apparently favored this particular class of molecules for the role
of original MDR substrates--need and opportunity. Unlike other substances,
amphipathic cations accumulate in the cell driven by the membrane potential,
which makes cations potentially the most dangerous toxins. At the same time,
amphipathic cations are highly hydrated and do not permeate the membrane as
readily as neutral compounds, making it feasible to design a defense based
on an efflux pump. The paucity of known cationic (non-basic) antimicrobials
might be a result of using MDR-expressing microbial cells for antibiotic
discovery. Plant amphipathic cations, the berberine alkaloids, are good MDR
substrates. The Berberis plants produce 5'-methoxyhydnocarpin-D, an MDR
inhibitor that potentiates the action of berberine. It is suggested that the
further evolution of MDR pumps was determined largely by the barrier
function of the membrane they reside in. Thus Gram negative bacteria have an
outer membrane barrier that slows the penetration of virtually all
amphipathic molecules, and transenvelope MDRs of the RND and EmrAB-type
extrude their substrates across this barrier. A low permeability of the
cytoplasmic membrane of yeast similarly allows for the operation of
broad-specificity ABC and MF MDRs. The presence of MDR sensors that regulate
the expression of some MDR pumps strongly suggests that defense against
external toxins is the function of these MDRs. The BmrR transcriptional
activator of the MerR family induces expression of the Bmr pump in B.
subtilis and is a sensor specifically designed to recognize amphipathic
cations. Similarly, the OacR repressor binds chemically unrelated cations,
which leads to the expression of the QacA pump in S. aureus. In E. coli, the
EmrR sensor of the MarR repressor family binds unrelated neutral molecules,
allowing for expression of the transenvelope EmrAB pump.
Coptidis Rhizoma inhibits growth and proteases of oral
bacteria.
Hu JP, Takahashi N, Yamada T.
Oral Diseases (2000) 6, 297-302
OBJECTIVE: The aim of this study was to investigate
the antibacterial effect of Coptidis Rhizoma (CR), a traditional medicinal
plant, on oral bacteria. MATERIALS AND METHODS: CR extract was prepared by
boiling CR in water for 2 h. Alkaloids contained in CR extract were assayed
by high performance liquid chromatography (HPLC). Antibacterial activity of
CR extract was estimated from the lowest concentration that did not permit
bacterial growth (minimum inhibitory concentration, MIC) and the
concentrations that inhibited 50% of bacterial proteolytic activity (IC50).
RESULTS: CR extract inhibited the growth of Actinomyces naeslundii,
Porphyromonas gingivalis, Prevotella intermedia, Prevotella nigrescens and
Actinobacillus actinomycetemcomitans at MIC of 0.031-0.25 mg ml-1, whereas
it had less inhibitory effect (MIC: 0.5-2 mg ml-1) on the growth of
Streptococcus and Lactobacillus. The major active component of CR extract
was berberine (Ber), an alkaloid, and its inhibiting specificity to
bacterial growth was similar to that of CR extract. CR extract and Ber
were bacteriostatic at the MICs against most of the bacteria, and
bacteriocidal at the concentrations higher than the MICs. Ber inhibited the
activities of collagenase from P. gingivalis and A. actinomycetemcomitans.
CONCLUSION: CR extract and Ber had an inhibitory
effect on periodontopathogenic bacteria. These results suggest the
possibility of their clinical application for the treatment of periodontal
diseases.
Synergy in a medicinal plant: Antimicrobial action of berberine potentiated by 5'-methoxyhydnocarpin, a multidrug pump inhibitor
Frank R. Stermitz, Peter Lorenz, Jeanne N. Tawara, Lauren A. Zenewicz, and Kim Lewis
PNAS February 15, 2000 vol. 97 no. 4 1433-1437
Multidrug resistance pumps (MDRs) protect microbial cells from both synthetic and natural antimicrobials. Amphipathic cations are preferred substrates of MDRs. Berberine alkaloids, which are cationic antimicrobials produced by a variety of plants, are readily extruded by MDRs. Several Berberis medicinal plants producing berberine were found also to synthesize an inhibitor of the NorA MDR pump of a human pathogen Staphylococcus aureus. The inhibitor was identified as 5'-methoxyhydnocarpin (5'-MHC), previously reported as a minor component of chaulmoogra oil, a traditional therapy for leprosy. 5'-MHC is an amphipathic weak acid and is distinctly different from the cationic substrates of NorA. 5'-MHC had no antimicrobial activity alone but strongly potentiated the action of berberine and other NorA substrates against S. aureus. MDR-dependent efflux of ethidium bromide and berberine from S. aureus cells was completely inhibited by 5'-MHC. The level of accumulation of berberine in the cells was increased strongly in the presence of 5'-MHC, indicating that this plant compound effectively disabled the bacterial resistance mechanism against the berberine antimicrobial.
Inhibition of Candida rugosa lipase by berberine and structurally related alkaloids, evaluated by high-performance liquid chromatography.
Grippa E, Valla R, Battinelli L, Mazzanti G, Saso L, Silvestrini B.
Biosci Biotechnol Biochem. 1999 Sep;63(9):1557-62.
It is known that certain microorganisms produce extracellular lipase to better colonize the skin and mucosal surfaces. Since different extracts from medicinal plants have anti-lipase activity (Shimura et al., Biosci. Biotechnol. Biochem., 56: 1478-1479, 1992), we examined the effects of selected natural substances on Candida rugosa lipase. In the presence of the compounds under examination, the enzyme was incubated with beta-naphthyl laurate, and beta-naphthol, produced by the enzymatic reaction, was extracted with ethyl acetate and analyzed by reversed phase HPLC, using a C-18 column. Thus, the inhibitory activity was calculated by a proper formula based on the variations of the area under the chromatographic peak of beta-naphthol. The method was validated by analyzing substances with known anti-lipase activity such as saturated fatty acids (C10-16) and tetracycline. Berberine and a number of structurally related alkaloids such as chelidonine, chelerythrine, and sanguinarine appeared active. This property of berberine and sanguinarine is of interest because they are used in pathological conditions in which microbial lipases could play a pathogenic role.
Growth-inhibiting effects of Coptis japonica root-derived isoquinoline alkaloids on human intestinal bacteria.
Chae SH, Jeong IH, Choi DH, Oh JW, Ahn YJ.
J Agric Food Chem. 1999 Mar;47(3):934-8.
The growth-inhibiting activity of Coptis japonica (Makino) root-derived materials toward eight human intestinal bacteria was examined using an impregnated paper disk method and compared to that of four commercially available isoquinoline alkaloids [berberine sulfate (BS), berberine iodide (BI), palmatine chloride (PC), and palmatine sulfate(PS)], as well as that of Thea sinensis leaf-derived epigallocatechin gallate (EGCG). The biologically active constituents of the Coptis extract were characterized as the isoquinoline alkaloids berberine chloride (BC), palmatine iodide (PI), and coptisine chloride (CC) by spectral analysis. The growth responses varied with both chemical and bacterial strain used. In a test using 500 microg/disk, BC and PI produced a clear inhibitory effect against Bifidobacterium longum, Bifidobacterium bifidum, Clostridium perfringens, and Clostridium paraputrificum, whereas weak or no inhibition was observed in Bifidobacterium adolescentis, Lactobacillus acidophilus, Lactobacillus casei, and Escherichia coli. At 1000 microg/ disk, CC revealed weak or no growth inhibition toward all test bacteria, whereas EGCG exhibited weak growth inhibition against only C. perfringens and C. paraputrificum. Among various isoquinoline alkaloids, BC exhibited more potent inhibitory activity toward C. perfringens than BI and BS, whereas the inhibitory effect was more pronounced in PI compared to PC and PS.
Antitubercular natural products: berberine from the roots of commercial Hydrastis canadensis powder. Isolation of inactive 8-oxotetrahydrothalifendine, canadine, beta-hydrastine, and two new quinic acid esters, hycandinic acid esters-1 and -2.
Gentry EJ, Jampani HB, Keshavarz-Shokri A,
Morton MD, Velde DV, Telikepalli H, Mitscher LA, Shawar R, Humble D, Baker
W.
J Nat Prod. 1998 Oct;61(10):1187-93.
Berberine (4) is responsible for the activity of an extract of a commercial root sample of Hydrastis canadensis against multiply drug resistant Mycobacterium tuberculosis. Two new quinic acid feruloyl esters, compounds 2 and 3, have been isolated from the same source along with canadine (1c), 8-oxotetrahydrothalifendine (1), and beta-hydrastine (5). These were found to be inactive. The structures of the new compounds were elucidated from spectral (1H, 13C, HMQC, HMBC, and H-H COSY) and chemical evidences.
Antimicrobial properties of alkaloids from
Xanthorhiza simplicissima.
Okunade AL, Hufford CD, Richardson MD, Peterson JR, Clark AM.
J Pharm Sci. 1994 Mar;83(3):404-6.
The organic extract of the whole plant Xanthorhiza simplicissima was found to exhibit good activity against the AIDS-related opportunistic pathogens Candida albicans, Cryptococcus neoformans, and Mycobacterium intracellularae. Bioassay-directed fractionation of the extract led to the isolation of the known alkaloid berberine as the major active component. A second alkaloid of the isohomoprotoberberine family, puntarenine, was isolated from this plant family for the first time. Puntarenine also showed marginal activity against the dermatophytic fungus Trichophyton mentagrophytes and the yeast Saccharomyces cerevisiae.
Berberine, a potential drug for trachoma.
Khosla PK, Neeraj VI, Gupta SK, Satpathy G.
Rev Int Trach Pathol Ocul Trop Subtrop Sante Publique. 1992;69:147-65.
The clinical serological response to topical treatment of trachoma with Berberine an indigenous drug has been studied in 32 microbiologically confirmed cases. Efficacy of Berberine 0.2% when compared to sulfacetamide 20% was found to be superior in both the clinical course of trachoma and in achieving a fall in the serum antibody titers (P < 0.05) against chlamydia trachomatis in the treated patients.
Effects of crude drugs and berberine hydrochloride on the activities of fungi.
Nakamoto K, Sadamori S, Hamada T.
J Prosthet Dent. 1990 Dec;64(6):691-4.
The effects of crude drugs on fungi have been used for a thousand years in China and Japan. These drugs include: Saussureae radix, Magnoliae cortex, Cinnamomi cortex, Hydrangeae dulcis folium, and Artemisiae capillarius flos. The activity of Coptidis rhizoma and Phellodendri cortex was stronger than other crude drugs against the three fungi. Berberine hydrochloride, which is a component of the two crude drugs, was investigated. Minimal inhibitory concentration values of berberine hydrochloride were 1, 0.125, and 0.5 mg/ml against Candida albicans, C. tropicalis, and C. glabrata, respectively. In C. glabrata, compared with C. albicans and C. tropicalis, berberine hydrochloride greatly inhibited the growth of fungi.
Influence of berberine sulfate on synthesis and expression of Pap fimbrial adhesin in uropathogenic Escherichia coli.
Sun D, Abraham SN, Beachey EH.
Antimicrob Agents Chemother. 1988 Aug;32(8):1274-7.
We investigated the influence of berberine sulfate, an ancient Chinese antibiotic, upon the adhesion of uropathogenic Escherichia coli to erythrocytes and epithelial cells. Although berberine sulfate in increasing concentrations had no effect on bacterial growth or on the synthesis of major outer membrane proteins of the E. coli organisms, it increasingly blocked adhesion. The decreased adhesion was accompanied by a reduction in the synthesis of fimbrial subunits and in the expression of assembled fimbriae. These results suggest that the anti-infectious activity of berberine sulfate in E. coli-induced urinary tract infections may be mediated by the selective suppression of the synthesis and assembly of fimbriae by uropathogenic organisms.
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