scholarly journals Phenylpropanoids and Furanocoumarins as Antibacterial and Antimalarial Constituents of the Bhutanese Medicinal Plant Pleurospermum amabile

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900
Author(s):  
Phurpa Wangchuk ◽  
Stephen G. Pyne ◽  
Paul A. Keller ◽  
Malai Taweechotipatr ◽  
Sumalee Kamchonwongpaisan
Keyword(s):  
Antibacterial Activity ◽  
Plasmodium Falciparum ◽  
Bacillus Subtilis ◽  
Medicinal Plant ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Multidrug Resistant ◽  
Scientific Data ◽  
Methyl Eugenol ◽  
Weak Antibacterial Activity

With the objective of determining safety and verifying the traditional uses of the Bhutanese medicinal plant, Pleurospermum amabile Craib & W. W. Smith, we investigated its crude extracts and the isolated phytochemicals for their biological activities. Four phenylpropanoids [( E)-isomyristicin (1), ( E)-isoapiol (2), methyl eugenol (3) and ( E)-isoelemicin (4)] and six furanocoumarins [psoralen (5), bergapten (6), isoimperatorin (7), isopimpinellin (8), oxypeucedanin hydrate (9) and oxypeucedanin methanolate (10)] were isolated from this plant. Among the test samples, compound 10 showed weak antibacterial activity against Bacillus subtilis and best antimalarial activity against the Plasmodium falciparum strains, TM4/8.2 (chloroquine and antifolate sensitive) and K1CB1 (multidrug resistant). None of the test samples showed cytotoxicity. This study generated scientific data that support the traditional medical uses of the plant.

scholarly journals GC/GC-MS Analysis, Isolation and Identification of Bioactive Essential Oil Components from the Bhutanese Medicinal Plant, Pleurospermum Amabile

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Phurpa Wangchuk ◽  
Paul A. Keller ◽  
Stephen G. Pyne ◽  
Malai Taweechotipatr ◽  
Sumalee Kamchonwongpaisan
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Medicinal Plant ◽  
Multidrug Resistant ◽  
Methyl Eugenol ◽  
Nmr Analysis ◽  
Isolation And Identification ◽  
Aerial Parts ◽  
Ms Analysis ◽  
Oil Components

We have hydrodistilled the essential oil (EO) from the aerial parts of the Bhutanese medicinal plant, Pleurospermum amabile using a Clevenger apparatus and evaluated this EO by GC/GC-MS and NMR analysis followed by testing for bioactivity. The GC-MS analysis identified 52 compounds with ( E)-isomyristicin as a major component (32.2%). Repeated purification yielded four compounds; ( E)-isomyristicin (1), ( E)-isoapiol (2), methyl eugenol (3) and ( E)-isoelemicin (4). Compound 2 and the mother EO showed the best antiplasmodial activity against the Plasmodium falciparum strains, TM4/8.2 (chloroquine and antifolate sensitive) and K1CB1 (multidrug resistant). They exhibited mild antibacterial activity against Bacillus subtilis. None of the test samples showed cytotoxicity.

scholarly journals Antibacterial Activity and Flavonoids Content of Artemisia cina Berg. ex Poljakov Ethyl Acetate Extracts

2021 ◽  
Vol 13 (1) ◽  
pp. 106-112
Author(s):  
Sri Kasmiyati ◽  
Elizabeth Betty Elok Kristiani ◽  
Maria Marina Herawati ◽  
Andreas Binar Aji Sukmana
Keyword(s):  
Antibacterial Activity ◽  
Medicinal Plant ◽  
Ethyl Acetate ◽  
Biological Activities ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Flavonoid Content ◽  
Gram Positive ◽  
Gram Negative ◽  
Significant Difference

The medicinal plant-derived bioactive compounds have a potential for many biological activities, including antimicrobial activity. Artemisia cina is a medicinal plant from the Compositae family with the potential of having antitumor, antifungal, and antibacterial activity. This study aimed to determine the antibacterial activity and the flavonoid content of A. Cina’s ethyl acetate extract. Plants samples were extracted by ethyl acetate maceration method. Antibacterial activity was tested against Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) by a disk diffusion method using 25, 50, and 100 mg/l extract concentrations. The flavonoid contents (quercetin and kaempferol) were measured using High-Performance Liquid Chromatography. The extracts of diploid and polyploid A. cina displayed some antibacterial activity, with the Gram-negative bacteria being more resistant than the Gram-positive counterpart. However, no significant difference was observed between the diploid and polyploid extracts. As for the flavonoid content, the highest quercetin content (0.5501 mg/ml) was found in the polyploid A. cina (J), while the highest kaempferol content (0.5818 mg/ml) was observed in the diploid A. cina (KJT). Although A. cina is widely grown in Indonesia, compared to other Artemisia species, A. cina has not been widely studied, especially its antibacterial  potential and in related to its flavonoid content and the use of ethyl acetate as the extraction solvent.  This study reveals the potential of A. cina as a natural antibacterial agent. 

scholarly journals The Antibacterial Assay of Tectorigenin with Detergents or ATPase Inhibitors against Methicillin-ResistantStaphylococcus aureus

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Dae-Ki Joung ◽  
Su-Hyun Mun ◽  
Kuang-Shim Lee ◽  
Ok-Hwa Kang ◽  
Jang-Gi Choi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Multidrug Resistant ◽  
Transmission Electron ◽  
Antibacterial Assay ◽  
Atpase Inhibitors ◽  
Resistant Strains ◽  
Activity Mechanism ◽  
Triton X

Tectorigenin (TTR) is an O-methylated isoflavone derived from the rhizome ofBelamacanda chinensis(L.) DC. It is known to perform a wide spectrum of biological activities such as antioxidant, anti-inflammatory, anti-tumor. The aim of this study is to examine the mechanism of antibacterial activity of TTR against methicillin-resistantStaphylococcus aureus(MRSA). The anti-MRSA activity of TTR was analyzed in combination assays with detergent, ATPase inhibitors, and peptidoglycan (PGN) derived fromS. aureus. Transmission electron microscopy (TEM) was used to monitor survival characteristics and changes inS. aureusmorphology. The MIC values of TTR against all the tested strains were 125 μg/mL. The OD(600) of each suspension treated with a combination of Triton X-100, DCCD, and NaN3with TTR (1/10 × MIC) had been reduced from 68% to 80%, compared to the TTR alone. At a concentration of 125 μg/mL, PGN blocked antibacterial activity of TTR. This study indicates that anti-MRSA action of TTR is closely related to cytoplasmic membrane permeability and ABC transporter, and PGN at 125 μg/mL directly bind to and inhibit TTR at 62.5 μg/mL. These results can be important indication in study on antimicrobial activity mechanism against multidrug resistant strains.

scholarly journals Plasmodium falciparum-Based Bioassay for Measurement of Artemisinin Derivatives in Plasma or Serum

2004 ◽  
Vol 48 (3) ◽  
pp. 954-960 ◽  
Author(s):  
Paktiya Teja-Isavadharm ◽  
James O. Peggins ◽  
Thomas G. Brewer ◽  
Nicholas J. White ◽  
H. Kyle Webster ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
High Performance ◽  
Antimalarial Activity ◽  
Drug Susceptibility ◽  
Multidrug Resistant ◽  
Response Curves ◽  
Artemisinin Derivatives ◽  
Treatment Regimens ◽  
Limit Of Quantitation

ABSTRACT Artemisinin and its derivatives, artesunate and artemether, are rapidly acting antimalarials that are used for the treatment of severe and uncomplicated multidrug-resistant falciparum malaria. To optimize treatment regimens that use this new class of antimalarials, there is a need for readily available and reproducible assays to monitor drug levels closely in patients. A sensitive and reproducible bioassay for the measurement of the concentrations of artemisinin derivatives in plasma and serum is described. By modifying the in vitro drug susceptibility test, it was found that antimalarial activity in plasma or serum containing an unknown concentration of drug could be equated to the known concentrations of dihydroartemisinin (DHA) required to inhibit parasite growth. Dose-response curves for a Plasmodium falciparum clone (clone W2) and DHA were used as a standard for each assay. Assays with plasma or serum spiked with DHA proved to be reproducible (coefficient of variation, ≤10.9%), with a lower limit of quantitation equivalent to 2.5 ng of DHA per ml. For plasma spiked with artesunate or artemether, there was good agreement of the results obtained by the bioassay and the concentrations measured by high-performance liquid chromatography (HPLC) with electrochemical detection. The bioassay for measurement of the antimalarial activities of artemisinin derivatives in body fluids requires a smaller volume of plasma or serum and is more sensitive than the presently available HPLC methods, can provide pharmacodynamic parameters for determination of activity against the parasite, and should enhance the design of more appropriate dosage regimens for artemisinin drugs.

scholarly journals Ribofuranose as a carrier of tetraoxane and 4-aminoquinoline antimalarial pharmacophores

2008 ◽  
Vol 73 (11) ◽  
pp. 1021-1025 ◽  
Author(s):  
Igor Opsenica ◽  
Kirsten Smith ◽  
Lucia Gerena ◽  
Sandra Gaica ◽  
Bogdan Solaja
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Carrier Molecule

Several tetraoxane and 4-aminoquinoline molecules were prepared in order to examine the influence of ribofuranose as a carrier molecule on the antimalarial activity of test compounds. The synthesized compounds showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. The aminoquinoline derivative 4 was more active against W2 and TM91C235 strains than the control compounds (CQ and MFQ).

scholarly journals ComparativeEx VivoActivity of Novel Endoperoxides in Multidrug-Resistant Plasmodium falciparum and P. vivax

2012 ◽  
Vol 56 (10) ◽  
pp. 5258-5263 ◽  
Author(s):  
Jutta Marfurt ◽  
Ferryanto Chalfein ◽  
Pak Prayoga ◽  
Frans Wabiser ◽  
Grennady Wirjanata ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Ex Vivo ◽  
Drug Susceptibility ◽  
Multidrug Resistant ◽  
Intrinsic Activity ◽  
Drug Resistant ◽  
The Novel ◽  
Content Type ◽  
Artemisinin Derivatives

ABSTRACTThe declining efficacy of artemisinin derivatives againstPlasmodium falciparumhighlights the urgent need to identify alternative highly potent compounds for the treatment of malaria. In Papua Indonesia, where multidrug resistance has been documented against bothP. falciparumandP. vivaxmalaria, comparativeex vivoantimalarial activity againstPlasmodiumisolates was assessed for the artemisinin derivatives artesunate (AS) and dihydroartemisinin (DHA), the synthetic peroxides OZ277 and OZ439, the semisynthetic 10-alkylaminoartemisinin derivatives artemisone and artemiside, and the conventional antimalarial drugs chloroquine (CQ), amodiaquine (AQ), and piperaquine (PIP).Ex vivodrug susceptibility was assessed in 46 field isolates (25P. falciparumand 21P. vivax). The novel endoperoxide compounds exhibited potentex vivoactivity against both species, but significant differences in intrinsic activity were observed. Compared to AS and its active metabolite DHA, all the novel compounds showed lower or equal 50% inhibitory concentrations (IC50s) in both species (median IC50s between 1.9 and 3.6 nM inP. falciparumand 0.7 and 4.6 nM inP. vivax). The antiplasmodial activity of novel endoperoxides showed different cross-susceptibility patterns in the twoPlasmodiumspecies: whereas theirex vivoactivity correlated positively with CQ, PIP, AS, and DHA inP. falciparum, the same was not apparent inP. vivax. The current study demonstrates for the first time potent activity of novel endoperoxides against drug-resistantP. vivax. The high activity against drug-resistant strains of bothPlasmodiumspecies confirms these compounds to be promising candidates for future artemisinin-based combination therapy (ACT) regimens in regions of coendemicity.

In vitro antimalarial activity of medicinal plant extracts against Plasmodium falciparum

2010 ◽  
Vol 108 (1) ◽  
pp. 15-22 ◽  
Author(s):  
Asokan Bagavan ◽  
Abdul Abdul Rahuman ◽  
Naveen Kumar Kaushik ◽  
Dinkar Sahal
Keyword(s):  
Plasmodium Falciparum ◽  
Medicinal Plant ◽  
Plant Extracts ◽  
Antimalarial Activity ◽  
Medicinal Plant Extracts

Synthesis of Metal Complexes of Primaquine and In-vitro Antimalarial Evaluation Against Plasmodium falciparum

2020 ◽  
Vol 15 (6) ◽  
pp. 631-636
Author(s):  
Rimmy Nandal ◽  
Aakash Deep ◽  
Ishwar Singh ◽  
Meenakshi Kaushik ◽  
Hoti S. L. ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Metal Complexes ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Supportive Therapy ◽  
Sufficient Information ◽  
Standard Drug ◽  
Parasite Plasmodium Falciparum ◽  
Relationship Of

Background: Resistance to malarial drugs represents a major obstacle in the treatment of disease, thereby increasing the need for more efficient drugs. The development of metal complexes offers the medicinal chemist an opportunity to expand the activity of drugs. For providing supportive therapy to the host to boost its immune system several new antimalarial drugs are being beneath research, but sufficient information on their efficacy is yet not available. Methods: In view of above, eight drug metal complexes (Ba (II), Ca (II), Zn (II), St (II), Hg (II), Fe (III), Cu (II), Ni (II) of Sulfamethoxazole (SMX) and Primaquine were synthesized and in-vitro evaluated for their antimalarial activity against malaria parasite Plasmodium falciparum by using fluorescence based assay. Result: The antimalarial activity of Nickel (EC50= 1.41µM) and Zinc (EC50=0.96µM) complexes have shown tremendous activity as compared to the standard drug Primaquine (EC50=0.07µM). The structures of all these newly synthesized derivatives were confirmed by spectral data (IR, 1H NMR, 13C NMR and Mass spectrometry). Conclusion: In conclusion, this study describes that the preparation and antimalarial evaluation of metal complexes of primaquine and sulphamethoxazole. Evaluation of their possible biological activities such as antimalarial activity was carried out and most of the synthesized compounds (Nickel and Zinc metal complexes) showed the good activity as compared to the standard drug primaquine. Therefore the compounds are appropriate candidates for more investigation and some more derivatives can be synthesized to get an imminent into the structure activity relationship of these compounds to be employed as biologically useful agents.

scholarly journals On peroxide antimalarials

2007 ◽  
Vol 72 (12) ◽  
pp. 1181-1190 ◽  
Author(s):  
Igor Opsenica ◽  
Dejan Opsenica ◽  
Milka Jadranin ◽  
Kirsten Smith ◽  
Wilbur Milhous ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Natural Product ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Activity Relationship ◽  
Similar Activity ◽  
Structure Activity ◽  
Relationship Of ◽  
Insight Into ◽  
Better Than

Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized.

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