1.Phosphagen Kinases of Parasites: Unexplored Chemotherapeutic Targets.
Blanca R JARILLA ; Takeshi AGATSUMA
The Korean Journal of Parasitology 2010;48(4):281-284
Due to the possible emergence of resistance and safety concerns on certain treatments, development of new drugs against parasites is essential for the effective control and subsequent eradication of parasitic infections. Several drug targets have been identified which are either genes or proteins essential for the parasite survival and distinct from the hosts. These include the phosphagen kinases (PKs) which are enzymes that play a key role in maintenance of homeostasis in cells exhibiting high or variable rates of energy turnover by catalizing the reversible transfer of a phosphate between ATP and naturally occurring guanidine compounds. PKs have been identified in a number of important human and animal parasites and were also shown to be significant in survival and adaptation to stress conditions. The potential of parasite PKs as novel chemotherapeutic targets remains to be explored.
Animals
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Antiparasitic Agents/*pharmacology
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Humans
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Parasites/*enzymology
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Phosphotransferases/*antagonists & inhibitors
2.Advances in studies on chemical constituents and biological activities of Lawsonia inermis.
Qian LI ; Wen-Qin GAO ; Yu-Qing ZHAO
China Journal of Chinese Materia Medica 2013;38(6):795-799
Lawsonia inermis is a single-species genus of the Lythraceae family, its leaves, stem bark, roots, flowers and seeds have been used in traditional medicine. It has been paid more attention by scholars from many countries because of their various types of compounds and significant physiological activities. The plant is reported to contain quinones, phenylpropanoids, flavonoids, terpenoids, phenolic compounds and fatty acids. Modern pharmacological studies have demonstrated that the plant performs antimicrobial, antioxidant, anticancer and antiparasitic activity. This article mainly summarizes the research advances of chemical constituents and biological activities of Lawsonia inermis, for its further development and utilization.
Anti-Infective Agents
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chemistry
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pharmacology
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Antineoplastic Agents
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chemistry
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pharmacology
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Antioxidants
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chemistry
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pharmacology
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Antiparasitic Agents
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chemistry
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pharmacology
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Drugs, Chinese Herbal
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chemistry
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pharmacology
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Humans
;
Lawsonia Plant
;
chemistry
3.Therapeutic Potential of Myrrh and Ivermectin against Experimental Trichinella spiralis Infection in Mice.
Maha M A BASYONI ; Abdel Aleem A EL-SABAA
The Korean Journal of Parasitology 2013;51(3):297-304
Trichinosis is a parasitic zoonosis caused by the nematode Trichinella spiralis. Anthelmintics are used to eliminate intestinal adults as well as tissue-migrating and encysted larvae. This study aimed to investigate the effects of ivermectin and myrrh obtained from the aloe-gum resin of Commiphora molmol on experimental trichinosis. Ninety albino mice were orally infected with 300 T. spiralis larvae. Drugs were tested against adult worms at day 0 and day 5 and against encysted larvae on day 15 and day 35 post-infection (PI). Mature worms and encysted larvae were counted in addition to histopathological examination of muscle specimens. Serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), total protein, albumin, globulin, urea, and creatinine values were estimated. Significant reductions in mean worm numbers were detected in ivermectin treated mice at day 0 and day 5 PI achieving efficacies of 98.5% and 80.0%, while efficacies of myrrh in treated mice were 80.7% and 51.5%, respectively. At days 15 and 35 post-infection, ivermectin induced significant reduction in encysted larval counts achieving efficacies of 76.5% and 54.0%, respectively, while myrrh efficacies were 76.6% and 35.0%, respectively. AST, ALT, urea, and creatinine levels were reduced, while total proteins were increased in response to both treatments compared to their values in the infected non-treated mice. Ivermectin use for controlling T. spiralis could be continued. Myrrh was effective and could be a promising drug against the Egyptian strains of T. spiralis with results nearly comparable to ivermectin.
Animals
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Antiparasitic Agents/administration & dosage/*pharmacology
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Drug Therapy, Combination
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Ivermectin/administration & dosage/*pharmacology
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Mice
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Terpenes/administration & dosage/*pharmacology
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*Trichinella spiralis
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Trichinellosis/*drug therapy
4.Plant-based Rasayana drugs from Ayurveda.
Subramani Paranthaman BALASUBRAMANI ; Padma VENKATASUBRAMANIAN ; Subrahmanya Kumar KUKKUPUNI ; Bhushan PATWARDHAN
Chinese journal of integrative medicine 2011;17(2):88-94
Rasayana tantra is one of the eight specialties of Ayurveda. It is a specialized practice in the form of rejuvenative recipes, dietary regimen, special health promoting behaviour and drugs. Properly administered Rasayana can bestow the human being with several benefits like longevity, memory, intelligence, freedom from diseases, youthful age, excellence of luster, complexion and voice, optimum strength of physique and sense organs, respectability and brilliance. Various types of plant based Rasayana recipes are mentioned in Ayurveda. Review of the current literature available on Rasayanas indicates that anti-oxidant and immunomodulation are the most studied activities of the Rasayana drugs. Querying in Pubmed database on Rasayanas reveals that single plants as well as poly herbal formulations have been researched on. This article reviews the basics of Rasayana therapy and the published research on different Rasayana drugs for specific health conditions. It also provides the possible directions for future research.
Animals
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Anti-Ulcer Agents
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pharmacology
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therapeutic use
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Antineoplastic Agents, Phytogenic
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pharmacology
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therapeutic use
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Antiparasitic Agents
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pharmacology
;
therapeutic use
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Aphrodisiacs
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pharmacology
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therapeutic use
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Free Radical Scavengers
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pharmacology
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therapeutic use
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Giardiasis
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drug therapy
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Herbal Medicine
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classification
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methods
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trends
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Humans
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Immunologic Factors
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pharmacology
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therapeutic use
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Medicine, Ayurvedic
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Models, Biological
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Neuroprotective Agents
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pharmacology
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therapeutic use
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Plant Preparations
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classification
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therapeutic use
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Radiation-Protective Agents
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pharmacology
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therapeutic use
5.In vitro anti-leishmanial activity of methanolic extracts of Calendula officinalis flowers, Datura stramonium seeds, and Salvia officinalis leaves.
Banafsheh NIKMEHR ; Habib GHAZNAVI ; Amir RAHBAR ; Samira SADR ; Saeed MEHRZADI
Chinese Journal of Natural Medicines (English Ed.) 2014;12(6):423-427
AIM:
The anti-leishmanial activity of methanolic extracts of Calendula officinalis flowers, Datura stramonium seeds, and Salvia officinalis leaves against extracellular (promastigote) and intracellular (amastigote) forms of Leishmania major were evaluated in this study.
METHOD:
In the first stage, promastigote forms of L. major, were treated with different doses of the plant extracts in a 96-well tissue-culture microplate and IC50 values for each extract were measured with colorimetric MTT assay. In the second stage, macrophage cells were infected with L. major promastigotes. Infected macrophages were treated with plant extracts. Then the macrophages were stained with Gimsa and the number of infected macrophages and amastigotes were counted with a light microscope.
RESULTS:
The results indicated that the plant extracts inhibited the growth of promastigotes and amastigotes of L. major. Inhibitory concentrations (IC50) for promastigote assay were 108.19, 155.15, and 184.32 μgmL(-1) for C. officinalis flowers, D. stramonium seeds and S. officinalis, respectively. The extracts also reduced the number of amastigotes in macrophage cells from 264 for control group to 88, 97, and 102 for test groups. Although the anti-leishmanial activity of the extracts were not comparable with the standard drug, miltefosine; but they showed significant efficiency in reducing the number of amastigotes in macrophages, in comparison with the control group (P < 0.001). These plant extracts had lower toxicity compared with miltefosine.
CONCLUSION
This study demonstrates the potential efficacy of the methanolic extracts of C. officinalis flowers, D. stramonium seeds, and S. officinalis leaves to control of cutaneous leishmaniasis.
Antiparasitic Agents
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pharmacology
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therapeutic use
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Calendula
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Cell Line
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Datura stramonium
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Flowers
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In Vitro Techniques
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Leishmania major
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drug effects
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Leishmaniasis
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drug therapy
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parasitology
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Macrophages
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drug effects
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parasitology
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Phytotherapy
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Plant Extracts
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pharmacology
;
therapeutic use
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Plant Leaves
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Salvia officinalis
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Seeds
6.Afatinib Reduces STAT6 Signaling of Host ARPE-19 Cells Infected with Toxoplasma gondii.
Zhaoshou YANG ; Hye Jin AHN ; Young Hoon PARK ; Ho Woo NAM
The Korean Journal of Parasitology 2016;54(1):31-38
Specific gene expressions of host cells by spontaneous STAT6 phosphorylation are major strategy for the survival of intracellular Toxoplasma gondii against parasiticidal events through STAT1 phosphorylation by infection provoked IFN-γ. We determined the effects of small molecules of tyrosine kinase inhibitors (TKIs) on the growth of T. gondii and on the relationship with STAT1 and STAT6 phosphorylation in ARPE-19 cells. We counted the number of T. gondii RH tachyzoites per parasitophorous vacuolar membrane (PVM) after treatment with TKIs at 12-hr intervals for 72 hr. The change of STAT6 phosphorylation was assessed via western blot and immunofluorescence assay. Among the tested TKIs, Afatinib (pan ErbB/EGFR inhibitor, 5 µM) inhibited 98.0% of the growth of T. gondii, which was comparable to pyrimethamine (5 µM) at 96.9% and followed by Erlotinib (ErbB1/EGFR inhibitor, 20 µM) at 33.8% and Sunitinib (PDGFR or c-Kit inhibitor, 10 µM) at 21.3%. In the early stage of the infection (2, 4, and 8 hr after T. gondii challenge), Afatinib inhibited the phosphorylation of STAT6 in western blot and immunofluorescence assay. Both JAK1 and JAK3, the upper hierarchical kinases of cytokine signaling, were strongly phosphorylated at 2 hr and then disappeared entirely after 4 hr. Some TKIs, especially the EGFR inhibitors, might play an important role in the inhibition of intracellular replication of T. gondii through the inhibition of the direct phosphorylation of STAT6 by T. gondii.
Antiparasitic Agents/pharmacology
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Blotting, Western
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Cell Line
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Enzyme Activation/drug effects
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Fluorescent Antibody Technique
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Humans
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Janus Kinase 1/metabolism
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Janus Kinase 3/metabolism
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Phosphorylation/drug effects
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Quinazolines/*pharmacology
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STAT6 Transcription Factor/*metabolism
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Signal Transduction/*drug effects
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Toxoplasma/*drug effects/physiology
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Toxoplasmosis/physiopathology