• Asian Pacific Journal of Cancer Prevention
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• 제17권3호
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• pp.1571-1576
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• 2016

Alteration of the acetylation status of chromatin and other non-histone proteins by HDAC inhibitors has evolved as an excellent epigenetic strategy in treatment of cancers. The present study was sought to identify compounds with positive pharmacological profiles targeting HDAC1. Analogues of Vorinostat synthesized by Cai et al, 2015 formed the test compounds for the present pharmacological evaluation. Hydroxamte analogue 6H showed superior pharmacological profile in comparison to all the compounds in the analogue dataset owing to its better electrostatic interactions and hydrogen bonding patterns. In order to identify compounds with even better high affinity and pharmacological profile than 6H and Vorinostat, virtual screening was performed. A total of 83 compounds similar to Vorinostat and 154 compounds akin to analogue 6H were retrieved. SCHEMBL15675695 (PubCid: 15739209) and AKOS019005527 (PubCid: 80442147) similar to Vorinostat and 6H, were the best docked compounds among the virtually screened compounds. However, in spite of having good affinity, none of the virtually screened compounds had better affinity than that of 6H. In addition SCHEMBL15675695 was predicted to be a carcinogen while AKOS019005527 is Ames toxic. From, our extensive analysis involving binding affinity analysis, ADMET properties predictions and pharmacophoric mappings, we report Vorinostat hydroxamate analogue 6H to be a potential candidate for HDAC inhibition in treatment of cancers through an epigenetic strategy.

• 셀메드
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• 제10권2호
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• pp.11.1-11.14
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• 2020

Nigella sativa commonly known as Black seed, Black cumin or Kalonji (Family Ranunculaceae) is a widely used for its miraculous healing power. Use of N. sativa seeds and oil has splendid historical past in diverse traditional systems of medicine and food. In Tibb-e-Nabwi (Prophetic Medicine), it is considered as one of the greatest forms of healing medicine. Phytochemically; it contains fixed oil, protein, alkaloids saponin and essential oil. Therapeutic properties of this plant are due to the presence of thymoquinone which is one of major active component and has different beneficial properties. In Unani System of Medicine the diseases are treated with nontoxic herbal drugs. As per Unani classical literature N. sativa perform various pharmacological actions like carminative, anti-inflammatory, analgesic, diuretic, emmenagogue, galactagogue, expectorant etc. Ample of phytochemical, pharmacological and clinical researches has been executed on N. sativa., which may include antidiabetic, anticancer, immunomodulator, analgesic, antimicrobial, anti-inflammatory, bronchodilator, hepato-protective, renal protective, gastro-protective, antioxidant properties, etc. This review is an effort to summarize the literature on scientific researches of pharmacognostical characteristics, chemical composition and pharmacological activities of the kalonji seeds

• International Journal of Oral Biology
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• 제33권1호
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• pp.1-5
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• 2008

Adenosine 5'-triphosphate (ATP) is an important extracellular signaling molecule which is involved in a variety of physiological responses in many different tissues and cell types, by acting at P2 receptors, either ionotropic (P2X) or G protein-coupled metabotropic receptors (P2Y). P2X receptors have seven isoforms designated as $P2X_{1^-}P2X_7$. In this study, we investigated the electrophysiological and pharmacological properties of rat $P2X_{1^-}P2X_4$ currents by using whole-cell patch clamp technique in a heterologous expression system. When ATP-induced currents were analyzed in human embryonic kidney (HEK293) cells following transient transfection of rat $P2X_{1^-}P2X_4$, the currents showed different pharmacological and electrophysiological properties. ATP evoked inward currents with fast activation and fast desensitization in $P2X_{^1-}$ or $P2X_{3^-}$ expressing HEK293 cells, but in $P2X_{2^-}$ or $P2X_{4^-}$ expressing HEK293 cells, ATP evoked inward currents with slow activation and slow desensitization. While PPADS and suramin inhibited $P2X_2$ or $P2X_3$ receptor-mediated currents, they had little effects on $P2X_4$ receptor-mediated currents. Ivermectin potentiated and prolonged $P2X_4$ receptor-mediated currents, but did not affect $P2X_2$ or $P2X_3$ receptor-mediated currents. We suggest that distinct pharmacological and electrophysiological properties among P2X receptor subtypes would be a useful tool to determine expression patterns of P2X receptors in the nervous system including trigeminal sensory neurons and microglia.

• 한국한의학연구원논문집
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• 제14권1호
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• pp.123-128
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• 2008

Glehnia littoralis (Umbelliferae), a perennial herb distributed along the coastline of northern Pacific countries, is the medicinal plant used traditionally for treatment of various diseases. This review focuses on the various pharmacological activities of Glehnia littoralis for understanding about its traditional medicinal applications, medicinal uses in the modern society, and potentials for drug development Glehnia littoralis was reported to have anti-oxidant, anti-tumor, anti-amnesic, blood circulation-promoting, immunomodulatory, anti-microbial, and allelopathic activities. However, their mechanisms remain to be clarified. Because Glehnia littoralis has been prescribed in traditional Oriental medicine as a tonic herb, Glehnia littoralis can be better than other chemical drugs and medicines which exert the equal pharmacological activities. Although the activities of Glehnia littoralis are not specifically high-potent with unique mode of action, it may turn out that it can be beneficial to exert multiple pharmacological activities. In view of low toxicity, relative cheapness, presence in the diet, and occurrence in various herbal remedies of Glehnia littoralis, it needs to be prudent to evaluate its properties and applications further.

• 셀메드
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• 제9권4호
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• pp.3.1-3.6
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• 2019

Melissa parviflora Benth. is an aromatic perennial herb of Lamiaceae family. It is one of the most influencial plant and used from centuries in Unani system of medicine for the treatment of various malady such as Epilepsy (mirgi), hemiplegia (falij), migraine (shaqeeqa), insomnia (sehar), indigestion (sue hazm) and palpitation (khafqaan) etc. The Persian physician Avicenna endorsed it for heart problems. It has antitubercular, antipyretic, analgesic and stomachic properties, also used to remove bad breath from mouth, strengthen the gums but its main action is as a tranquillizer and nervine relaxant, it is greatly esteemed for its calming properties. Preliminary performed phytochemical analysis revealed that tannin, flavonoid and saponins are the major components of the plant extract. The plants containing saponins or flavonoids exhibit anticonvulsant activity whereas the flavonoids show various biological activities including antioxidant, anti-inflammatory and cytotoxic-antitumor etc. Keeping in view the tremendous medicinal importance of the plant Badranjboya in Unani Medicine, this review provides updated information on its phytochemistry, therapeutic uses and pharmacological properties.

• 한국어병학회지
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• 제4권1호
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• pp.49-57
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• 1991

• 생약학회지
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• 제22권3호
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• pp.145-155
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• 1991

Peroxides in natural products have been recently received a considerable attention due to their various biological and pharmacological properties. Nearly 300 peroxides have been isolated and structually characterized from natural sources, mainly as constituents of Compositae and marine sponge, and occur randomly in about 10 other plant families. Among peroxides studied, sesquiterpene endoperoxide, quinghaosu, has been already clinically applied as a new antimalarial drug. Based on the peroxides reported, structural classification, natural distribution and biological and pharmacological activities are reviewed. Color reagent and spectroscopic identification of peroxide are also described.

• Archives of Pharmacal Research
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• 제12권1호
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• pp.22-25
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• 1989

Ethylacetate fraction from Orobanche crenata, contained two phenylpropanoid glycosides, exhibited some pharmacological properties. It was found to be non-toxic to rats in oral doses up to 500mg/100gm body weight. In large doses, it lowered the arterial blood pressure of anaethetised rats, and produced significant analgesic effect in mice and diuretic effect in rats. It further showed smooth muscle relaxant and antispasmodic effects in the isolated rabbit intestine and guinea-pig ileum respectively.

• Biomolecules & Therapeutics
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• 제6권2호
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• pp.159-164
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• 1998

General pharmacological properties of recombinant human parathyroid hormone (hPTH) were examined. The administration of hPTH (7, 35 and 175 lU/kg sc) in mice had no effects in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazol solution. hPTH (9 and 44 lU/kg, sc) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration, and it did not influence the responses produced by injection of acetylcholine or epinephrine. It showed no direct effect at 4.4$\times$10$_{-2}$IU/ml in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also showed no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence intestinal propulsion at the doses of 7,35 and 175 lU/kg sc in mice. This drug exhibited no effect on urinary excretion at the doses of 7 and 35 lU/kg sc in rats. However, at a dose of 175 lU/kg sc, it showed a decreased urination along with decreased excretion of potassium, sodium and chloride ion. These results indicate that hPTH does not exert any of serious pharmacological effects except the inhibition of urination at a highest dose used.

• 대한한의학방제학회지
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• 제16권1호
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• pp.55-64
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• 2008

The span of life of human beings has lengthened because of medical progress and so on. Consequently, the old have begun to remark that quality of life (QOL) is as important as extension of the life expectancy. However, some diseases such as stroke, cancer induce decrease of QOL. In case of the stroke, it is followed by chronic headache and dementia as an aftereffect, causing serious decrease of QOL. Jodeungsan, traditional medicine, have been prescribed for headache and hypertension. Many clinical trials and laboratory experiments about pharmacological effects of Jodeungsan have been reported. Jodeungsan ameliorated chronic headache and improved recognitive deficit. Moreover, Jodeungsan lowered blood pressure in hypertensive condition which is one of a major cause of stroke. These effects of Jodeungsan on several diseases are partly attributed to antioxidant effect. This report reviews the pharmacological effect of Jodeungsan in the view of stroke-related diseases.