• Title/Summary/Keyword: Synthetic drugs

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Ethnopharmacology, bioactivities and chemical constituents of some anti-cancer plants in Malaysia

  • Chooi, Ong-Hean
    • Plant Resources
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    • v.3 no.1
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    • pp.46-58
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    • 2000
  • Many plant species are used in Malaysia in folk medicine for the treatment of cancer. This paper presents some of these species with details on other ethnopharmacological uses, the known bioactivities and some chemical constituents of each of the species given. It is normal practice in traditional medicine that one species of plant is used to treat various ailments. Thus the plant species listed are all used to treat cancer but have various other ethnophrmacological uses as well, some with few other uses and rest with many other uses. Information on bioactivities of each species resulting from tests on human and experimental animals are also given. Proven bioactivities give strength to ethnopharmacological claims on the efficacies of plant resources in the treatment of cancer and various other ailments but will but will not necessarily lead to the production of new pharmaceutical drugs. Many of the known chemical constituents of each species are given. This shows the richness and variety of chemicals containes in each of the species listed. The chemicals listed may or may not prove to be important in the pharmaceutical sciences but is an indication of what each species contatin in thrms of plant chemicals. It is a well known fact that many of the pharmaceutical prescriptions in present day use are of plant origin and semi-synthetic or fully synthetic chemicals produced using knowledge gained from studies of phytochemicals. Thus the paper presented will give useful information and also shows the richness of plant species that have high potentials for the development of anti-cancer resources from plants in Malaysia.

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General Pharmacology of DWQ-013, A New Synthetic Quinolone Antibiotics (Effects on the Central Nervous System) (신규 합성 퀴놀론계 항생물질(DWQ-013)의 일반 약리 작용 -중추신경계에 대한 작용-)

  • Lim, Seung-Wook;Kim, Young-Man;Yu, Young-Hyo;Lee, Jae-Wook
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.586-594
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    • 1994
  • The general pharmacological effects of DWQ-013, a new synthetic quinolone antibacterial agent, were examined on the central nervous system in experimentral animals and the following results were obtained. Drug interaction of DWQ-013 with theophylline, fenbufen and nonsteroidal antiinflammatory drugs was also examined. DWQ-013 decreased touch escape effect on the general behavior and decreased body temperature at a concentration of 1000 mg/kg in mice. But DWQ 013 had no effect on the locomotor activity, rotarod perfomance and traction test in mice. Furthermore, DWQ-013 increased pentobarbital-induced sleeping time and affected the onset time in acetic acid-induced writhing test in mice. DWQ-013 reduced onset time and death time on strychnine-induced convulsions and death time on pentylenetetrazole-induced convulsions at a concentration of 1000 mg/kg in mice. But, the drug had no effect on the electroshock. DWQ-013 did not interact with fenbufen and any other NSAIDs but it did interact with theophylline. From these results, it could be suggested that DWQ-013 had less pharmacological effect than other quinolones on the central nervous system.

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Polysaccharides Obtained from Vegetables: an effective source of alternative excipient

  • Ananta Choudhury;Satyabrat Sarma;Snehashis Sarkar;Madhusmita Kumari;Biplab Kumar Dey
    • Journal of Pharmacopuncture
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    • v.25 no.4
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    • pp.317-325
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    • 2022
  • Polymers are the major constructive material of pharmaceutical formulations that play a prime role in designing effective drug-delivery systems and releasing drugs at their sites of application. Polymers are composed of multiple repeating units of high molecular mass components with attendant properties. Most synthetic polymers are non-biocompatible, expensive, and extremely inclined to deliver adverse impacts. Meanwhile, edible polymers obtained from natural sources have gained remarkable recognition for their promising use in modern medicine. Moreover, polymers derived from natural sources are generally preferred due to certain of their unique features such as abundant availability, biocompatibility, nontoxicity, economical, safe, and effective functions that fit the purpose. Polysaccharides including starch, cellulose, hemicellulose, pectin, and mucilage are identified as a major class of naturally obtained molecules that have a substantial role as functional polymers. This review summarizes the potential role of polysaccharides derived from vegetable sources such as adhesives, anticaking agents, binders, disintegrants, emulsifiers, film-framing agents, and thickeners. This is simply an opportunity to abandon synthetic excipients that hurt our bodies and think back to nature from where we originate.

Inhibition of Tumor Growth and Angiogenesis by KJ3, Betulinic Acid, and Fumagillin in Mouse Neuroblastoma (신생혈관 억제제 KJ3, Betulinic acid, Fumagillin의 혈관형성억제 및 신경모세포종에 대한 치료효과)

  • Choi, Seung-Hoon;Lee, Jung-Hee;Hwang, Eui-Ho
    • Advances in pediatric surgery
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    • v.8 no.2
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    • pp.101-106
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    • 2002
  • The antiangiogenic effects of novel agent KJ3, Betulinic acid, and Fumagillin on the neovascularization were studied by examining ultrastructural alterations in the vasculature of synthetic gelform and mouse neuroblastoma C1300. Small pieces of gelform with 0.4% agar were introduced subcutaneously (s.c.) in 7 week old male CH3/HeJ mice. After the $LD_{50}s$ were determined by FACS analysis, a third of $LD_{50}$ of three drugs were injected either locally or intraperitoneally every other day for 14 days. A/J mice were inoculated s.c. with the C1300 neuroblastoma cell line, then either saline or three drugs were injected in the same manner. The antiangiogenic effects of three drugs were studied by measuring the histologic changes in tumors, and immunostaining for CD34, VIII/vWF, CD105, and thymidine phosphorylase. In the drug treated groups, the number of vessels in gelform experiments and C1300 neuroblastoma experiments were lower than the corresponding values in the control. The histologic findings were significantly different in drug treated groups on day 7, but these were not significant on day 14. These results imply that antiangiogenic agents were effective when the tumor burden is minimal.

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Druggability for COVID-19: in silico discovery of potential drug compounds against nucleocapsid (N) protein of SARS-CoV-2

  • Ray, Manisha;Sarkar, Saurav;Rath, Surya Narayan
    • Genomics & Informatics
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    • v.18 no.4
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    • pp.43.1-43.13
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    • 2020
  • The coronavirus disease 2019 is a contagious disease and had caused havoc throughout the world by creating widespread mortality and morbidity. The unavailability of vaccines and proper antiviral drugs encourages the researchers to identify potential antiviral drugs to be used against the virus. The presence of RNA binding domain in the nucleocapsid (N) protein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) could be a potential drug target, which serves multiple critical functions during the viral life cycle, especially the viral replication. Since vaccine development might take some time, the identification of a drug compound targeting viral replication might offer a solution for treatment. The study analyzed the phylogenetic relationship of N protein sequence divergence with other 49 coronavirus species and also identified the conserved regions according to protein families through conserved domain search. Good structural binding affinities of a few natural and/or synthetic phytocompounds or drugs against N protein were determined using the molecular docking approaches. The analyzed compounds presented the higher numbers of hydrogen bonds of selected chemicals supporting the drug-ability of these compounds. Among them, the established antiviral drug glycyrrhizic acid and the phytochemical theaflavin can be considered as possible drug compounds against target N protein of SARS-CoV-2 as they showed lower binding affinities. The findings of this study might lead to the development of a drug for the SARS-CoV-2 mediated disease and offer solution to treatment of SARS-CoV-2 infection.

The Abuse Potential of α-Piperidinopropiophenone (PIPP) and α-Piperidinopentiothiophenone (PIVT), Two New Synthetic Cathinones with Piperidine Ring Substituent

  • Botanas, Chrislean Jun;Yoon, Seong Shoon;de la Pena, June Bryan;dela Pena, Irene Joy;Kim, Mikyung;Woo, Taeseon;Seo, Joung-Wook;Jang, Choon-Gon;Park, Kyung-Tae;Lee, Young Hun;Lee, Yong Sup;Kim, Hee Jin;Cheong, Jae Hoon
    • Biomolecules & Therapeutics
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    • v.25 no.2
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    • pp.122-129
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    • 2017
  • A diversity of synthetic cathinones has flooded the recreational drug marketplace worldwide. This variety is often a response to legal control actions for one specific compound (e.g. methcathinone) which has resulted in the emergence of closely related replacement. Based on recent trends, the nitrogen atom is one of the sites in the cathinone molecule being explored by designer type modifications. In this study, we designed and synthesized two new synthetic cathinones, (1) ${\alpha}-piperidinopropiophenone$ (PIPP) and (2) ${\alpha}-piperidinopentiothiophenone$ (PIVT), which have piperidine ring substituent on their nitrogen atom. Thereafter, we evaluated whether these two compounds have an abuse potential through the conditioned place preference (CPP) in mice and self-administration (SA) in rats. We also investigated whether the substances can induce locomotor sensitization in mice following 7 days daily injection and challenge. qRT-PCR analyses were conducted to determine their effects on dopamine-related genes in the striatum. PIPP (10 and 30 mg/kg) induced CPP in mice, but not PIVT. However, both synthetic cathinones were not self-administered by the rats and did not induce locomotor sensitization in mice. qRT-PCR analyses showed that PIPP, but not PIVT, reduced dopamine transporter gene expression in the striatum. These data indicate that PIPP, but not PIVT, has rewarding effects, which may be attributed to its ability to affect dopamine transporter gene expression. Altogether, this study suggests that PIPP may have abuse potential. Careful monitoring of this type of cathinone and related drugs are advocated.

Preparation of Silica Microcapsules containing Water-Soluble UV Absorbers by a W/O Microemulsion Sol-Gel Process (W/O 마이크로에멀젼 졸-겔 법을 이용한 수용성 UV 흡수제를 함유한 실리카 마이크로캡슐의 제조)

  • 함경국;안복엽;석상일
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2003.03a
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    • pp.220-220
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    • 2003
  • The microencapsulation of droplets or particles within a solid shell leads to the formation of core-shell particles. Microencapsulation provides protection and controlled release of core materials such as drugs, vitamins, enzymes, perfumes, and the like. Such particles have, therefore, found a diverse range of applications in the pharmaceutical, agricultural, cosmetic, and food industries. UV absorbers are widely used for cosmetics to screen out ultra violet (UV) rays which have side effects on human skin. The absorbers are made generally from synthetic organic compounds, which can stimulate the human skins to develop allergic phenomena.

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Synthesis and Screening of Cyclooxygenase Activity of Hydantoin and 2-Thiohydantoin Derivatives (Hydantoin 및 2-Thiohydantoin 유도체의 합성과 사이클로옥시게나제 활성 검색)

  • 신혜순;최희전;권순경
    • YAKHAK HOEJI
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    • v.48 no.2
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    • pp.141-146
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    • 2004
  • Selective COX-2 inhibitors were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of gastric and renal side effect associated with non-steroidal anti-inflammatory drugs. This study reported the syntheses of novel 2-thiohydantoin and hydantoin derivatives which have the structure of 5-membered heterocyclic ring substituted with two aryl groups, phenyl group at 5-position and p-sulfamylphenyl or p-methoxyphenyl group at 1-position. These synthetic compounds showed significant COX-2 activities in vitro screening. Among them, 5-phenyl-2-thiohydantoin and hydantoin substituted with benzyl group at 3-position, compounds 5 and 8, could be considered as lead compounds with $IC_{50}$/=13.13∼18.78 $\mu\textrm{g}$/$m\ell$ for the development of COX-2 inhibitors.

Study on Cosmeceutical Acitivies of Natural Material (천연소재의 화장품약리활성에 관한 연구)

  • Kim, Young-Hun;Cho, Woo-A;Lee, Jin-Tae
    • Journal of the Korean Society of Fashion and Beauty
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    • v.5 no.3
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    • pp.99-104
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    • 2007
  • The most extensively used synthetic antioxidants are butylated hydroxyanisole (BHA), butylated hydroxy toluene (BHT) and tert-butylhydroquinone (TBHQ). However BHT and BRA have been suspented of being responsible for liver damage andcar cinogenesis. Therefore, the importance of the search and exploitation of natural antioxidant, especially of plant origin, has greatly increased in recent years. Plant contain a wide variety of chemicals that have potent biological effects. As a result, there has been a growing interest in the use of herbs as a source of therapeutic drugs. The aim of this study was to assess the antioxidant and cosmeceutical of natural materials. The antioxidant and cosmeceutical activity of natural materials were investigated by hydroxyl radical scavenging, superoxide dismutase (SOD) -like, xanthine oxidase inhibition, tyrosinase inhibition, anti-microbial and astringent.

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Synthesis and Physical Properties of Biodegradable Polymers -Poly (glycine-co-lactic acid) and Poly (glycine-co-glycolic acid)- (생체분해성 고분자의 합성 및 물성에 관한 연구 -Poly (glycine-co-lactic acid) 와 Poly (glycine-co-glycolic acid)-)

  • 성용길;김정엽
    • Journal of Biomedical Engineering Research
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    • v.9 no.1
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    • pp.37-46
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    • 1988
  • Synthetic biodegradable polymers are of great interest for biomedical applications such as surgical sutures and drug delivery systems. The copolymers of ${alpha}-amino$ acids and ${alpha}-hydroxy$ matrices having the required permeability for drugs. Poly (glycine.co-lactic acid) and poly (glycine-co-glycolic acid) have been synthesized by ring-opening polymerization. Morpholine-2, 5-diane, lactide, and glycolid have been used as starting materials for polydepsipeptides. The synthesized monomers and copoylmers have been identified by NMR and FT-lR spectrophotometer. The thermal properties and glass transition temperatures ($T_g$) of the copolymers have been measured by differential scanning calorimetry. The $T_g$ values of poly (glycine-co-lactic acid) and poly (glycine co.glycolic acid) are increased with increasing mole fraction of morpholine-2, 5-dione in the copolymers.

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