Separation procedures for the pharmacologically active components of rhubarb

2004 ◽  
Vol 812 (1-2) ◽  
pp. 175-181 ◽  
Author(s):  
H ZHANG ◽  
M LIU
Keyword(s):  
Active Components ◽  
Pharmacologically Active

Metal-organic Nanopharmaceuticals

2020 ◽  
Vol 8 (3) ◽  
pp. 163-190
Author(s):  
Benjamin Steinborn ◽  
Ulrich Lächelt
Keyword(s):  
Metal Ions ◽  
Coordination Polymers ◽  
Active Agent ◽  
Lewis Base ◽  
High Loading ◽  
Active Components ◽  
Base Functions ◽  
Metal Organic ◽  
Theranostic Applications ◽  
Pharmacologically Active

: Coordinative interactions between multivalent metal ions and drug derivatives with Lewis base functions give rise to nanoscale coordination polymers (NCPs) as delivery systems. As the pharmacologically active agent constitutes a main building block of the nanomaterial, the resulting drug loadings are typically very high. By additionally selecting metal ions with favorable pharmacological or physicochemical properties, the obtained NCPs are predominantly composed of active components which serve individual purposes, such as pharmacotherapy, photosensitization, multimodal imaging, chemodynamic therapy or radiosensitization. By this approach, the assembly of drug molecules into NCPs modulates pharmacokinetics, combines pharmacological drug action with specific characteristics of metal components and provides a strategy to generate tailorable multifunctional nanoparticles. This article reviews different applications and recent examples of such highly functional nanopharmaceuticals with a high ‘material economy’. : Lay Summary: Nanoparticles, that are small enough to circulate in the bloodstream and can carry cargo molecules, such as drugs, imaging or contrast agents, are attractive materials for pharmaceutical applications. A high loading capacity is a generally aspired parameter of nanopharmaceuticals to minimize patient exposure to unnecessary nanomaterial. Pharmaceutical agents containing Lewis base functions in their molecular structure can directly be assembled into metal-organic nanopharmaceuticals by coordinative interaction with metal ions. Such coordination polymers generally feature extraordinarily high loading capacities and the flexibility to encapsulate different agents for a simultaneous delivery in combination therapy or ‘theranostic’ applications.

scholarly journals Comparison of the Protective Effects of Bee Venom Extracts with Varying PLA2 Compositions in a Mouse Model of Parkinson’s Disease

Toxins ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 358 ◽  
Author(s):  
Kyung Hwa Kim ◽  
Minhwan Kim ◽  
Jaehwan Lee ◽  
Hat Nim Jeon ◽  
Se Hyun Kim ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Mouse Model ◽  
Therapeutic Potential ◽  
Bee Venom ◽  
Neuroprotective Activity ◽  
Protective Effects ◽  
Active Components ◽  
Therapeutic Benefits ◽  
Pharmacologically Active

Bee venom contains a number of pharmacologically active components, including enzymes and polypeptides such as phospholipase A2 (PLA2) and melittin, which have been shown to exhibit therapeutic benefits, mainly via attenuation of inflammation, neurotoxicity, and nociception. The individual components of bee venom may manifest distinct biological actions and therapeutic potential. In this study, the potential mechanisms of action of PLA2 and melittin, among different compounds purified from honey bee venom, were evaluated against Parkinson’s disease (PD). Notably, bee venom PLA2 (bvPLA2), but not melittin, exhibited neuroprotective activity against PD in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD. MPTP-induced behavioral deficits were also abolished after bvPLA2 treatment, depending on the PLA2 content. Further, bvPLA2 administration activated regulatory T cells (Tregs) while inhibiting inflammatory T helper (Th) 1 and Th17 cells in the MPTP mouse model of PD. These results indicate that bvPLA2, but not melittin, protected against MPTP and alleviated inflammation in PD. Thus, bvPLA2 is a promising and effective therapeutic agent in Parkinson’s disease.

The pharmacologically active components of oxytropis falcata bungereduce ischemic-reperfusion injury in the rat heart

2016 ◽  
Author(s):  
Dejun Zhang ◽  
Ruofei Jiang ◽  
Eun-Kyung Hong ◽  
Guosheng Tan ◽  
Dianxiang Lu ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Reperfusion Injury ◽  
Pathological Change ◽  
Total Flavonoids ◽  
Active Components ◽  
Ischemic Reperfusion Injury ◽  
Rat Serum ◽  
Ischemic Reperfusion ◽  
Pharmacologically Active ◽  
Ethyl Acetate Extracts

Oxytropis falcata is used as the main material to prepare various Tibetan traditional medicine, which its activity was reported that anti-inflammation and analgesia. Flavonoids is the chemical basis for the anti-inflammatory and anti-oxidant efficacy. The influence of total flavonoids of Tibetan herb O. falcata on myocardial ischemic-reperfusion injury was investigated using ethanol, chloroform, and ethyl acetate extracts. Rats were pretreated with different concentrations of the extract for 7 days. The model of myocardial ischemic-reperfusion injury was established by ligating the left anterior descending (LAD) artery in the heart. Following reperfusion for 40 minutes, the enzyme activity of creatine kinase (CK), lactic acid dehydrogenase (LDH), superoxide dismutase (SOD), and glutathione peroxidase (GSH-Px), and the concentration of malondialdehyde (MDA) in the rat serum were measured. The ultrastructural pathological change was observed under transmission electron microscopy (TEM). The serum levels of CK, LDH, and MDA were reduced, and the activity of SOD and GSH-Px were increased significantly, by chloroform and ethyl acetate extracts (P Less Than 0.01, PP Less Than 0.05). The ultrastructural pathological change in myocardial ischemic-reperfusion injury was alleviated by both extracts. The major components in chloroform extract were 7-hydroxy-flavonone and 2',4'-dihydroxy chalcone. 7-Hydroxy-flavanon naringenine naringetol and 2',4'-dihydroxy chalcone were the major components in ethyl acetate extract. Total flavonoids of Tibetan herb O. falcata might alleviate myocardial ischemic-reperfusion injury.

scholarly journals Phytotherapy for diabetes mellitus; A review of Middle Eastern and North African folk medicinal plants

2020 ◽  
Vol 10 (1) ◽  
pp. 1-13
Author(s):  
Sara S Abouzekry ◽  
Marwa T Badawy ◽  
Nada M Ezzelarab ◽  
Ahmed Abdellatif
Keyword(s):  
Diabetes Mellitus ◽  
Medicinal Plants ◽  
Middle Eastern ◽  
Folk Medicine ◽  
North African ◽  
Active Components ◽  
Large Numbers ◽  
Few Data ◽  
Pharmacologically Active ◽  
Further Development

Diabetes mellitus (DM) is considered as one of the most common metabolic disorders affecting huge number of people worldwide. Despite the availability of large numbers of drugs in the market to treat the disease, there is still a need for new sources to deal with the problem and avoid side effects. In the pursuit of discovering safer and more effective anti-diabetic drugs, herbal and folk medicine drugs from regions all over the world have captured researchers’ interest. Middle Eastern and North African medicinal plants contain a variety of pharmacologically active components that have shown to possess promising anti-diabetic potential. However, few data have been reported about medicinal plants from these regions in comparison to plants from other regions. Anti-diabetic medicinal plants from the MENA (the Middle East and North Africa) region, their role in controlling DM, and suggested mechanisms for the anti-diabetic activity of some medicinal plants are discussed in this review. Many of these plants have not been fully investigated and characterized, yet they have great potential for further development as anti-diabetic drugs.

scholarly journals Quantitative standardization of pharmacologically active components from antiplasmodial plant Solanum nudum Dunal (wild and in vitro)

2022 ◽  
Vol 21 (1) ◽  
pp. 41-50
Author(s):  
Ana Maria Mesa-Vanegas ◽  
◽  
Esther Julia Naranjo-Gomez ◽  
Felipe Cardona ◽  
Lucia Atehortua-Garces ◽  
...  
Keyword(s):  
Pacific Coast ◽  
Inhibitory Concentration ◽  
Quality Parameter ◽  
Antimalarial Treatment ◽  
Active Components ◽  
Steroidal Compound ◽  
Pharmacologically Active ◽  
Article Study ◽  
Over Time

Solanum nudum Dunal (Solanaceae) is most commonly known and used by the population of the colombian Pacific coast as an antimalarial treatment. This article study into optimization and quantitative analysis of compounds steroidal over time of development of this species when grown in vitro and wild. A new steroidal compound named SN6 was elucidated by NMR and a new method of quantification of seven steroidal compounds (Diosgenone DONA and six steroids SNs) using HPLC-DAD-MS in extracts of cultures in vitro and wild was investigated. Biology activity of extracts was found to a range of antiplasmodial activity in FCB2 and NF-54 with inhibitory concentration (IC50) between (17.04 -100 μg/mL) and cytotoxicity in U-937 of CC50 (7.18 -104.7 μg/mL). This method creates the basis for the detection of seven sterols antiplasmodial present in extracts from S. nudum plant as a quality parameter in the control and expression of phytochemicals.

Absorption, metabolism, and excretion of 14C gimatecan (LBQ707) after oral administration in patients with advanced cancer

2007 ◽  
Vol 25 (18_suppl) ◽  
pp. 2564-2564 ◽  
Author(s):  
M. M. Woo ◽  
L. Rodriguez ◽  
H. Gu ◽  
K. Crenshaw-Williams ◽  
F. Rocha ◽  
...  
Keyword(s):  
Advanced Cancer ◽  
Topoisomerase I ◽  
Oral Absorption ◽  
Total Radioactivity ◽  
Fecal Excretion ◽  
Active Components ◽  
Good Tolerability ◽  
Radiometric Detection ◽  
Pharmacologically Active

2564 Background: Gimatecan (Gim), a new potent oral topoisomerase I inhibitor is a lipophilic 7-oxyiminomethyl derivative of camptothecin. Its in vitro cytoxicity is more sustained than CPT-11 and topotecan, it has excellent anti-tumor activity in mouse xenografts, and shown good tolerability with Ph I activity. The study aim was to profile its disposition in cancer patients. Methods: 4 patients with advanced cancer received a single oral 1.5 mg dose of [14C] Gim (60 μCi) followed by standard Gim treatment on Day 15. Whole blood, plasma, urine, and feces were collected over 7 days with spot fecal collections up to Day 19. Total radioactivity was measured by liquid scintillation counting. Gim and metabolite concentrations in plasma and excreta were measured by LC- MS/MS and HPLC with radiometric detection. Results: Gim showed a rapid first-order absorption and a long elimination phase and was well tolerated. The median (range) Tmax for Gim was 1 h (0.5 to 3 h) and mean t1/2 and oral clearance values were 91 h and 0.6 L/h, respectively. Gim was the major moiety and its active metabolite LCF775 (t-butyl-mono-hydroxy Gim) was the main metabolite (albeit minor, 2–9%) in plasma. Trace glucuronide and sulfate metabolites were also detected in plasma. Mean recovery of radioactivity in urine (0-Day 7) and feces (0-Day 11) was 70.5 % (56.2–80.0%) of the dose. Incomplete recovery is attributed to opiates use in 2 patients and incomplete (sporadic) fecal sampling at later timepoints. Fecal excretion (0-Day 11) was prolonged and major in 3/4 patients (46- 73% of the dose, of which 14–23% is the unchanged Gim suggesting the drug is well absorbed). An additional 1.3–3.5% was recovered in spot collections (Days 14, 15 and 19). Urine excretion (0-Day 7) was 7.2–10.3% of the dose in 3 patients, one patient (cachectic, on opiates) excreted only 21% in feces and 46% in urine. Gim and several Gim metabolites (and glucuronide conjugates thereof) were the major components in excreta. Conclusions: Gim and its minor metabolite, LCF775 were the principal pharmacologically active components in plasma. Fecal excretion is the main elimination pathway in most patients. A long half-life (90hr) of Gim, uncomplicated metabolism, and good oral absorption make Gim an attractive candidate for Ph II development. [Table: see text]

scholarly journals Network Pharmacology-Based Dissection of the Comprehensive Molecular Mechanisms of the Herbal Prescription FDY003 Against Estrogen Receptor-Positive Breast Cancer

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110443
Author(s):  
Ho-Sung Lee ◽  
In-Hee Lee ◽  
Kyungrae Kang ◽  
Sang-In Park ◽  
Minho Jung ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Molecular Mechanisms ◽  
Network Pharmacology ◽  
Active Components ◽  
Cellular Processes ◽  
Incidence And Mortality ◽  
Estrogen Receptor Positive ◽  
Pharmacologically Active ◽  
Positive Breast Cancer

Estrogen receptor-positive breast cancer (ERPBC) is the commonest subtype of breast cancer, with a high prevalence, incidence, and mortality. Herbal drugs are increasingly being used to treat ERPBC, although their mechanisms of action are not fully understood. Therefore, in this study, we aimed to analyze the therapeutic properties of FDY003, a herbal anti-ERPBC prescription, using a network pharmacology approach. FDY003 decreased the viability of human ERPBC cells and sensitized them to tamoxifen, an endocrine drug that is widely used in the treatment of ERPBC. The network pharmacology analysis revealed 18 pharmacologically active components in FDY003 that may interact with and regulate 66 therapeutic targets. The enriched gene ontology terms for the FDY003 targets were associated with the modulation of cell survival and death, cell proliferation and growth arrest, and estrogen-associated cellular processes. Analysis of the pathway enrichment of the targets showed that FDY003 may target a variety of ERPBC-associated pathways, including the PIK3-Akt, focal adhesion, MAPK, and estrogen pathways. Overall, these data provide a comprehensive mechanistic insight into the anti-ERPBC activity of FDY003.

scholarly journals Alteration of the Structure of Human Stratum Corneum Facilitates Transdermal Delivery

2014 ◽  
Vol 8 (1) ◽  
pp. 72-79
Author(s):  
Anne Mundstock ◽  
Rawad Abdayem ◽  
Fabrice Pirot ◽  
Marek Haftek
Keyword(s):  
Stratum Corneum ◽  
Ex Vivo ◽  
Morphological Changes ◽  
Skin Permeation ◽  
Ultrastructural Changes ◽  
Active Components ◽  
Transmission Electron ◽  
Liquid Systems ◽  
Hydrophilic Compounds ◽  
Pharmacologically Active

Transdermal transport of pharmacologically active components into the skin depends on the ability of galenic formulations to overcome the stratum corneum (SC) barrier. Microemulsions (ME) are thermodynamically stable liquid systems composed of water, oil and surfactants which may be used for skin permeation and enhance penetration of hydrophobic as well as hydrophilic compounds. We investigated using transmission electron microscopy the effect of ME on human epidermis ex vivo, in order to establish relationship between the type of ME, i.e.: oil-in-water, water-in-oil, gellike, thickened or not with colloidal silica, and the ultrastructural changes in SC barrier resulting from their topical application. ME induced various degrees of dissociation of the SC. The intercellular lipid matrix in the SC became disorganized, which contributed to the separation of corneocytes. This effect was intensified with the increasing oil content in the ME and also when ME were applied under occlusion. The observed morphological changes were in agreement with the increased permeability of ME-treated skin to both lipophilic and hydrophilic compounds reported in the literature. Severe deterioration of the SC barrier induced with the selected ME makes them suitable for selected indications only.

scholarly journals СHARACTERISTICS OF DIETARY FEEDS FOR DOMESTIC ANIMALS AVAILABLE ON THE MARKET OF UKRAINE

2021 ◽  
Vol 22 (1) ◽  
pp. 95-102
Author(s):  
Yu. M. Kosenko ◽  
O. S. Vezdenko ◽  
L. Ye. Zaruma ◽  
O. A. Sekh ◽  
O. S. Shkilnyk
Keyword(s):  
Kidney Stones ◽  
Animal Species ◽  
Animal Feed ◽  
European Federation ◽  
Active Components ◽  
Joint Tissue ◽  
Nutritional Needs ◽  
Digestive Disorders ◽  
Pharmacologically Active ◽  
Domestic Products

Complete and complementary dietary feeds are feeds intended for special nutritional purposes and used when the nutritional needs of the animal's body are met. The labeling of feeds intended for special nutritional purposes must contain the word "dietary". Their composition is balanced by proteins, fats, carbohydrates, vitamins, minerals, pre- and probiotics, and other pharmacologically active components that affect the digestive processes, excretion or prevention of kidney stones, strengthening joint tissue, suspending allergic reactions, renal dysfunction, liver, promote recovery from stress, etc. The article describes the characteristics of feeds intended for special nutritional purposes for pets, that are imported or the domestic products, which are authorized in Ukraine for the period 2015-2019. The names of finished feed products, in addition to trademarks, reflect the animal species and purpose, depending on the identified abnormalities in their health, which determines the special purpose for their use. According to the authorized products list, the largest number of names falls on dietary foods for pets used in kidney disease and kidney stones (70), digestive disorders (51) and allergies (37). A significant number (28) are low-calorie diets for overweight cats and dogs. The share occupied by certain groups of complete feeds by purpose meets the needs of the domestic market of complete dietary feeds for pets. This distribution of feeds intended for special nutritional purposes helps to ensure proper care for pets of different ages and breeds that are prone to disease. Feeds entering the market in Ukraine meet the requirements of national regulations and the main safety criteria of the European Federation of Animal Feed Manufacturers (FEDIAF) and the ISO standard 22 000: 2005. According to scientific research, the most common groups of feeds intended for special nutritional purposes for pets are described; the characteristics of the main feed ingredients in the formulas, and substantiated their function as a part of nutrition at special nutritional purposes of the animal's body.

scholarly journals PHARMACOECONOMICAL ANALYSIS OF ANTI-PERIODONTOSIS DRUGS

REPORTS ◽  
2020 ◽  
Vol 5 (333) ◽  
pp. 13-18
Author(s):  
E.G. Tolokonnikov ◽  
◽  
A.S. Adekenova ◽  
O.V. Maslova ◽  
◽  
...  
Keyword(s):  
Periodontal Diseases ◽  
Pharmacoeconomic Analysis ◽  
Experimental Studies ◽  
Pharmaceutical Market ◽  
Active Components ◽  
National Medical ◽  
Cost Of Disease ◽  
High Adhesion ◽  
Gel Preparation ◽  
Pharmacologically Active

In this work, a retrospective analysis of anti-periodontosis drugs is carried out using the methods of pharmacoeconomic analysis: analysis of the "cost of disease" (direct costs), "cost-effectiveness" for promoting the original drug "Matripin-Dent" on the pharmaceutical market. In the clinic of the Dental Institute of Kazakh National Medical University named after S.D. Asfendiyarov (Almaty), clinical trials of a new domestic phytopreparation “Dental gel Matripin-Dent” were carried out. The gel preparation was used in the complex therapy of periodontal diseases of an inflammatory and inflammatory-destructive nature. As a result of the experimental studies, it was found that "Matripin-Dent", due to the original composition of the gel composition, provides high adhesion to mucous surfaces, ensures reliable fixation of the drug on the gums, contributes to a better distribution of active components due to good absorption of the ointment base composition. It has been proven that the developed dosage form "Matripin-Dent" based on pharmacologically active compounds of Populus balsamifera L. buds and flowers, leaves, buds of Matricaria chamomilla L. has a number of advantages in comparison with the drugs existing on the pharmaceutical market used in dental practice.

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