Composition Analysis and Pharmacological Activity of Avocado/Soybean Unsaponifiable Products Used in the Treatment of Osteoarthritis

Objective: Avocado/soybean unsaponifiables (ASUs) are commonly used to treat OA symptoms. However, there are many ASU mixtures on the market with differing compositions and pharmacological activities. This study aimed to compare the composition and pharmacological activity of seven commercially available ASU products on human osteoarthritis chondrocytes.Methods: The contents of the lipidic part of ASUs were characterized by gas chromatography analysis using a VARIAN 3400 chromatograph. The pharmacological activity of the ASU products was tested on human osteoarthritis chondrocytes cultured in alginate beads. Their effects were evaluated on aggrecan, interleukin (IL)-6 and -8, and matrix metalloproteases (MMP)-3 using immunoassays and on nitric oxide through measurement of nitrite via spectrometry.Results: PIASCLEDINE-ExpASU® showed a specific profile with the presence of chromatographic peaks corresponding to an alkyl furan fraction and alkyl triols. PIASCLEDINE-ExpASU®, Persemax, Insaponifiable 300, Arthrocen, and Arthocare contained quantifiable amounts of tocopherol, while tocopherol was undetectable in Avovida and Saponic. Squalene was found only in PIASCLEDINE-ExpASU®. The abundance of sterols varied depending on the product. PIASCLEDINE-ExpASU® was the most active of the tested ASU products in inhibiting nitric oxide, IL-6, and IL-8 production by chondrocytes. With the exception of Saponic and Persemax, all the ASU mixtures either slightly or significantly increased aggrecan production. MMP-3 levels were significantly decreased by Insaponifiable 300 and PIASCLEDINE-ExpASU® and significantly increased by Saponic.Conclusion: The composition of PIASCLEDINE-ExpASU® is different to that of the other evaluated ASU mixtures. This specific composition explains its better pharmacological activity, including the higher inhibitory effect on pro-inflammatory and pro-catabolic factors. Our findings are helpful in providing a basis for understanding the symptomatic effect of PIASCLEDINE-ExpASU® in patients with osteoarthritis.

Formulation and Evaluation of Nagarmotha Hair Oil

The Presenace study investigation oil isolation form cyperus rotundus and the chemical composition of essential oil of root's of Cyprus rotundus.In india it's commonly known as nagarmotha.and it belongs to the family cyperacea.the major chemical components of this herb are essential oils.flavonoids, terpenoids, sesauiterpenes, cyproten, cyperene, aselinene, rotundene, valencene, cyperol, gurjunene, transcalamenenene, cad'Alene, cyperoutundone, mustskone, isocyperol, acyperone etc. Reserch studies have shown that it possesses various Pharmacological activity Such as diuretic,carmenative emmenagogue, anthelmintic, analgesic, anti-inflammatory, anti-dysentery, anti-rheumatic activities.an extensive review of the ancient traditional literature and madern research revealead that the drug has numerous therapeutic action. Several of which have been established scientifically, which may help the reserchers to set their minds for approaching the utility efficiency and potency of nagarmotha. Keywords: cyperus rotundus, cyprotene flavanoids nagarmotha.

Identification and Quantification, Metabolism and Pharmacokinetics, Pharmacological Activities, and Botanical Preparations of Protopine: A Review

Through pharmacological activity research, an increasing number of natural products and their derivatives are being recognized for their therapeutic value. In recent years, studies have been conducted on Corydalis yanhusuo W.T. Wang, a valuable medicinal herb listed in the Chinese Pharmacopoeia. Protopine, one of its components, has also become a research hotspot. To illustrate the identification, metabolism, and broad pharmacological activity of protopine and the botanical preparations containing it for further scientific studies and clinical applications, an in-depth and detailed review of protopine is required. We collected data on the identification and quantification, metabolism and pharmacokinetics, pharmacological activities, and botanical preparations of protopine from 1986 to 2021 from the PubMed database using “protopine” as a keyword. It has been shown that protopine as an active ingredient of many botanical preparations can be rapidly screened and quantified by a large number of methods (such as the LC-ESI-MS/MS and the TLC/GC-MS), and the possible metabolic pathways of protopine in vivo have been proposed. In addition, protopine possesses a wide range of pharmacological activities such as anti-inflammatory, anti-platelet aggregation, anti-cancer, analgesic, vasodilatory, anticholinesterase, anti-addictive, anticonvulsant, antipathogenic, antioxidant, hepatoprotective, neuroprotective, and cytotoxic and anti-proliferative activities. In this paper, the identification and quantification, metabolism and pharmacokinetics, pharmacological activities, and botanical preparations of protopine are reviewed in detail to lay a foundation for further scientific research and clinical applications of protopine.

Pharmacological Activity of Garcinia indica (Kokum): An Updated Review

Garcinia indica (commonly known as kokum), belonging to the Clusiaceae family (mangosteen family), is a tropical evergreen tree distributed in certain regions of India. It has been used in culinary and industrial applications for a variety of purposes, including acidulant in curries, pickles, health drinks, wine, and butter. In particular, G. indica has been used in traditional medicine to treat inflammation, dermatitis, and diarrhea, and to promote digestion. According to several studies, various phytochemicals such as garcinol, hydroxycitric acid (HCA), cyanidin-3-sambubioside, and cyanidin-3-glucoside were isolated from G. indica, and their pharmacological activities were published. This review highlights recent updates on the various pharmacological activities of G. indica. These studies reported that G. indica has antioxidant, anti-obesity, anti-arthritic, anti-inflammatory, antibacterial, hepatoprotective, cardioprotective, antidepressant and anxiolytic effects both in vitro and in vivo. These findings, together with previously published reports of pharmacological activity of various components isolated from G. indica, suggest its potential as a promising therapeutic agent to prevent various diseases.

IDENTIFICATION AND CONTENT OF PHENOLIC COMPOUNDS IN A BUTANOL FRACTION OF EXTRACT FROM THE FLOWERS OF TANACETUM VULGARE

Tanacetum vulgare L. (syn.: Chrysanthemum vulgare (L). Bernh) is a perennial medicinal plant with a Euro-Asian type of habitat. Tansy extracts have a wide biological and pharmacological activity. At the All-Russian Institute of Medicinal and Aromatic Plants, on the basis of the butanol fraction of the T. vulgare flowers extract was developed a drug with high choleretic and anti-inflammatory activity. In this regard, the aim of this work was to study the qualitative composition and quantitative content of phenolic compounds of the butanol fraction, which are supposed to determine its biological activity. For this was obtained a phenolic compounds fraction, isolated from the extract of inflorescences of T. vulgare plants grown on the VILAR experimental plot. High-performance liquid chromatography with diode-array detection in combination with high-resolution mass spectrometry (UPLC-PDA-HRMS) was used for the analysis. Our studies have shown that the butanol fraction of T. vulgare contains 7 phenolic compounds, among which myricetin-3-glucoside was detected for the first time. The content of phenolic compounds reaches 90%, while the main compounds are neochlorogenic, 3,5- and 4,5-dicofeylquinic acids, the proportion of which is 69%. Thus, the obtained data indicate that the pharmacological activity of the drug based on the butanol fraction of the extract from tansy flowers is due to the high content of caffeoylquinic acids.

A Review of Botanical Characteristics, Chemical Composition, Pharmacological Activity and Use of Scorodocarpus borneensis

Scorodocarpus borneensis, an indigenous tree from Kalimantan, was used traditionally. This forest plant is from the genus Olacaceae with a unique characteristic of their bark that smells like onions. The scientific information about the potential activity of this plant was very limited. In this study, the chemical compounds and potential activities of S. borneensis were reviewed in this article. The information was collected from several databases, such as Google Scholar, PubMed, Science Direct, DOAJ, and Elsevier. Chemical compounds of S. borneensis were dominated by the volatile compound. That species has several activities, such as antioxidant, antibacterial

A Novel Approach for Quantifying the Pharmacological Activity of T-Cell Engagers Utilizing In Vitro Time Course Experiments and Streamlined Data Analysis

CD3-bispecific antibodies are a new class of immunotherapeutic drugs against cancer. The pharmacological activity of CD3-bispecifics is typically assessed through in vitro assays of cancer cell lines co-cultured with human peripheral blood mononuclear cells (PBMCs). Assay results depend on experimental conditions such as incubation time and the effector-to-target cell ratio, which can hinder robust quantification of pharmacological activity. In order to overcome these limitations, we developed a new, holistic approach for quantification of the in vitro dose–response relationship. Our experimental design integrates a time-independent analysis of the dose–response across different time points as an alternative to the static, “snap-shot” analysis based on a single time point commonly used in dose–response assays. We show that the potency values derived from static in vitro experiments depend on the incubation time, which leads to inconsistent results across multiple assays and compounds. We compared the potency values from the time-independent analysis with a model-based approach. We find comparably accurate potency estimates from the model-based and time-independent analyses and that the time-independent analysis provides a robust quantification of pharmacological activity. This approach may allow for an improved head-to-head comparison of different compounds and test systems and may prove useful for supporting first-in-human dose selection.