Antirheumatic Activity Research Articles

Evaluating the Bioactivity of <i>Ardisia solanacea</i> Leaf Extracts for Rheumatoid Arthritis Therapy: Inhibition of TNF-α and IL-6 through <i>In Silico</i> and <i>In Vitro</i> Studies

Background: Ardisia solanacea (Poir.) Roxb, a member of the Myrsinaceae family, is regarded as a significant medicinal plant according to traditional claims. This herb is documented to address various conditions, including mental disorder, dysmenorrhea, diarrhoea, gout, RA, vertigo, and skin sores. Aim: The study investigates the inhibitory effect of A. solanacea (family: Myrsinaceae), an indigenous medicinal plant against pro inflammatory cytokines such as Interleukin-6 (IL-6) and Tumour Necrosis Factor-alpha (TNF-α) using in vivo, ex vivo, and in silico approaches. Methods: The anti-rheumatic potential of A. solanacea leaf extracts was assessed in an adjuvant-induced arthritis rat model. The key metabolites present in the extracts were analyzed using GC-MS, and in-vitro studies confirmed significant anti-rheumatic activity. In silico studies were conducted using Autodock 1.5.6, BIOVIA Discovery Studio 4.0, and Open Babel GUI to explore interactions with IL-6 (PDB ID: 1IL-6) and TNF-α (PDB ID: 2AZ5). Results: The metabolites in the extracts exerted a strong inhibitory effect onIL-6 and TNF- α, indicating their therapeutic potential for rheumatoid arthritis. Ex vivo assays demonstrated that A. solanacea leaf extracts shows significant inhibitory effects in albumin denaturation and human red blood cell with inhibition levels of 71.37% and 148.03%, respectively. Comparatively, diclofenac sodium showed inhibition levels of 82.58% and 149.39% in these assays. Additionally, the molecular docking results were aligned with the in vivo results, supporting the observed inhibitory action of the plant metabolites on IL- 6 and TNF-α. Conclusion: The study highlights the potent inhibitory effects of A. solanacea leaf extracts on IL-6 and TNF-α, indicating their potential as therapeutic agents for rheumatoid arthritis management. Major Findings: The GC-MS study confirmed the presence of carboxylic acids, methyl esters, and relevant compounds in the leaf extract that are responsible to exert anti-arthritic and anti-inflammatory effect. The molecular docking and in-vitro anti-arthritic study co-relates and confirms the anti-arthritic effect of A. solanacea through IL-6, TNF-α, and IL-1 inhibition.

Effect of Geinstein on Regulation of Estrous Cycle in Albino Rats, Isolated from Flemingia vestita, an Ethnomedicinally Important Plant of Meghalaya, India

Flemingia vestita is a flowering plant belonging to the family of Fabaceae which is usually found in the Indian region including Khasi and Jaintia Hills of Meghalaya, India. It is cultivated for therapeutic use for its anti-microbial, anti-fungal, anti-helmintic, anticancer, anti-rheumatic, anti-inflammatory, antioxidant, and anti-histamine activities. The present study is to ascertain the phytochemical analysis of the root-tuber extract and modulating the effect of the Estrous Cycle in albino mice using Geinstein. The phytoestrogens present in the extract are iso-flavones and genistein which have a wide spectrum of biological activities including estrogenic effect. The number of leucocytes during the Meta-estrous at 0.1 ml/10 gm dose/body weight was maximum at ethanol extract while at 0.3 ml/10 gm dose/body weight was similar and maximum in both ethanol and methanol extract. Comparative cell number of interstitial connective tissues was maximum in ethanol followed by methanol and acetone extract. The present study concluded that the extract has a potential to modulate the estrogenic cycle in albino rats.

Development and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis.

The current project was designed to develop piperine-loaded solid lipid microparticles (SLMs) to assess the anti-arthritic potential of piperine (PIP). Variable proportions of carnauba wax, beeswax, and tween 80 were employed for preparing SLMs by using the solvent evaporation technique. The developed formulations were subjected to particle size measurements, entrapment efficiency (EE), and zeta potential (ZP) determination. Microparticles were also investigated for piperine-lipid compatibility, thermal analysis, surface morphology, piperine (PIP) release trend, and anti-rheumatic activity in rats. The network's grafting was confirmed by FTIR and XRD results. The thermal stability of the constructed network was confirmed by the DSC and TGA results. SEM findings confirm porous surface morphology. The dissolution experiments on SLMs confirmed the sustained release profile, delivering 87.82% to 94.92% of piperine at 7.4 pH for 24h. All developed formulations followed a zero-order kinetic model and the Korsmeyer-Peppas model. Furthermore, the anti-rheumatic potentials of piperine from SLMs were also investigated and compared with diclofenac sodium (the standard treatment) in a rat model. The analysis revealed that PIP significantly reduced the severity of arthritis, as confirmed by the findings of multiple arthritic assessment parameters.

Anti-inflammatory and analgesic effects of Filipendula ulmaria extract

The present study investigated the chemical content, analgesic, and anti-inflammatory properties of Filipendula ulmaria (L.) Maxim. (meadowsweet) aerial part extract. F. ulmaria is native to Bulgaria. Based on its phytochemicals, meadowsweet has a vast range of pharmacological activities, like antipyretic, analgesic, anti-inflammatory, antirheumatic, immunostimulating, anti-microbial, anti-allergic, and gastroprotective activity. In our experiment, F. ulmaria aerial part extract was practically non-toxic (oral LD50 > 2000 mg/kg). The performed experiments revealed that diclofenac possesses better anti-inflammatory and antinociceptive activity than F. ulmaria extracts (100 and 200 mg/kg). The results revealed a dose-dependent moderate inhibition of the inflammation and pain induced by 3 days of oral pretreatment with methanolic extract of F. ulmaria extracts. No additive effect of FUA extracts on the effects of diclofenac was noted. F. ulmaria extracts did not induce any alterations in blood biochemical analysis.

Betanin Mitigates Inflammation and Ankle Joint Damage by Subduing the MAPK/NF-κB Pathway in Arthritis Triggered by Type II Collagen in Rats.

Rheumatoid Arthritis (RA), a chronic inflammatory autoimmune illness, is characterized by synovitis, progressive joint damage, and bone erosion. Even though the potent drugs available contain biologics, several patients fail to react to them or cause hostile effects. Betanin (BTN), the betacyanin present in the red beetroot, has antioxidant, antiinflammatory, and apoptotic properties. In this study, we assessed the anti-inflammatory and apoptotic effect of BTN on collagen-induced arthritis (CIA). The rats were arbitrarily separated into four sets: Normal, CIA, CIA+BTN (25 mg/kg bw), and CIA+BTN (50 mg/kg bw). The hematological, biochemical markers, cytokines, inflammatory enzymes, histopathology of the ankle joint, and protein expression of inflammatory and apoptotic proteins were studied. Inflammatory enzymes, histopathological variations, cytokines generation, and joint inflammation were strongly alleviated, and apoptosis was augmented by BTN in a concentrationdependent manner. Bcl-2 and MAPK/NF-κB proteins were reduced, while the caspase-3, caspase- 9, and Bax were intensified. The anti-rheumatic action of BTN was correlated to the attenuation of the MAPK/NF-κB pathway, which suppresses cytokine production, inflammation, and reduced cartilage impairments. These outcomes recommend that BTN can be employed as a strong healing alternative for RA management.

Kundur (Boswellia Serrata): Medicinal Importance in Perspective of Unani Medicine and Pharmacological Studies

Kundur, the Indian olibanum tree, is a member of the Burseraceae family and grows best in the dry mountainous regions of the Middle East, Northern Africa, and India. This tree has small to huge branches. The tree's oleo-gum resin is removed and stored from the incision created in its trunk. Resin makes roughly 30–60% of oleo-gum resin, with organic solvent-soluble essential oils making up the remaining 5–10%. Gum-resin extracts from Boswellia serrata have long been used in traditional medicine to treat a variety of chronic inflammatory diseases. Four primary pentacyclic triterpenic acids found in the resinous component of Boswellia serrata are β-boswellic acid, acetyl-β-boswellic acid, 11-keto-β-boswellic acid, and acetyl-11-keto-β-boswellic acid. This oleo-gum resin is quite popular among traditional practitioners of traditional Chinese and Indian Systems of medicine because of its wide range of useful biological properties such as anti-inflammatory, anti-arthritic, anti-rheumatic, anti-diarrheal, anti-hyperlipidemic, anti-asthmatic, anti-cancer, anti-microbial, anti-fungal, anti-complementary, and analgesic activity etc.

Formulation and evaluation of naringenin niosomes for topical drug delivery and antirheumatic activity

Formulation and evaluation of naringenin niosomes for topical drug delivery and antirheumatic activity

Sporidiobolus pararoseus polysaccharides relieve rheumatoid arthritis by regulating arachidonic acid metabolism and bone remodeling signaling pathway

Rheumatoid arthritis (RA) is an autoimmune-mediated disease with the highest disability rate. Sporidiobolus pararoseus polysaccharides (SPP) have been demonstrated to have anti-rheumatoid and microbiota-modulatory effects; however, the underlying mechanisms remain unclear. This study employed collagen-induced arthritis (CIA) mice to explore the metabolic and genetic pathways. The results revealed SPP intervention significantly reduced the serum levels of rheumatoid and pro-inflammatory complement factors. SPP promoted the transition of macrophages of CIA mice toward the M2 phenotype (F4/80+/CD206+) from an inflammatory phenotype (F4/80+/CD86+) using flow cytometry analysis. A total of 44 metabolites were upregulated, and 110 metabolites were significantly downregulated by SPP compared to those in RA group. The decreased metabolites, 12(S)-HPETE, prostaglandin H2, 15-HETE, hepoxilin B3, and 15-keto-prostaglandin F2a, were mostly enriched in arachidonic acid metabolism (enrichment = 11.4 %), which was highly correlated with the anti-rheumatic activity of SPP. Gene expression analysis revealed that SPP significantly regulated OPG/RANKL/TRAF6 signaling pathway, stimulating osteogenic remodeling. Furthermore, arachidonic acid metabolism was identified as the critical metabolic driver of RA phenotypes and osteoclast differentiation, potentially associated with SPP-reshaped intestinal microbiota (i.e., Rikenellaceae_RC9_gut_group, Bacteroides, and Parabacteroides). Collectively, this study utilized an integrated approach of metabolomics and gene expression analysis to investigate the regulatory role of SPP in RA progression.

GC-MS Analysis and In-silico Molecular Docking of Phytoconstituents of Sansevieria roxburghiana against IL-1β and TNF-α for Anti-Rheumatic Activity

Background: Rheumatoid arthritis (RA) is recognized as a long-term inflammatory form of arthritis. This inflammation becomes long-lasting, and the synovial tissue thickens as a result of increased cell activity, protein production, and other variables in the joint, causing discomfort, redness, and warmth. It can also harm the joints of the hands, wrists, fingers, elbows, shoulders, toes, spinal column, and knees. Due to the autoimmune response, there is an aberrant production of inflammatory mediators such as Tumour necrosis factor- alpha (TNF-a), Interleukins (IL-1, IL-6, IL-7, IL-15, IL-17, IL-18, and IL-23), Granulocyte-macrophage colony-stimulating factor (GM-CSF), and Interferon (IFN)-ϒ. By inhibiting their production, those inflammatory mediators will play a pivotal role in the therapy of RA. Purpose of the Study: The goal of the current study was to explore the anti-rheumatic activity of Sansevieria roxburghiana using the computational docking method. Research Rationale: Administration of Non-steroidal anti-inflammatory drugs, steroidal medicaments, and Disease-modifying anti-rheumatoid therapies creates substantial adverse effects in people suffering with RA. To overcome the burdens and toxicity of drug products herbal medicines were taken into the field of research. Materials and Methods: For this, 14 bioactive compounds from ethanolic extract of S. roxburghiana leaves were identified using the GC-MS (Gas chromatography-mass spectrometry) study and utilized as a binding compound (ligand) for biological target interactions. The crystallographic geometries of two targeted molecules, Interleukin-1β (IL-1β) and Tumour necrosis factor-alpha (TNF-α), have been retrieved from the PDB database. Methotrexate, a well-known medication for IL-1β and TNF-α inhibitors, was chosen as the reference for the comparative analysis. Computational docking was performed using the Autodock4 (version 1.5.6) choice based on the score functions. Results: The results displayed the binding energy as follow -10.13, -9.77, -8.98 and -8.67 Kcal/mol of 2-isopropyl-5 methyl cyclohexyl 3-(1-(4-chlorophenyl)-3-oxobutyl)-C, 3-chloro-5-cholestene, stigmasterol, and cycloartanol against IL-1 β (PDB ID: 4GAI) and standard methotrexate was -8.14 Kcal/mol. For TNF-α (PDB ID: 5M2J) the binding energy is -8.94, -8.85, -8.46, and -8.24 Kcal/mol of cycloartanol, stigmasterol, 2-isopropyl-5 methyl cyclohexyl 3-(1-(4-chlorophenyl)-3-oxobutyl)-C and 3-chloro-5-cholestene by with comparing methotrexate (-8.89 Kcal/mol). Conclusion: Hence, it was indicated that the phytoconstituents of S. roxburghiana could serve as a potential approach for designing future antirheumatic drugs.

Lemon Oil Enhances the Anti-Rheumatic Activity of Woody Essential Oils in Formaldehyde-Induced Arthritis in Wistar Rats

Lemon Oil Enhances the Anti-Rheumatic Activity of Woody Essential Oils in Formaldehyde-Induced Arthritis in Wistar Rats

Exploring the molecular mechanism of Epimedium for the treatment of ankylosing spondylitis based on network pharmacology, molecular docking, and molecular dynamics simulations.

Ankylosing spondylitis (AS) is a rheumatic disease that causes inflammation and bone formation in the spine. Despite significant advances in treatment, adverse side effects have triggered research into natural compounds. Epimedium (EP) is a traditional Chinese herb with a variety of pharmacological activities, including antirheumatic, anti-inflammatory, and immunomodulatory activities; however, its direct effects on AS treatment and the underlying molecular mechanisms have not been systematically studied. Thus, here, we used network pharmacology, molecular docking, and molecular dynamics simulations to explore the targets of EP for treating AS. We constructed an interaction network to elucidate the complex relationship between EP and AS. Sixteen active ingredients in EP were screened; 80 potential targets were identified. In particular, 8-(3-methylbut-2-enyl)-2-phenylchromone, anhydroicaritin, and luteolin were the core components and TNF, IL-6, IL-1β, MMP9, and PTGS2 were the core targets. The GO and KEGG analyses indicated that EP may modulate multiple biological processes and pathways, including the AGE-RAGE, TNF, NF-κB/MAPK, and TLR signaling pathways, for AS treatment. Molecular docking and molecular dynamics simulations showed good affinity between the active components and core targets of EP, with stable binding within 100 nanoseconds. In particular, 8-(3-methylbut-2-enyl)-2-phenylchromone possessed the highest free energy of binding to PTGS2 and TNF (-115.575 and - 87.676kcal/mol, respectively). Thus, EP may affect AS through multiple pathways, including the alleviation of inflammation, oxidative stress, and immune responses. In summary, we identified the active components and potential targets of EP, highlighting new strategies for the further experimental validation and exploration of lead compounds for treating AS.

Integrated computational analysis, in vitro, in vivo investigation on Myristica fragrans Houtt. essential oils for potential anti rheumatic activities

Rheumatoid arthritis (RA) is an inflammation associated autoimmune disorder that is prevalent worldwide. Occurrence of severe side effects with current therapeutic regimens is major concern these days. We investigated Myristica fragrans mace and seed for management of inflammation and RA. Oils were extracted and analyzed using ATR-FTIR conforming occurrence of the aromatic amine, phenolic, and carboxylic acid groups mostly found in terpenoids. Most of tested compounds exhibited compliance with drug likeness, bioavailability and ADMET set parameters of safety. Molecular docking analysis showed interaction (-0.6 ΔG (kJ mol-1) of Myristicin with 4F5S. A significant antioxidant activity with DPPH, H2O2 and FRAP assays was observed in case of essential oil. Essential oil part also presented a significant protective effect during heat induced hemolysis (66 ± 1.0 %), BSA denaturation assay (61 ± 1.4 %) and higher levels of proteinase inhibition (70 ± 1.4 %). Acute antiflammatory model in rat presented a significant decrease in inflammation with essential oil. It was concluded that Myrictica fragrans essential oil possess significant (p < 0.005) anti-inflammatory potential that can play a key role in management of RA.

Identification and quantification of flavonoids and hydroxycinnamic acids in yellow wood anemone (&lt;i&gt;Anemone ranunculoides&lt;/i&gt; L.) by UHPLC-DAD-HESI/MS analysis

Introduction. Yellow wood anemone (Anemone ranunculoides L.) is a herbaceous perennial. This plant grows in the European parts of Russia, Ciscaucasia, Siberia, Central Europe and other regions. It has many different pharmacological activities: immunomodulatory, sedative, anti-inflammatory, antitoxic, diuretic, antibacterial, antioxidant, antitumor and antirheumatic activity. These various effects are due to their biologically active compounds, which include ephemeroids, protoanemonin, saponins, tannins, resins, ascorbic acid, ranunculin, oils lipids and triterpene glycosides. As to phenolic compounds, currently there is no sufficient information on flavonoids and hydroxycinnamic acids (HCAs) profiles in different species of genus Anemone. Because these groups of compounds are quite specific for yellow wood anemone, their detailed study seems to be relevant.Aim. The objective of this research is to identify and quantify flavonoids, HCAs, and their conjugates in Yellow wood anemone leaves, flowers and rhizomes with roots.Materials and methods. The identification was carried out by using ultra-high-performance liquid chromatography with diode array and electrospray ionization-mass spectrometric detection (UHPLC–DAD–ESI-MS) with quantification of individual compounds by external calibration method.Results and discussion. Among the 47 compounds, 30 flavonoids and 17 derivatives of HCAs were detected. Quercetin glycosides were found to be the major flavonoids in aerial parts whereas chalcone glycosides – in underground parts. The major HCA in rhizomes with roots was feruloyltartaric acid (1.18 mg/g) whereas chlorogenic acid was predominant in leaves and flowers (8.68 mg/g and 2.62 mg/g accordingly). The total content of phenolic compounds was estimated at 60 mg/g on a dry weight basis.Conclusion. As a result of the research a detailed profile of flavonoids and HCAs acids of anemon was described. The data obtained can serve to identify this species in the standardization of medicinal plant materials and taxonomic studies.

Development and In vitro Assessment of Topical Microemulsion Based Pluronic-Lecithin Organogel for the Management of Arthritic Pain

Background: Topical delivery of NSAIDs through organogels might transport lornoxicam to the site of action, minimizing gastrointestinal problems and adverse effects. Methods: In the current investigation, a lecithin organogel containing lornoxicam was made by microemulsion method. For this purpose, a certain amount of pure soya lecithin was dispersed in suitable isopropyl myristate as a dispersant and emulsifier at room temperature to form the oily phase. The lecithin was completely dissolved in the combination by the next morning. Sorbic acid was then added to the mixture as a preservative, Pluronic F-127 and potassium sorbate were weighed out, and then they were mixed with cold water to create an aqueous phase, and menthol was added. On the next morning, lornoxicam, the active component, became soluble in polyethylene glycol-400 and combined with the lecithin isopropyl palmitate mixture. The oily portion was agitated using a mechanical stirrer at 400 rpm while the aqueous phase was introduced gradually. Results: The lornoxicam organogel preparation was it was assessed for its physical appearance, organoleptic characteristics, consistency, gelation temperature, drug content, and in vitro release studies. The active ingredient content of formulation F5 was the highest at 93.33. Formulations F4 and F5 were selected for kinetic studies because they had all physical characteristics under reasonable limits, the active ingredient level was the greatest, and the active ingredient release was the fastest in eight hours. Conclusion: The transdermal organogel formulation of lornoxicam was found to be effective for topical distribution of the drug and when administered topically, it has strong anti-inflammatory and anti-rheumatic action.

Spectroscopic method to estimate 3-Acetyl-11-keto-β-boswellic acid in complex lipid nanocarriers and skin matrices

3-Acetyl-11-keto-β-boswellic acid (AKBA) is a phytoconstituent derived from Boswellia serrata extract. It shows anti-rheumatic activity by selectively and non-competitively inhibiting the 5-Lipoxygenase (5-LOX) enzyme. AKBA is utilized for complex nanocarriers for its effective topical delivery at the arthritic site. There is a demand to develop a rapid, sensitive, and economical UV–Visible spectroscopic method for AKBA, which can be utilized in nanoformulation designing and day-to-day analysis of in vitro and ex vivo samples. In this research work, an analytical method was developed for the estimation of AKBA in two solvent systems, methanol and phosphate buffer saline pH 7.4, using a UV–Visible spectrophotometer. Further, the developed method was validated for linearity, range, limit of detection, limit of quantification, accuracy, precision, solution stability, and specificity as per regulatory guidelines. The method exhibited a linearity range of 10–50 µg/mL in both media with the obtained value of the high correlation coefficient (>0.9995). Interday and intraday precision samples showed less than 2 % relative standard deviation (% RSD) that exhibited the reliability of the developed method. The accuracy study reflected the % recovery between 99 and 101 % in both media. Further, the developed method was explored to quantify AKBA in formulated lipid nanocarriers (LNCs) formulation. The methanol method was effectively used to estimate the entrapment efficiency in LNCs and skin retention of AKBA. For the quantification of AKBA in in vitro release and ex vivo permeation samples, the phosphate buffer saline pH 7.4 method was utilized. Results indicated that the method could quantify the AKBA in the presence of different sample matrices with reproducibility in nature. In conclusion, a sensitive, simple, economical, precise, and accurate UV–Visible spectroscopic method was developed and validated to quantify AKBA.

Analysis of anti-rheumatic activity of Nyctanthes arbor-tristis via in vivo and pharmacovigilance approaches.

Introduction: Rheumatoid arthritis (RA) is an immune-mediated disease associated with chronic inflammation of numerous joints. Nyctanthes arbor-tristis (NAT) is a traditional remedy for RA, a chronic inflammatory disorder. Aim: The current project aims to demonstrate the role of the NAT extracts in sub-acute toxicity, pharmacovigilance, and anti-rheumatic biomarkers. Method: Hydroethanolic extract (1:1) of plant leaves was prepared by using the reflux method. The safety of the dose was evaluated in Sprague-Dawley rats, and the anti-inflammatory effects of NAT on RA symptoms, including paw volumes, body weight, arthritic index, withdrawal latency, hematology and serological test, radiology, and histopathology, were evaluated in Freund's complete adjuvant (FCA)-induced arthritis Sprague-Dawley rat models. The inflammatory (TNF-α and COX-2) and anti-inflammatory markers (IL-10) were analyzed in control and experimental groups. Result: The study showed that 500mg/kg BW NAT leaf extract was found to be least toxic without showing any subacute toxicity symptoms. The pharmacovigilance study highlighted the potential side effects of NAT, such as drowsiness, sedation, and lethargy, at high dosages. Treatment with the plant extract mitigated paw edema, restored the immune organ and body weights, and ameliorated the level of blood parameters such as hemoglobin, red blood cells, platelets, white blood cells, aspartate aminotransferase (AST), alanine transaminase (ALT), C-reactive proteins, and rheumatoid factor. Treatment with the plant extracts also reduced the level of cyclooxygenase 2 and TNF-α and increased the level of IL-10 in the serum of arthritic rats dose-dependently. Radiographic analysis of the ankle joint showed an improvement in the hind legs. Histological examination of the ankle joints revealed that the plant extract treatment decreased pannus formation, inflammation, and synovial hyperplasia in arthritic animals. Conclusion: NAT 500mg/kg could serve as a promising therapeutic option for the treatment of inflammatory arthritis.

Anti-inflammatory Effect of Gambier Catechin (Uncaria gambir Roxb) on Rheumatoid Arthritis: A Review

BACKGROUND: Rheumatoid arthritis (RA) is a chronic inflammatory disease of the joints and varies in severity in patients. Inflammation in the joints causes high levels of systemic pro-inflammatory cytokines such as interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) which have an impact on permanent damage to the joints. Until now, the treatment of RA is only symptomatic, without being able to prevent the progression of damage to the joints, and this treatment also causes side effects such as gastrointestinal and cardiovascular toxicity. Therefore, many patients are looking for alternative medicine to complement their treatment. METHODS: This research was a narrative review that was performed using PubMed, Science Direct, and Google Scholar using pre-clinical and clinical studies which aim to determine whether the therapeutic mechanism of gambier catechin (Uncaria gambir Roxb) on RA. A literature review is carried out to formulate a scientific basis for innovation. RESULTS: The gambier plant is a typical plant of West Sumatra, which is rich in phytochemicals. The active compounds in gambier are catechins which are classified as flavanols/flavonoids. Catechins are compounds that are well-known as antioxidant, anti-inflammatory compounds, the highest found in gambier plants. Catechins affect the expression of inflammation-related genes and proteins such as TNF-α, IL-1, and show their anti-inflammatory roles. This research is a literature review using secondary data from original research based on in vitro, in vivo, and clinical trials. The results showed that catechins can inhibit the production of IL-1, TNF-α, prostaglandin and increase levels of cyclic adenosine monophosphate in rats. On histological findings, peri-synovial inflammation and cartilage damage decreased in the group given epigallocatechin-3-gallate which showed anti-rheumatic activity and increased CD4+ and CD25+ regulatory T cells, thereby inhibiting the B cell population effectively suppresses inflammation and arthritis pain and shows its therapeutic potential in the treatment of RA. CONCLUSION: It can be concluded that gambier catechins have the potential as a candidate for RA therapy. This, if developed, can certainly improve the health status of the community locally and globally.

Orchids of Dibru-Saikhowa: A Systematic Review on Their Traditional Use, Pharmacological Activity and Phytochemistry.

Dibru-Saikhowa National Park and Biosphere Reserve (DSNPBR), Assam, India, is a part of biodiversity hotspots and a store house of many orchid species. This systematic review was conducted to document the medicinal importante of orchids available in DSNPBR and to analyse their importance in drug discovery. This systematic review was conducted using the Preferred Reporting Items for Systematic Review and Meta-Analysis (PRISMA) guidelines. Scientific databases were used to search relevant literature to document ethnomedicinal uses, pharmacological activity and phytochemistry of orchid species available in DSNPBR. We have analysed 84 articles to document relevant information on 52 orchid species available in DSNPBR. Dendrobium (n=13) is the top genus. Different orchid species available in DSNPBR were used traditionally in India, Nepal, Bangladesh, and China to cure gastrointestinal disorders, disease-associated pain and inflammation, skin diseases, wound, arthritis, menstrual pain, tuberculosis etc. The pre-clinical investigations confirmed that extract/fraction/isolated compounds of orchids possess antirheumatic, anticancer, antitumor, anti-inflammatory, antidiabetic, antimicrobial, nephroprotective and neuroprotective activities through different mechanisms. Biomolecules isolated from orchid species like Dendrobium nobile alkaloids, polysaccharides have shown a potential to be developed as future drug molecules. Many phytochemicals isolated have demonstrated in vitro anticancer activities. The lack of clinical data in support of the therapeutic effectiveness of orchids is a major limitation. Orchids found in DSNPBR hold great significance in traditional culture for their medicinal properties and have been effectively studied for their bioactivities. Nevertheless, to confirm their effectiveness as therapeutics, conducting methodical research, examining their molecular mechanisms, and performing toxicity tests are necessary.

Chitosan coated clove oil-based nanoemulsion: An attractive option for oral delivery of leflunomide in rheumatoid arthritis

Rheumatoid arthritis (RA), a distressing inflammatory autoimmune disease, is managed mainly by Disease-modifying antirheumatic drugs (DMARDs), e.g. leflunomide (LEF). LEF (BCS class II) has limited solubility and adverse effects following its systemic exposure. The appealing antirheumatic properties of both clove oil and chitosan (CS) were exploited to design oral leflunomide (LEF)-loaded nanoemulsion (NE) system to augment the therapeutic action of LEF and decrease its systemic side effects as well. Different LEF-NEs were prepared using clove oil, Tween® 20 (surfactant), and PEG 400(co-surfactant) and characterized by thermodynamic stability, percentage transmittance, cloud point, size analysis, and drug content. Optimized LEF-NE was subjected to CS coating forming LEF-CS-NE that exhibited nanometric size range, prolonged drug release, and good physical stability. In vivo anti-rheumatic activity of pure LEF, market LEF, and LEF-CS-NE was assessed utilizing a complete Freund’s adjuvant (CFA) rat model. Treatment with LEF-CS-NE reduced edema rate (48.68% inhibition) and caused a marked reduction in interleukin-6 (IL-6) (510.9 ± 2.48 pg/ml), tumor necrosis factor- α (TNF-α) (397.3 ± 2.53 pg/ml), and rheumatoid factor (RF) (42.58 ± 0.49 U/ml). Furthermore, LEF-CS-NE reduced serum levels of glutamic pyruvic transaminase (GPT) to (83.19%) and glutamic oxaloacetic transaminase (GOT) to (40.68%) compared to the control + ve group. The effects of LEF-CS-NE were also superior to both pure and market LEF and showed better results in histopathological studies of paws, liver, kidney, lung, and heart. The remarkable therapeutic and safety profile of LEF-CS-NE makes it a potential oral system for the management of RA.

Dandelion (Taraxacum Genus): A Review of Chemical Constituents and Pharmacological Effects.

Dandelion (Taraxacum genus) is a perennial herb belonging to the Asteraceae family. As a well-known and extensively studied genus, dandelion comprises numerous species. Some species have been widely used in both complementary and alternative medicine to clear heat, detoxify, activate blood circulation, dispel stasis, and discharge urine. Multiple pharmacological studies have highlighted its therapeutic potential, including anti-bacterial, anti-oxidant, anti-cancer, and anti-rheumatic activities. Furthermore, bioactive compounds associated with these effects include sesquiterpenoids, phenolic compounds, essential oils, saccharides, flavonoids, sphingolipids, triterpenoids, sterols, coumarins, etc. Based on recent studies about the Taraxacum genus, the present review critically evaluates the current state of dandelion utilization and summarizes the significant roles of dandelion and its constituents in different diseases. We also focus on the reported phytology, chemical composition, pharmacology, and toxicity of dandelion, along with the main possible action mechanisms behind their therapeutic activities. Meanwhile, the challenges and future directions of the Taraxacum genus are also prospected in this review, thus highlighting its pharmaceutical research and practical clinical applications.