diospyros and Edema

Rheumatoid arthritis is a chronic inflammatory disorder of polyarticular tissues, characterised by progressive synovitis. Its prolonged treatment imparts a huge burden on the healthcare system and results in toxicity, which necessitates the search for safe, efficacious and cost-effective therapies. Diospyros malabarica (Desr.) Kostel is traditionally used for anti-inflammatory purposes; however, to the best of our knowledge, there is no detailed study reporting the in vivo anti-inflammatory potential of this plant. Therefore, in the current study, the methanol extract of D. malabarica (Desr.) Kostel fruit (mDMF) was evaluated for its antioxidant, anti-inflammatory and anti-arthritic potentials, along with its underlying mechanisms. The antioxidant activity was evaluated by DPPH assay. Total phenolic and flavonoid contents were estimated via colorimetric and high-performance liquid chromatography (HPLC) methods. Different doses (250, 500 and 750 mg/kg) of mDMF were used to evaluate the anti-inflammatory and anti-arthritis actions in acute inflammatory (carrageenan and histamine-induced paw oedema) and Freund's complete adjuvant (FCA)-induced arthritis rat models. Levels of various pro- and anti-inflammatory biomarkers were estimated using ELISA and RT-PCR techniques. Paw samples were used for different histopathological and radiographic studies. Qualitative phytochemical and HPLC analyses indicated the presence of various polyphenolic compounds in mDMF, which exhibited marked antioxidant activity in the DPPH assay. mDMF showed time-dependent anti-inflammatory and anti-arthritic effects in in vivo models. ELISA assay data showed significant (p < 0.05) reduction in the serum levels of C-reactive protein and rheumatoid factor in the mDMF treatment groups. RT-PCR data showed significant (p < 0.05) down-regulation of various pro-inflammatory markers (TNF-α, NF-κB, COX-2, IL-1β and IL-6) and up-regulation of anti-inflammatory markers (IκB, IL-4 and IL-10) in serum samples of rats treated with mDMF. The histopathology of the ankle joints showed reduced pannus formation, joint swelling and synovial hyperplasia in mDMF-treated animals when compared with the untreated disease control group. Overall, it may be concluded that the antioxidant, anti-inflammatory and anti-arthritis properties of mDMF are due to its flavonoid and phenolic constituents. Further studies using a stable oral dosage form of D. malabarica (Desr.) Kostel fruits extract are warranted to explore i

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Arthritis, Experimental; Biomarkers; Cytokines; Diospyros; Edema; Flavonoids; Fruit; Inflammation; Plant Extracts; Rats; Rats, Sprague-Dawley

Diospyros lotus L. is traditionally used in various diseases including pain and sleep disorders. The pain and inflammation are the common problems, which are treated with various synthetic analgesic drugs, and associated the side effects. The natural products have gained significant importance over synthetic drugs. The importance of phyto-medicine the current study has been designed with the aim to investigate the analgesic and anti-inflammatory effects of Diospyros lotus and bioassay guided isolation from its crude fractions. Seven known compounds; lupeol (1), 7-methyljuglone (2), β-Sitosterol (3), stigmasterol (4) betulinic acid (5), diospyrin (6; DS) and 8-hydroxyisodiospyrin (7; HDS) which were hitherto unreported from D. lotus. The chloroform fraction (CFDL) and isolated compounds DS and HDS were evaluated for anti-nociceptive, sedative and anti-inflammatory effects. The acetic acid induced writing was significantly (p<0.001) protected by CFDL (72.43%), DS (40.87%) and HDS (65.76%) at higher doses which exhibited peripheral and central analgesic effects in acetic acid and hot-plat pain paradigms. Regarding the anti-inflammatory effect the CFDL (77.43%), DS (80.54%) and HDS (75.87%) protected the carrageenan paw edema after 3rd h. The central analgesic effect was significantly antagonized with naloxone (0.5 mg/kg), showing opiodergic mechanism of action. The CFDL, DS and HDS were also proved sedative in open field animal models. In acute toxicity study the chloroform fraction [CFDL (50, 100 and 150 mg/kg)], DS (5 and 10 mg/kg) and HDS (5 and 10 mg/kg) were found safe. Our study concluded that CFDL, DS and HDS have marked anti-nociceptive, anti-inflammatory and sedative effect. The anti-nociceptive and anti-inflammatory effects of the roots of D. lotus are partially attributed due to the presence of analgesic constituents like diospyrin (DS), 8-hydroxyisodiospyrin (HDS) and strongly supports the ethno-pharmacological uses of D. lotus as anti-nociceptive, anti-inflammatory and sedative.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Carrageenan; Chloroform; Diospyros; Drug Evaluation, Preclinical; Edema; Female; Hypnotics and Sedatives; Male; Mice, Inbred BALB C; Naphthoquinones; Plant Extracts; Toxicity Tests, Acute

This study investigated the analgesic effects of taraxeren-3-one, which is an ingredient from Diospyros maritima (DM), using the models of acetic acid-induced writhing response and the formalin test, and its anti-inflammatory effects using the model of λ-carrageenan (Carr)-induced paw edema. Treatment of male ICR mice with taraxeren-3-one inhibited the numbers of writhing response and formalin-induced pain in the late phase, significantly. In the anti-inflammatory test, taraxeren-3-one decreased paw edema at 4 and 5 h after Carr administration and increased the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), and glutathione (GSH) in the liver tissue at 5 h after Carr injection. Taraxeren-3-one affects malondialdehyde (MDA), nitric oxide (NO), and tumor necrosis factor-α (TNF-α) levels from both the edema paw and serum at 5 h after Carr injection. Western blotting revealed that taraxeren-3-one decreased Carr-induced inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions. These anti-inflammatory mechanisms of taraxeren-3-one might be related to the decrease in the level of MDA in the edema paw via increasing the activities of SOD, CAT, GPx, and GSH in the liver. Also, taraxeren-3-one could affect the production of NO and TNF-α and, therefore, affect the anti-inflammatory effects.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Carrageenan; Catalase; Diospyros; Edema; Formaldehyde; Glutathione Peroxidase; Liver; Male; Mice; Mice, Inbred ICR; Nitric Oxide; Pain; Plant Stems; Superoxide Dismutase; Triterpenes; Tumor Necrosis Factor-alpha

In this study we evaluated the analgesic and anti-inflammatory activities of the methanol extract of stem bark of Diospyros cordifolia (MEDC) Roxb. The analgesic effects of the stem bark of the plant was assessed in mice using the tail-flick method while carrageenan, histamine and dextran induced paw oedema was used to study the antiinflammatory effects in rats. The MEDC exhibited significant (p<0.01) analgesic effects comparable to the reference drug diclofenac sodium. MEDC also was evaluated for its anti-inflammatory potential against carrageenan, histamine and dextran induced rat paw edema. The methanol extract (25 and 50 mg / kg body weight) exhibited significant (p<0.01) activity against all phlogistic agents used in a dose dependent manner. All these effects were compared with reference drug phenylbutazone (100 mg/kg body weight).

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Diospyros; Dose-Response Relationship, Drug; Edema; Female; Male; Mice; Pain; Pain Measurement; Phytotherapy; Plant Extracts; Plant Stems; Rats