| Description: |
Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities.Friedelin rich fraction (IND-HE) shows estrogenic activity as indicated by vaginal cornification, increase in uterine weight and rise in serum estrogen. Friedelin may be beneficial to mimic insulin action that would be useful in the treatment of diabetes type 2 patients.
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| In vitro: |
| Food Chem. 2013 Aug 15;139(1-4):860-5. | | Antioxidant, free radical scavenging and liver protective effects of friedelin isolated from Azima tetracantha Lam. leaves.[Pubmed: 23561182] | The aim of the present study was to evaluate the antioxidant, free radical scavenging and liver protective effects of friedelin isolated from Azima tetracantha Lam. leaves.
METHODS AND RESULTS:
In in vitro antioxidant study, the free radical scavenging effect of friedelin on 2,2-diphenyl-picrylhydrazyl (DPPH), hydroxyl, nitric oxide and superoxide radicals were evaluated. Friedelin showed very good scavenging effect on DPPH (IC50 21.1 mM), hydroxyl (IC50 19.8 mM), nitric oxide (IC50 22.1 mM) and superoxide (IC50 21.9 mM) radicals. Friedelin also showed strong suppressive effect on lipid peroxidation. In in vivo antioxidant study, CCl4 induced oxidative stress on rats produced significant increase in serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and lactate dehydrogenase (LDH) levels along with reduction in liver superoxide dismutase (SOD), catalase (CAT), reduced glutathione (GSH) and glutathione peroxidase (GPx) levels. Pre-treatment of rats with friedelin at 40 mg/kg for 7 days restored these levels to normality and showed liver protection, comparable to the standard, silymarin (25 mg/kg).
CONCLUSIONS:
These results clearly demonstrated that friedelin possessed marked antioxidant and liver protective effects. | | Nat Prod Res. 2013 Mar;27(4-5):417-24. | | Friedelin and lanosterol from Garcinia prainiana stimulated glucose uptake and adipocytes differentiation in 3T3-L1 adipocytes.[Pubmed: 22988818] | Friedelin and lanosterol have been isolated from twigs of Garcinia prainiana. Their structures were elucidated by spectroscopic methods. The compounds were examined for their effects on 3T3-L1 adipocytes.
METHODS AND RESULTS:
In the MTT assay, it was found that the compounds had no cytotoxic effects up to 25 µM. Adipocyte differentiation analysis was carried out by Oil Red O staining method. In the presence of adipogenic cocktail (MDI), it was found that friedelin and lanosterol enhanced intracellular fat accumulation by 2.02 and 2.18-fold, respectively, compared with the vehicle-treated cells. Deoxyglucose uptake assay was used to examine the insulin sensitivity of adipocytes in the presence of the compounds. It was found that friedelin was able to stimulate glucose uptake up to 1.8-fold compared with insulin-treated cells.
CONCLUSIONS:
It was suggested that friedelin and lanosterol may be beneficial to mimic insulin action that would be useful in the treatment of diabetes type 2 patients. | | Pharm Biol . 2018 Dec;56(1):363-367. | | In vitro inhibitory effects of Friedelin on human liver cytochrome P450 enzymes[Pubmed: 30122094] | | Abstract
Context: Friedelin is a triterpenoid with several biological activities. However, the affects of Friedelin on the activity of human liver cytochrome P450 (CYP) enzymes remains unclear.
Objective: This study investigates the inhibitory effects of Friedelin on the major human liver CYP isoforms (CYP3A4, 1A2, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8).
Materials and methods: First, the inhibitory effects of Friedelin (100 μM) on the eight human liver CYP isoforms were investigated in vitro using human liver microsomes (HLMs), and then enzyme inhibition, kinetic studies, and time-dependent inhibition studies were conducted to investigate the IC50, Ki and Kinact/KI values of Friedelin.
Results: The results indicate that Friedelin inhibited the activity of CYP3A4 and 2E1, with the IC50 values of 10.79 and 22.54 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that Friedelin is not only a noncompetitive inhibitor of CYP3A4, but also a competitive inhibitor of CYP2E1, with Ki values of 6.16 and 18.02 μM, respectively. In addition, Friedelin is a time-dependent inhibitor of CYP3A4 with Kinact/Ki value of 4.84 nM/min.
Discussion and conclusion: The in vitro studies of Friedelin with CYP isoforms suggested that Friedelin has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4 and 2E1. Further clinical studies are needed to evaluate the significance of this interaction.
Keywords: CYP2E1; CYP3A4; drug–drug interactions. |
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| In vivo: |
| Eur J Pharmacol. 2015 Mar 5;750:167-75. | | Protective effects of friedelin isolated from Azima tetracantha Lam. against ethanol-induced gastric ulcer in rats and possible underlying mechanisms.[Pubmed: 25617794 ] | The current study was aimed to investigate the gastroprotective effects of friedelin isolated from the hexane extract of leaves of Azima tetracantha.
METHODS AND RESULTS:
Ethanol-induced gastric ulcer model was used to investigate the gastroprotective effects of friedelin. Antioxidant enzymes, lipid peroxidation, nitric oxide, gastric vascular permeability, pro and anti-inflammatory cytokines and apoptosis level have been investigated. Ethanol caused severe gastric damage and friedelin pretreatment protected against its deleterious role. Antioxidant enzyme activities, anti-inflammatory cytokines, prostaglandin E2 (PGE2), constitutive nitric oxide synthase (cNOS) and mucus weight have been increased significantly. However, the vascular permeability, pro-inflammatory cytokines, inducible nitric oxide synthase (iNOS), caspase-3 and apoptosis level have significantly been decreased after friedelin ingestion.
CONCLUSIONS:
The present study has clearly demonstrated the anti-ulcer potential of friedelin, these findings suggested that friedelin could be a new useful natural gastroprotective tool against gastric ulcer. | | South Indian Journal of Biological Sciences, 2015,1(1):34-3. | | Anti-Diarrhoeal Activity of Friedelin Isolated from Azima tetracantha Lam. in Wistar Rats.[Reference: WebLink] | The present study was aimed to evaluate the anti-diarrhoeal activity of Friedelin isolated from leaves of Azima tetracantha Lam.
METHODS AND RESULTS:
The anti-diarrhoeal effect of Friedelin was studied by using castor oil-induced diarrhoea, gastrointestinal motility test, magnesium sulphate-induced diarrhea and castor oil-induced enteropooling in rats. Friedelin (20 mg/kg) showed significant (P < 0.0001) reduction of intestinal transit and gastric emptying which were similar to the anti- motility activity as known compound atropine (0.1 mg/kg). Friedelin (20 mg/kg) also exerted significant anti-enteropooling effects, against castor oil-induced enteropooling in rats. The defaecation frequencies and the faecal droppings wetness were significantly (P < 0.0001) reduced. Additionally, Friedelin (20 mg/kg) revealed significant (P < 0.0001) inhibition (89.64%) of castor oil-induced diarrhea.
CONCLUSIONS:
The overall results elucidated that the anti-diarrhoeal activity of Friedelin may be due to its anti-secretory and anti-motility properties, which consequently provide evidence for the traditional claim. |
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