| Description: |
Gossypin has antidiabetic, antioxdiant, anticonvulsant, anti-allergic, antiinflammatory, antinociceptive, cytotoxic and antibacterial activities; it inhibits the NF-kappaB activation pathway, which may explain its role in the suppression of inflammation, carcinogenesis, and angiogenesis. Gossypin is a new hypocholesterolemic agent that up-regulates LDLR expression independent of SREBP-2 but is dependent on ERK activation. Gossypin has ameliorative effect against gentamicin-induced nephrotoxicity in rats. Gossypin also shows inhibitory effects on RANKL-induced osteoclast differentiation and bone resorption in murine macrophages (LB364). |
| In vitro: |
| Arch Pharm Res. 2004 Apr;27(4):454-9. | | Gossypin protects primary cultured rat cortical cells from oxidative stress- and beta-amyloid-induced toxicity.[Pubmed: 15180313] | The present study investigated the effects of Gossypin, 3,3',4',5,7,8-hexahydroxyflavone 8-glucoside, on the toxicity induced by oxidative stress or beta-amyloid (Abeta) in primary cultured rat cortical cells.
METHODS AND RESULTS:
The antioxidant properties of Gossypin were also evaluated by cell-free assays. Gossypin was found to inhibit the oxidative neuronal damage induced by xanthine/xanthine oxidase or by a glutathione depleting agent, D,L-buthionine (S,R)-sulfoximine. In addition, Gossypin significantly attenuated the neurotoxicity induced by Abeta(25-35). Furthermore, Gossypin dramatically inhibited lipid peroxidation initiated by Fe2+ and ascorbic acid in rat brain homogenates. It also exhibited potent radical scavenging activity generated from 1,1-diphenyl-2-picrylhydrazyl.
CONCLUSIONS:
These results indicate that Gossypin exerts neuroprotective effects in the cultured cortical cells by inhibiting oxidative stress- and Abeta-induced toxicity, and that the antioxidant properties of Gossypin may contribute to its neuroprotective actions. | | Indian Journal of Pharmacology,2008, 39(6):281-283. | | Free radical scavenging activity of gossypin and nevadensin: An in-vitro evaluation.[Reference: WebLink] | The antioxidant potential of Gossypin and nevadensin, two flavonoid compounds, were evaluated by in vitro methods.
METHODS AND RESULTS:
Gossypin, nevadensin, and the reference standard, butylated hydroxyl toluene (BHT), were evaluated for DPPH (1, 1-diphenyl-2-picrylhydrazyl), nitric oxide, superoxide, and hydroxyl radical scavenging activity. Gossypin and BHT showed the potential for significant DPPH radical inhibition of up to 88.52 and 91.45% at 100 μg/ml concentration. With a 100 μg/ml concentration of Gossypin, the in vitro nitric oxide, superoxide, and hydroxyl radical scavenging activity was found to be 74.00, 74.22, and 67.15%, respectively; and with 100 μg/ml of BHT the corresponding values were 82.24, 81.76, and 73.03% of inhibition, respectively.
CONCLUSIONS:
The study results showed that Gossypin has significant antioxidant activity. | | Natural Product Sciences,2007,13(4):300-303. | | Cytotoxic and antibacterial activities of gossypin.[Reference: WebLink] |
METHODS AND RESULTS:
Gossypin, a naturally occurring polyhydroxy flavonoid, when subjected to in vitro cytotoxic screening against vero cell lines exhibited 68.75% inhibition at a concentration of 1000 μg. When tested against five bacteria and five fungi, the flavone derivative showed a moderate activity against Staphylococcus aureus and Escherichia coli, mild inhibition against Pseudomonas aerugenosa and Salmonella typhi and no activity against any of the tested fungi, in the concentrations studied. | | Faseb Journal, 2014, 28. | | Inhibitory effects of gossypin on RANKL-induced osteoclast differentiation and bone resorption in murine macrophages (LB364)[Reference: WebLink] | Bone-remodeling imbalance between bone formation by osteoblasts and bone resorption by osteoclasts results in the metabolic bone diseases such as osteoporosis. Gossypin is a naturally-occurring bioflavonoid seen in vegetables and fruit, as being a treatment for melanoma.
METHODS AND RESULTS:
The present study investigated that 1-20 μM Gossypin suppressed RANKL-induced bone resorption in Raw 264.7 macrophages. To differentiate to osteoclasts, macrophages were treated with 50 ng/ml RANKL for 5 days. RANKL enhanced multi-nucleated osteoclast formation and tartrate-resistance acid phosphatase activity, which was dose-dependently attenuated by Gossypin. Western blot analysis revealed that Gossypin suppressed RANKL induction of integrin β3 and carbonic anhydrase II in macrophage-derived osteoclasts.
CONCLUSIONS:
These results demonstrate that Gossypin retarded the differentiation and activation of osteoclasts to be integrated on bone tissue. Therefore, Gossypin is a potent agent in alleviating bone resorption of osteoclasts. |
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| In vivo: |
| Phytother Res. 2009 Jun;23(6):878-84. | | Antiinflammatory and antinociceptive activities of gossypin and procumbentin--cyclooxygenase-2 (COX-2) inhibition studies.[Pubmed: 19107863] |
In the present study the antiinflammatory and antinociceptive activities of a few selected flavonoids were investigated.
METHODS AND RESULTS:
Procumbentin, Gossypin, chrysin and methylhespiridin were studied for antiinflammatory and antinociceptive activities using in vitro enzymatic assays and in animal models utilizing acetic acid-induced writhing in mice and hind paw edema in rats. In vitro studies were performed using TMPD (NNN'N'-tetramethyl-p-phenylene diamine) and oxygraphic methods for COX-1 (cyclooxygenase-1), COX-2, 5-LOX (5-lipoxygenase) and 15-LOX. Gossypin and procumbentin showed COX-2 inhibitory activity and exhibited IC(50) (COX-2/COX-1) ratios of 0.14 and 0.11, respectively. None of the flavonoids tested in this study showed LOX inhibitory activity. Four groups were studied for each test compound following intraperitoneal (i.p.) administration of doses of 10, 30 and 100 mg/kg. Antiinflammatory activity was measured by the carrageenin-induced rat hind paw edema model and antinociceptive activity by acetic acid-induced writhing.
CONCLUSIONS:
Procumbentin and Gossypin showed antinociceptive activity at the 100 mg/kg dose. Gossypin showed antiinflammatory activity at doses of 10, 30, 100 mg/kg. Procumbentin and Gossypin exhibited COX-2 inhibitory activity when tested by in vitro methods. Procumbentin and Gossypin showed antinociceptive, and Gossypin showed antiinflammatory, activities. | | J Diabetes. 2012 Mar;4(1):41-6. | | Antidiabetic activity of gossypin, a pentahydroxyflavone glucoside, in streptozotocin-induced experimental diabetes in rats.[Pubmed: 21722326] | Most of the currently available oral hypoglycemic drugs for the treatment of diabetes mellitus elicit detrimental side effects. Hence, the search for plant-derived products for the treatment of diabetes continues. Gossypin, a pentahydroxy flavone glucoside found in the flowers of Hibiscus vitifolius, has many biological properties, including as an antioxidant, anti-inflammatory and anticancer agent. The aim of the present study was to evaluate the effect of gossypin in streptozotocin (STZ)-induced experimental diabetes in rats.
METHODS AND RESULTS:
Diabetic rats were administered 20 mg/kg per day gossypin orally for 30 days. On the 28th day, rats were subjected to an oral glucose tolerance test. In addition, blood glucose, plasma insulin, hemoglobin, and HbA1c levels were determined, as was the glycogen content of the liver and muscles. Plasma protein and blood urea were also estimated.
Oral administration of gossypin to diabetic rats resulted in improved glucose tolerance. Increased blood glucose and HbA1c levels and the reduced plasma insulin and hemoglobin levels in diabetic rats were significantly reversed to near normal after oral administration of gossypin. Furthermore, the glycogen content of the liver and muscles was significantly improved after gossypin treatment of diabetic rats, and plasma protein and blood urea levels were almost normalized. The data obtained in gossypin-treated rats were comparable with those obtained following gliclazide treatment of rats, a standard reference drug for diabetes.
CONCLUSIONS:
The results of the present study indicate that gossypin has potent antidiabetic activity in STZ-induced experimental diabetes in rats. |
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