| Description: |
Protosappanin B possesses antitumor, anti-inflammation and anti-oxidation properties, it protects PC12 cells against oxygen–glucose deprivation-induced neuronal death by maintaining mitochondrial homeostasis via induction of ubiquitin-dependent p53 protein degradation. |
| Targets: |
MMP(e.g.TIMP) | p53 | Caspase | Bcl-2/Bax | NOS | NO |
| In vitro: |
| Integr Cancer Ther. 2016 Mar;15(1):87-95. | | Antitumor Effects of Purified Protosappanin B Extracted From Lignum Sappan.[Pubmed: 26036624 ] | To assess the antitumor effects of protosappanin B extracted from Lignum Sappan.
METHODS AND RESULTS:
Lignum Sappan was sequentially extracted by boiling water and ethyl acetate. The resulting extract was separated by column chromatography, to yield protosappanin B. The compound was then identified by thin-layer chromatography, high-performance liquid chromatography, elemental analysis, and spectrometry (infrared and ultraviolet). The effects on tumor cell viability and growth of purified protosappanin B were evaluated in vitro by trypan blue exclusion and MTT assays, respectively. And the effects of protosappanin B were assessed in vivo, on H22 mouse liver cancer cell invasion and the survival of tumor-bearing mice.
Protosappanin B (2 mg/mL) reduced the viability of human bladder cancer T24 cells and mouse bladder cancer BTT cells in a time-dependent manner (P < .05) and significantly inhibited the growth of the human colon cancer cell lines HCT-116 and SW-480. IC50 values of 21.32, 26.73, and 76.53 µg/mL were obtained for SW-480, HCT-116, and BTT cells, respectively, after 48 hours of treatment with protosappanin B. In addition, pretreatment of H22 cells with protosappanin B (final concentration = 6.25 mg/mL) resulted in complete inhibition of tumor formation in KM mice. Furthermore, protosappanin B (200 and 300 mg/kg) significantly increased the survival of BTT tumor-bearing T739 mice, at a rate comparable to that of 1 mg/kg mitomycin.
CONCLUSIONS:
Protosappanin B extracted from Lignum Sappan exerts marked antitumor effects both in vitro and in vivo. |
|
| In vivo: |
| J Ethnopharmacol. 2013 Jul 9;148(2):682-90. | | An LC/MS/MS method for simultaneous quantitation of two homoisoflavones: protosappanin B and brazilin with hypoglycemic activity in rat plasma and its application to a comparative pharmacokinetic study in normal and streptozotocin-treated rats.[Pubmed: 23707335] | The heartwood of Caesalpinia sappan L. (Leguminosae), a widely used Chinese medicine in folk, has been used for the treatment of traumatic injury, stasis pain, amenorrhea, dysmenorrheal, as well as stabbing pain in the chest, abdomen and so on. Protosappanin B and brazilin, as the major bioactive homoisoflavones of Sappan Lignum, are used as the marker components for the quality control of the herb in China Pharmacopoeia. To establish a sensitive LC/MS/MS method for investigating the pharmacokinetic properties of Protosappanin B and brazilin in rats after oral administration of Sappan Lignum extract, and compare their pharmacokinetics difference between normal and streptozotocin-treated rats.
METHODS AND RESULTS:
A rapid, selective and sensitive LC/MS/MS method was developed and validated for the simultaneous quantification of Protosappanin B and brazilin in rat plasma. Normal and streptozotocin-treated rats were orally administered with the Sappan Lignum extract at the same dose of 2.83 g extract/kg body weight (equivalent to 35.56 mg/kg of Protosappanin B and 52.25 mg/kg of brazilin), respectively. After oral administration of Sappan Lignum extract, a remarkable increase (p<0.05) in the value of AUC0-24h, AUC0-∞, Cmax and T1/2 associated with Protosappanin B and brazilin was observed in the streptozotocin-treated group. Compared with the normal rats, elimination of both compounds in the streptozotocin-treated rats was slower.
CONCLUSIONS:
The established method was successfully applied to compare the pharmacokinetic behaviors of Protosappanin B and brazilin in rat plasma after oral administration of Sappan Lignum extract between normal and streptozotocin-treated groups; the results might suggest the accumulation of both compounds in diabetic pathologic states and the adverse reaction should be considered when it was used. |
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