Croton stellatopilosus (Plaunoi) leaves accumulate several diterpenes and possess various pharmacological activities. The present study aimed to prepare, characterize and assess the antibacterial activity of inclusion complexes prepared by mixing plaunotol (PL) or plaunoi extract (PE) with cyclodextrins (CD), including α-CD, β-CD, γ-CD, and hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were characterized using SEM, XRD, DSC, and FT-IR and evaluated for aqueous solubility and thermal stability. The PL and PE lyophilized complexes with HP-β-CD were further evaluated for their antibacterial activity against acne-causing bacteria. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of PL, PE, and the inclusion complexes evaluated using the agar dilution method revealed that the MIC and MBC values of the inclusion complexes were lower than those of PL or PE alone. Interestingly, the complexes had a synergistic activity with clindamycin after testing with checkerboard assay. The hydrogel containing the inclusion complex and clindamycin were assessed for antibacterial activity using the agar well diffusion method. The results indicated that the hydrogels showed significant inhibition of bacterial growth. In conclusion, the prepared solid dispersion of PL or PE with HP-β-CD could enhance antibacterial activity by increasing the drug solubility. The hydrogels containing PL or PE complex and clindamycin could be considered as a candidate for the treatment of acne vulgaris.

01 Apr 2013·Journal of Natural MedicinesQ4 · MEDICINE

Protective effect of plaunotol against doxorubicin-induced renal cell death

Q4 · MEDICINE

Article

Author: Pithi Chanvorachote ; Wanchai De-Eknamkul ; Chatchai Chaotham

In searching for a safe and effective compound to be used as a chemoprotective agent to prevent toxicity of the anthracyclin doxorubicin to renal cells, the present study demonstrated that plaunotol, a purified acyclic diterpene from Croton stellatopilosus Ohba, showed potential protection against doxorubicin-induced cell death in human proximal tubule cells. Treatment of renal cells with doxorubicin resulted in a significant decrease in viability of the cells, and we next proved that such toxicity was mainly due to apoptotic cell death. Pretreatment of the cells with plaunotol for at least 9 h prior to doxorubicin exposure improved the cells' survival. Plaunotol was shown to up-regulate the anti-apoptotic myeloid cell leukemia-1 (Mcl-1) level whereas it had no effect on the Bcl-2 level. The reduction in Mcl-1 after doxorubicin treatment was shown to be closely associated with the toxic action of the drug, and the increase in Mcl-1 induced by plaunotol pretreatment was able to prevent cell death induced by doxorubicin. Furthermore, the protective effect of plaunotol was evaluated in human lung and melanoma cells. Results indicated that plaunotol had no significantly protective effect in human lung carcinoma cells, whereas it sensitized melanoma cells to drug-induced cell death.

01 Jan 2013·BioMed Research InternationalQ3 · BIOLOGY

Acute and Chronic Oral Toxicity of a Partially Purified Plaunotol Extract fromCroton stellatopilosusOhba

Q3 · BIOLOGY

ArticleOA

Author: Chivapat, Songpol ; De-Eknamkul, Wanchai ; Chaotham, Chatchai ; Chaikitwattana, Anan

Plaunotol, an acyclic diterpenoid with highly effective antigastric ulcer properties, has been commercially isolated from leaves ofCroton stellatopilosusOhba. This Thai medicinal plant was traditionally used in the form of crude extracts, suggesting that it is possible to administer these plaunotol-containing extracts without toxicity. To confirm its safety, the oral toxicity of a partially purified plaunotol extract (PPE) was evaluatedin vivo. The PPE was simply prepared by 95% ethanol reflux extraction followed by hexane partition. The obtained extract was analyzed and found to contain 43% w/w of plaunotol and another compound, likely a fatty acid-plaunotol conjugate that is considered a major impurity. Oral administration of PPE to ICR mice and Wistar rats was conducted to evaluate acute and chronic toxicity of the plaunotol extract, respectively. The acute toxicity study demonstrated that PPE was practically nontoxic based on its high median lethal dose value (LD50=10.25 g/kg). The chronic toxicity studies also showed the absence of mortality and clinical symptoms in all rats treated with 11–1,100 mg/kg/day of PPE during a 6-month period. Histopathological and hematological analyses revealed that altered liver and kidney function and increased blood platelet number, but only at the high doses (550–1,100 mg/kg/day). These results suggest that PPE is potentially safe for further development as a therapeutic agent in humans.

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