Angiogenesis plays a crucial role in malignant tumor progression and development. The present study aimed to identify lead plants with selective anti-angiogenic properties. A total of 26 methanolic extracts obtained from 18 plants growing in Saudi Arabia and Jordan that belong to the Lamiaceae family were screened for their cytotoxic and anti-angiogenic activities using MTT and rat aortic ring assays, respectively. Four novel extracts of Thymbra capitata (L.) Cav., Phlomis viscosa Poir, Salvia samuelssonii Rech.f., and Premna resinosa (Hochst.) Schauer were identified for their selective anti-angiogenic effects. These extracts did not exhibit cytotoxic effects on human endothelial cells (EA.hy926) indicating the involvement of indirect anti-angiogenic mechanisms. The active extracts are potential candidates for further phytochemical and mechanistic studies.
Huernia Sp. Nov. aff. Boleana, Apocynaceae, grows in the high mountains of southwest Saudi Arabia and is widely used as a remedy for the treatment of diabetes. The present study investigated the anti‑inflammatory, wound healing and inhibitory effects on migration of Huernia Sp. Nov. aff. Boleana. The anti‑inflammatory effect was assessed in mice using formalin‑induced edema. Wound healing effects were assessed in rats using a circular excision wound model. An in vitro 'scratch' test was used to investigate the inhibitory effects on melanoma cell (B16‑F10) migration. The anti‑inflammatory effects of total extract, hexane and chloroform fractions were greater or equal to indomethacin (control). The relatively non‑polar fractions (hexane and chloroform) exhibited higher anti‑inflammatory activities compared with the aqueous fraction. The percentage of wound contraction among animals treated with the plant extract was higher compared with the control; however, this difference was not statistically significant (P>0.05). The total plant extract increased wound healing by inhibiting the inflammatory response, promoting angiogenesis, and significantly promoting the proliferation of fibroblasts, particularly on days 7 and 14 post‑wounding. Furthermore, the plant extract promoted wound repair via the enhancement of collagen synthesis, and complete epithelization with well‑formed and differentiated epithelial tissues. The in vitro 'scratch' test indicated the inhibitory effects of this plant on melanoma cell migration in a dose‑dependent manner. The present study indicated that Huernia Sp. Nov. aff. Boleana may have potential as an anti‑inflammatory, wound-healing and migration-inhibiting ethno medicine.
Background: Limited drug penetration into solid tumors has been one of the potential causes of resistance to chemotherapy for the treatment of bladder cancer. The aim of the study is to develop non-toxic self-nanoemulsifying formulations (SNEFs) of paclitaxel and to evaluate their ability to serve as a tool increasing the stability and solubility of paclitaxel in formulations utilizing the drug intravesical administration. Methods:Various oil-in-water non-toxic self-nanoemulsifying formulations (SNEFs) were developed using Cremercoor MCT, Kollisolv MCT, Miglyol 812, 810, Capmul MCM, Imwitor 988, Imwitor 742 with TO106V, Tween 85, HCO30, Kolliphor EL and Cremophor RH40 at size ranges from approximately 19 to 110 nm that are capable of enhancing the solubility and stability of paclitaxel. Visual assessment and droplet size measurements were taken into initial consideration for optimised SNEFs. Paclitaxel was added with the oil/surfactant mixture before dispersing the mixture in water to form SNEF. The cytotoxicity of the optimal SNEFs was compared with the raw paclitaxel dispersion in vitro. Results: Initial characterisation and solubility studies showed that mixed glycerides of Kollisolv MCT/Imwitor 742 with water-soluble surfactant (high HLB) containing formulations generated highly efficient SNEFs as they are stable and produced lower nanodroplets with higher drug loading. The results have demonstrated that the SNEFs have good ability to retain its characteristics under conditions similar to that found in the urinary bladder up to 48 hours. However, the results also showed that chemosensitivity of cancer cells exposed to paclitaxel was attenuated in the presence of SNEFs. Larger size SNEFs have shown to induce more inhibitory effects on paclitaxel activity. Conclusion: optimised SNEFs have demonstrated the ability to enhance the solubility of paclitaxel with stable construction of SNEFs under variable physiological conditions. The reduction of the efficacy of SNEF-loaded paclitaxel indicates a strong encapsulation of the drug within the nano-carriers causing limitation in drug release. Such drug encapsulation may facilitate the penetration due to reduced cellular metabolism the drug. Further investigations are warranted.
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