Influence of Benincasa hispida Peel Extracts on Antioxidant and Anti-Aging Activities, including Molecular Docking Simulation.

Benincasa hispida peel, a type of postconsumer waste, is considered a source of beneficial phytochemicals. Therefore, it was subjected to investigation for biological activities in this study. B. hispida peel was extracted using 95% v/v, 50% v/v ethanol and water. The obtained extracts were B95, B50 and BW. B95 had a high flavonoid content (212.88 ± 4.73 mg QE/g extract) and phenolic content (131.52 ± 0.38 mg GAE/g extract) and possessed high antioxidant activities as confirmed by DPPH, ABTS and lipid peroxidation inhibition assays. Moreover, B95 showed inhibitory effects against collagenase and hyaluronidase with values of 41.68 ± 0.92% and 29.17 ± 0.66%, which related to anti-aging activities. Via the HPLC analysis, one of the potential compounds found in B95 was rutin. Molecular docking has provided an understanding of the molecular mechanisms underlying the interaction of extracts with collagenase and hyaluronidase. All extracts were not toxic to fibroblast cells and did not irritate the hen's egg chorioallantoic membrane, which indicated its safe use. In conclusion, B. hispida peel extracts are promising potential candidates for further use as antioxidant and anti-aging agents in the food and cosmetic industries.

In vitro bioactivities and preparation of nanoemulsion from coconut oil loaded Curcuma aromatica extracts for cosmeceutical delivery systems.

Curcuma aromatica (CA) is a herbaceous plant in the Zingiberaceae family. It has antioxidative activity and anti-inflammatory properties. The purpose of this study was to investigate the effect of solvents and extraction methods on CA rhizomes. The crude extracts were tested for phenolic and flavonoid contents, antioxidative activity by DPPH and lipid peroxidation assay, and protein denaturation inhibition. The crude extracts with 95% ethanol by maceration technique showed good results. It had phenolic content at 99.28 ± 1.09 mg GAE/g extract, flavonoid content at 397.00 ± 27.54 mg QE/g extract, antioxidative activity by DPPH assay and lipid peroxidation assay at IC50 value of 0.55 ± 0.02 mg/ml and 0.60 ± 0.10 mg/ml, respectively. The percentage of protein denaturation inhibition was 65.97 ± 4.68%. The crude extract with 95% ethanol by maceration technique was selected to formulate nanoemulsion. Nanoemulsion formulation consisted of DI water, Tween 80, CA extract, coconut oil and Span 80 at 72.50, 12.93, 7.07, 5.00 and 2.5%w/w, respectively. Its appearance was an opaque yellow liquid with no precipitation and no phase separation at room temperature. The particle size, pH, and viscosity were 70.20 ± 0.38 nm, 5.87 ± 0.01 and 3.56 ± 0.24 cP, respectively. Nanoemulsion loaded CA extract had bioactivities and highly stable characteristics after heating-cooling test for 6 cycles. This study has demonstrated the potential of nanoemulsion from coconut oil loaded CA extract for further development to novel cosmetic products.

Potent Anti-Proliferation on the Colon Cancer Cell Line (HT-29) of Liposomal Formulations Entrapped with Semi-Purified Job's Tears (Coix lacryma-jobi Linn.) Fractions.

Liposomes, entrapped with Job's Tears fractions, were prepared by the supercritical carbon dioxide fluid (scCO2) technique with and without sonication. Physical characteristics, which were the particle size, zeta potential, vesicular morphology, microviscosity and bioactivities including anti-proliferative, apoptotic and antioxidative activities of the S1L-S5L liposomal systems, were investigated. The potent anti-proliferative activity with the IC50 value of 4.44±2.31 ug/ml in a colon cancer cell (HT-29) was observed in the S5L. S5L also showed the apoptotic activity of 4.45±0.92% in an HT-29 cell. For antioxidative activities, the S3L showed the highest free radical scavenging activity and lipid peroxidation inhibition, whereas the S4L gave the highest metal chelating activity. This study has demonstrated the potent anti-proliferative activity on an HT-29 cell of the S5L liposomal formulation prepared by the scCO2 technique which can be further developed towards a novel anticancer drug.

Potent in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job's tear (Coix lacryma-jobi Linn.) extracts on human colon adenocarcinoma (HT-29) xenografted mice.

The in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job's tear (Coix lacryma-jobi Linn.) extracts (S5L), prepared by supercritical carbon dioxide fluid technique, on human colon adenocarcinoma (HT29) xenografted mice were investigated. For the stability and the physicochemical characteristics, S5L showed a high stability of pH, good dispersibility, small particle size and stable zeta potential. Liposomes can protect linoleic acid in the extract comparing with the free S5. S5L kept at 4 °C for 3 months showed the highest linoleic acid content of 63.50%, whereas at 45 °C, the lowest linoleic acid content of 42.66% was observed. The anticancer activity and toxicity on xenografted mice were observed for 14 days. At the end of the experiment, the relative tumor volume (RTV) in the S5L-treated xenografted mice showed a significant RTV reduction. The high dose of S5 and S5L were potent with the highest inhibition of tumor growth of 48.67 and 54.75%, which was 86.94% and 97.81% of 5-fluorouracil, respectively. The apoptotic activity was shown in xenografted mice treated with S5 at medium and high dose, S5L, 5-fluorouracil and commercial product. All treated xenografted mice showed no toxic signs and symptoms, abnormality of internal organs histopathology and blood chemistry. This study has demonstrated the high physicochemical stability of liposomes encapsulated with semi-purified Job's tear extract and their potent anticancer activity on human colon adenocarcinoma xenografted model with the potential for further development to anticolon cancer drug.

Potent in vitro anti-proliferative, apoptotic and anti-oxidative activities of semi-purified Job's tears (Coix lachryma-jobi Linn.) extracts from different preparation methods on 5 human cancer cell lines.

ETHONOPHARMACOLOGICAL RELEVANCES: Job's tears (Coix lacryma-jobi Linn.) is commonly used as an herbal medicine. The low incidence of cancer has been observed in the area of China where regularly consume Job's tears. The effects of preparation methods of Job's tears on anti-cancer activities were investigated. Potent in vitro anti-proliferative, apoptotic and anti-oxidative activities of semi-purified Job's tears extracts from different preparation methods on 5 human cancer cell lines comparing with standards and commercial product were observed. AIM OF STUDY: To study the anti-proliferative, apoptotic and anti-oxidative activities of semi-purified Job's tear extracts from different preparation methods on 5 human cancer cell lines. MATERIALS AND METHODS: The crude methanolic extracts of non-cooked, steamed and roasted Job's tears cultivars were prepared and further semi-purified by liquid-liquid extraction techniques. Both of crude and semi-purified extracts were tested for anti-proliferative, apoptotic induction, anti-oxidative activities and phytochemicals content. RESULTS: The highest yields of crude and-purified extracts were 4.60% and 1.46%, respectively. In crude extracts, the steamed whole Thai Black Loei Job's tears (W-TBL-S1) extract showed the highest anti-proliferative activity in mouth epidermal carcinoma cell (KB) at the IC50 of 43.61±0.76µg/ml (0.005 folds of doxorubicin), whereas the roasted whole Laos White Loei Job's tears (W-LWL-R2) extract showed the highest apoptotic activity in cervical adenocarcinoma (HeLa) at 21.52±1.50% (0.22 and 15.05 folds of doxorubicin and commercial product, respectively). After liquid-liquid extraction, almost all of the semi-purified extracts showed increases in anti-proliferative activity. Ethyl acetate fraction of the roasted whole Laos White Loei Job's tears (W-LWL-R2) showed the highest anti-proliferative activity in HeLa cell at the IC50 of 0.97±0.82µg/ml (7.82 and 45.39 folds of doxorubicin and crude extract, respectively) and apoptotic activity of 18.77±6.31% (0.19 folds of doxorubicin). The commercial product showed no anti-proliferative activity in all cell lines but induced apoptosis in HeLa cell at 1.43±0.34%. The butanol and hexane soluble fractions of the roasted whole of Laos White Loei Job's tears (W-LWL-R2) showed the highest free radical scavenging (SC50) and metal chelating activity (MC50) of 0.31±0.06mg/ml (0.64 folds of ascorbic acid) and 0.08±0.01mg/ml (6.37 folds of EDTA), respectively. All ethyl acetate fractions contain high content of carotenoid and tannin, whereas the hexane soluble fraction of the roasted hull of Laos Black Loei Job's tears (H-LBL-R1) showed the highest linoleic acid content of 8.09±0.74% w/w. CONCLUSIONS: This study has demonstrated the potent anti-cancer activity of the semi-purified extracts from roasted Job's tears with high potential for further development to modern anti-cancer drug.

In vitro anti-cancer activities of Job's tears (Coix lachryma-jobi Linn.) extracts on human colon adenocarcinoma.

The whole seed (W), endosperm (E) and hull (H) of five cultivars of Job's tears (Coix lachryma-jobi Linn. var. ma-yuen Stapf) including Thai Black Phayao, Thai Black Loei, Laos Black Loei, Laos White Loei and Laos Black Luang Phra Bang were processed before solvent extraction by non-cooking, roasting, boiling and steaming Each part of the Job's tears was extracted by the cold and hot process by refluxing with methanol and hexane. The total of 330 extracts included 150 methanol extracts and 180 hexane extracts were investigated for anti-proliferative activity on human colon adenocarcinoma cell line (HT-29) by the sulforhodamine B (SRB) assay. The extracts which gave high anti-proliferative activity were tested for apoptotic activity by acridine orange and ethidium bromide double staining and anti-oxidative activities including free radical scavenging and lipid peroxidation inhibition activities. The extract from the hull of Thai Black Loei roasted before extracting by hot methanol (M-HTBL-R2) showed the highest anti-proliferative activity on HT-29 with the IC50 values of 11.61 ± 0.95 µg/ml, while the extract from the non-cooked hull of Thai Black Loei by cold methanol extraction (M-HTBL-N1) gave the highest apoptosis (8.17 ± 1.18%) with no necrosis. In addition, M-HTBL-R2 and M-HTBL-N1 indicated free radical scavenging activity at the SC50 values of 0.48 ± 0.12 and 2.47 ± 1.15 mg/ml, respectively. This study has demonstrated the anti-colorectal cancer potential of the M-HTBL-R2 and M-HTBL-N1 extracts.

Hypoglycemic activity and stability enhancement of human insulin-tat mixture loaded in elastic anionic niosomes.

This study aimed to investigate the synergistic effect of trans-activator of transcription (Tat) and niosomes for the improvement of hypoglycemic activity of orally delivered human insulin. The elastic anionic niosomes composing of Tween 61/cholesterol/dicetyl phosphate/sodium cholate at 1:1:0.05:0.02 molar ratio loaded with insulin-Tat mixture (1:3 molar ratio) was prepared. Deformability of the elastic anionic niosomes decreased after loaded with the mixture of 1.35 times. For the in vitro release, the insulin (T10 = 4 h) loaded in the elastic anionic niosomes indicated the slower release rate than insulin in the mixture (T10 = 3 h) loaded in niosomes. At room temperature (30 ± 2 °C), the mixture loaded in elastic anionic niosomes was more chemical stable than the free mixture of 1.3, 1.4 and 1.7 times after stored for 4, 8 and 12 weeks, respectively. Oral administration in the alloxan-induced diabetic mice of the mixture loaded in elastic anionic niosomes with the insulin doses at 25, 50 and 100 IU/kg body weight indicated significant hypoglycemic activity with the percentage fasting blood glucose reduction of 1.95, 2.10 and 2.10 folds of the subcutaneous insulin injection at 12 h, respectively. This study has demonstrated the synergistic benefits of Tat and elastic anionic niosomes for improving the hypoglycemic activity of the orally delivered human insulin as well as the stability enhancement of human insulin when stored at high temperature. The results from this study can be further developed as an effective oral insulin delivery.

Anticancer activities of the extract from Longkong (Lansium domesticum) young fruits.

UNLABELLED: "Longkong"(Lansium domesticum Corr., Family: Meliaceae) is a fruit found in the south of Thailand. This plant has been used in traditional medicines. OBJECTIVES: To investigate the antiproliferative activities and the phytoconstituents of Longkong extracts. MATERIALS AND METHODS: Cytotoxicity and apoptotic activity of 48 extracts were tested using the SRB assay and acridine orange (AO)/ethidium bromide (EB) staining, respectively. The extracts which gave the highest anticancer activity were selected to prepare the semipurified extracts and analysis for the constituents by gas chromatography-mass spectrometry (GC/MS). RESULTS: The highest percentage yield (59.38%) was from the cold water extract of Longkong ripe fruits (RFWC). The highest total phenolic and flavonoid contents were observed in cold and hot methanol extract of Longkong stalks (STMC and STMH). The hot and cold chloroform young Longkong fruit extracts (YFCH and YFCC) exhibited a cytotoxic effect (IC(50) < 1 mg/mL) against cancer cells. For apoptotic induction, YFCH demonstrated the highest activity against KB of 13.84 ± 4.21% at 0.5 mg/mL which was 0.88 and 1.35 times of cisplatin and 5-FU, respectively, while apoptotic cells in HT-29 were 8.68 ± 1.85% at 5 mg/mL, which was 0.61 and 1.43 times of cisplatin and 5-FU, respectively. YFCC showed the highest apoptotic effect against KB cells at 10.70 ± 2.15% at 0.5 mg/mL, which was 0.68 and 1.07 times of cisplatin and 5-FU, respectively. The major phytoconstituents in YFCH were hexadecanoic acid (11.53%) and ethyl oleate (10.58%). DISCUSSION AND CONCLUSION: The crude extracts of Longkong showed anticancer activities and may provide new lead compounds for the development of anticancer products.

Anti-proliferative and apoptosis induction activities of extracts from Thai medicinal plant recipes selected from MANOSROI II database.

UNLABELLED: ETHONOPHARMACOLOGICAL RELEVANCES: Traditional medicines have long been used by the Thai people. Several medicinal recipes prepared from a mixture of plants are often used by traditional medicinal practitioners for the treatment of many diseases including cancer. The recipes collected from the Thai medicinal text books were recorded in MANOSROI II database. Anticancer recipes were searched and selected by a computer program using the recipe indication keywords including Ma-reng and San which means cancer in Thai, from the database for anticancer activity investigation. AIM OF STUDY: To investigate anti-cancer activities of the Thai medicinal plant recipes selected from the "MANOSROI II" database. MATERIALS AND METHODS: Anti-proliferative and apoptotic activities of extracts from 121 recipes selected from 56,137 recipes in the Thai medicinal plant recipe "MANOSROI II" database were investigated in two cancer cell lines including human mouth epidermal carcinoma (KB) and human colon adenocarcinoma (HT-29) cell lines using sulforhodamine B (SRB) assay and acridine orange (AO) and ethidium bromide (EB) staining technique, respectively. RESULTS AND CONCLUSIONS: In the SRB assay, recipes NE028 and, S003 gave the highest anti-proliferation activity on KB and HT29 with the IC(50) values of 2.48±0.24 and 6.92±0.49µg/ml, respectively. In the AO/EB staining assay, recipes S016 and NE028 exhibited the highest apoptotic induction in KB and HT-29 cell lines, respectively. This study has demonstrated that the three Thai medicinal plant recipes selected from "MANOSROI II" database (NE028, S003 and S016) gave active anti-cancer activities according to the NCI classification which can be further developed for anti-cancer treatment.