A systematic review with meta-analysis on the antihypertensive efficacy of Nigerian medicinal plants.

ETHNOPHARMACOLOGICAL RELEVANCE: Despite the promising effects of herbal preparations in lowering blood pressure (BP), hypertension remains a major clinical challenge in Nigeria. The BP-lowering effects of medicinal plants are due to the presence of bioactive compounds. AIM OF THE STUDY: This meta-analysis presents a precise estimate of the therapeutic benefits of medicinal plants utilized in Nigeria for the management of hypertension in animals and humans. METHODS: A systematic literature search was performed through Cochrane, PubMed, Science Direct and Scopus databases from inception until February 28, 2021 using search terms related to randomized controlled trials of Nigerian medicinal plants for hypertension. Additional studies were identified through manual search. BP was the main outcome that was measured after the intervention. Meta-analysis was performed using the Review Manager and Meta-Essential. RESULTS: Nineteen trials comprising of 16 preclinical and 3 clinical studies were enrolled for the meta-analysis. A total number of 16 plants was identified of which H. sabdariffa was the highest reported plant. The plant extracts significantly lowered the systolic blood pressure (SBP) and diastolic blood pressure (DBP) of the hypertensive subjects compared to control. Weighted mean difference (WMD) for SBP (-43.60 mmHg, 95% CI: -63.18, -24.01; p<0.0001) and DBP (-29.50 mmHg, 95 CI: -43.66, -15.34; p<0.0001) was observed for the preclinical studies. For clinical trials, the WMD was -13.98 mmHg, 95 CI: -19.08, -8.88; p<0.00001 for SBP and -10.00 mmHg, 95 CI: -12.22, -7.78; p<0.00001 for DBP. High heterogeneity was observed for the outcome measures of preclinical studies, but not for the clinical studies. The observed substantial heterogeneity in preclinical studies may be linked to methodological shortcomings as evidenced by the results of the risk of bias assessment. There was no evidence of publication bias in animal trials for BP using the funnel plot and Egger's regression test (SBP, p=0.239 and DBP, p=0.112). CONCLUSIONS: This study provides evidence of medicinal preparations for the treatment of hypertension. A well-conducted trial with methodological rigour and a longer duration of follow-up is required for their effective clinical utilization.

Limonoids and tricyclic diterpenoids from Azadirachta indica and their antitumor activities.

The chemical constituents of the roots, seeds, and bark of Azadirachta indica var. siamensis were investigated, leading to the isolation of six tricyclic diterpenoids and five limonoids, including two new compounds (2, 5). The structures were elucidated based on NMR spectroscopic techniques, mass spectrometry and single-crystal X-ray diffraction as well as comparison with the literature. Moreover, the cytotoxicity activities of the isolates were evaluated. The results indicated that the compounds 1-3, 5-9 exhibited cytotoxicities against one or more cancer cell lines tested, with IC50 values in the range of 1.7-88.1 µM. The mechanism of action studies indicated that the most active compound, compound 5, could induce the apoptosis of AZ521 cells. Furthermore, the Western blot analysis showed that compound 5 could reduce the expression levels of procaspases-3, -8, -9 and promote the expression of Bid and AIF.

A biological active artificial saliva formulation containing flower mucilage from Ceylon Spinach (Basella alba Linn.).

Ceylon Spinach (Basella albe) is an edible perennial vine found in tropical Asia and Africa, known as vegetables containing mucilage. Its mucilage from flowers was extracted by microwaving and precipitated with 95% ethanol. Five artificial saliva formulations composing of mucilage from Ceylon Spinach, calcium chloride (CaCl2), potassium chloride (KCl) and sodium fluoride (NF) were developed. The best formulation No.5 containing 0.61% of the mucilage with the non-Newtonian pseudoplastic flow (8.9 ± 0.2 cP) and the wetting time (12.50 ± 2.24 min) similar to the normal human saliva was selected. This artificial saliva formulation exhibited biological activities including an antioxidative activity by DPPH free radical scavenging with the SC50 of 14.26 ± 2.00 mg/ml (0.05 folds of ascorbic acid), and the adhesion inhibition of S. mutans on hydroxyapatite beads at 17.01 ± 7.75%, while the natural human saliva exhibited an increase bacterial adhesion of 33.10 ± 9.70%. The safety of this formulation which gave no cytotoxicity on normal human gingival fibroblasts at 99.20 ± 21.09% cell viability was also demonstrated. The results from this study have indicated high biological activity and safety of the developed formulation containing mucilage from Ceylon Spinach which is potential to be used as artificial saliva for xerostomia patients.

Potent in vitro Anti-mouth Cancer (KB) and Immunostimulating Activities of the Job's Tears (Coix lachryma-jobi Linn.) Seed Semi-purified Extract Cocktails Containing Linoleic Acid.

The crude methanolic and hexane extracts of non-cooked, steamed and roasted from three Job's Tears cultivars were prepared and further semi-purified by liquid-liquid extraction techniques and silica gel column. The six single semi-purified extracts (F1-F6) were combined as nine cocktails (CT1, CT6, CT8, CT13, CT14, CT21, CT24, CT25 and CT31) according to the IC50 values from the preliminary study and investigated for anti-proliferative and apoptotic induction on mouth cancer cell line (KB) and immunostimulating as well as antioxidative activities. The highest anti-proliferative activity was observed in CT13 showing the IC50 value of 0.53±0.45 µg/mL which was higher than 5-fluorouracil and doxorubicin of 20.34 and 1.60 times, respectively. CT1 which was the combination of F1-F6 and CT13 which was the combination of F4-F6 exhibited significant strong synergistic activity with the combination index value (CI) of 0.28. CT1 at 200 µg/mL showed the highest percentages of apoptotic cells (40.65±10.97%) with no necrotic cells, but lower than cisplatin (100 µg/mL) of 2.18 times. CT14 gave the highest immunostimulating activity with the phagocytosis percentage of 13.0±1.7%, but lower than lipopolysaccharide of 1.08 times. CT31 gave the highest free radical scavenging and metal chelating activities with the SC50 and MC50 values of 0.73±0.07 and 1.99±0.24 µg/mL, but lower than ascorbic acid and EDTA of 18.25 and 4.33 times, respectively. The linoleic acid contents related to anti-cancer activity were also examined by HPLC. This study has demonstrated that CT1 composing of F1-F6 at the percentage ratio of 0.71:2.06:81.38: 8.47:4.92:2.46 was the potential cocktails of the semi-purified extracts from the Job's Tears which can be further developed as a novel active compound for oral cancer treatment.

Characterization, quantitation, similarity evaluation and combination with Na+,K+-ATPase of cardiac glycosides from Streblus asper.

Streblus asper Lour. (Moraceae) is a medicinal plant in Asian countries including India and Thailand, possessing activities of anti-tumor, anti-allergy, anti-parasitic and anti-bacterial. In this paper, characterization, quantitation and similarity evaluation of cardiac glycosides in different parts of S. asper were investigated by HPLC-Q-TOF-MS and chemometric methods. Then, the inhibition of Na+,K+-ATPase activity by the compounds isolated from S. asper was measured. Meanwhile, enzyme kinetics and molecular docking were determined to exhibit the combination modes between cardiac glycosides and Na+,K+-ATPase. As a result, twenty peaks of cardiac glycosides were assigned. Strophanthidin-3-O-α-l-rhamnopyranosyl-(1 → 4)-6-deoxy-ß-d-allopyranoside (1), glucostrebloside (2), strebloside (4) and mansonin (8) with a significant activity of inhibiting Na+,K+-ATPase (IC50 7.55-13.60 µM) were chosen for the determination of enzyme kinetics, exhibiting anticompetitive inhibitory characteristics towards Na+,K+-ATPase. Compound 4 could reasonably bind to the active sites of Na+,K+-ATPase, proved by molecular docking. Furthermore, the contents of the major compounds in four different parts of S. asper were extremely different, analyzed by chemometric methods, similarity analysis and principle compounds analysis. All these findings indicated that the contents of major compounds in different parts of S. asper were extremely different with a significant activity of inhibiting Na+,K+-ATPase, providing a reference for determination of effective part and administered dosage. The combination modes between cardiac glycosides and Na+,K+-ATPase were also revealed by enzyme kinetics and molecular docking, which provided a basis for further study of pharmacological activity.

Characteristics and in vitro anti-skin aging activity of gallic acid loaded in cationic CTAB niosome.

Physicochemical characteristics and in vitro anti-skin aging activity of gallic acid loaded in niosomes were investigated. Gallic acid was loaded in neutral (Brij 52/cholesterol at 7:3) and cationic CTAB niosomes (Brij 52/cholesterol/cetyltrimethylammonium bromide at 7:3:0.65). The maximum loading capacity and entrapment efficiency of gallic acid were 3.5, 4.48 ±â€¯2.10 in neutral and 50%, w/w, 10.94 ±â€¯0.78% in cationic CTAB niosomes, respectively. All gallic acid loaded in niosomes showed the unilamellar structure under transmission electron microscope with size range of 131.23-508.03 nm at initial and after storage for 3 months. The highest remaining percentage of gallic acid at all storage temperatures after 3 months was about 77% when loaded in the cationic CTAB niosome, whereas gallic acid in solution was about 64%. The release profiles of gallic acid loaded in neutral and cationic CTAB niosomes revealed the gradual release in 24 h. The cytotoxicity of gallic acid loaded in neutral and cationic CTAB niosomes appeared the non-cytotoxic effect in B16F10 melanoma cells and human skin fibroblasts. The cationic CTAB niosome loaded with gallic acid demonstrated the highest anti-skin aging activity, including melanin suppression effect (55.92 ±â€¯4.92% of control) by inhibition of tyrosinase (53.18 ±â€¯3.67% of control) and tyrosinase-related protein-2 (24.61 ±â€¯7.92% of control), antioxidant (87.03 ±â€¯0.99% cell viability) and inhibition of matrix metalloproteinase-2 (38.46 ±â€¯1.53% of control). This study has demonstrated the superior stability and anti-skin aging activity of gallic acid loaded in cationic CTAB niosome for potential utilization in pharmaceutical and 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.

Potential cancer chemopreventive and anticancer constituents from the fruits of Ficus hispida L.f. (Moraceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Ficus hispida L.f. (Moraceae) has been used as alternative for traditional medicine in the treatment of various ailments including cancer-cure. The aim of this study was to evaluate the cancer chemopreventive and anticancer activities of crude extracts of F. hispida, with the objective to screen the inhibition of Epstein-Barr virus early antigen, and cytotoxic active components, and provide foundation for potential applications of this promising medical plant. MATERIALS AND METHODS: Compounds were isolated from the MeOH extract of F. hispida fruits, and their structure elucidation was performed on the basis of extensive spectroscopic analysis. The isolated compounds were evaluated for their inhibitory activities against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells, and cytotoxic activities against human cancer cell lines (HL60, A549, SKBR3, KB, Hela, HT29, and HepG2) and a normal cell (LO2) using MTT method. For the compound with potent cytotoxic activity, its apoptosis inducing activity was evaluated by the observation of ROS generation level expression, and membrane phospholipid exposure and DNA fragmentation in flow cytometry. The mechanisms of the apoptosis induction were analyzed by Western blotting. RESULTS: Nineteen compounds, 1-19, including two new isoflavones, 3'-formyl-5,7-dihydroxy-4'-methoxyisoflavone (2) and 5,7-dihydroxy-4'-methoxy-3'- (3-methyl-2-hydroxybuten-3-yl)isoflavone (3), were isolated from the MeOH extract of F. hispida fruits. Five compounds, isowigtheone hydrate (1), 2, 3, 9, and 19, showed potent inhibitory effects on EBV-EA induction with IC50 values in the range of 271-340 molar ratio 32 pmol-1 TPA. In addition, five phenolic compounds, 1-3, 10, and 13, exhibited cytotoxic activity against two or more cell lines (IC50 2.5-95.8µM), as well as compounds 1 and 3 were also displayed high selectivity for LO2/HepG2 (SI 23.5 and 11.8, respectively), while the compound 1-induced ROS generation leads to activated caspases-3, -8, and -9 apoptotic process in HL60 cells. CONCLUSION: This study has established that the MeOH extract of F. hispida fruits contains isoflavones, coumarins, caffeoylquinic acids, along with other compounds including phenolics and steroid glucoside as active principles, and has demonstrated that the chemical constituents of F. hispida may be valuable as potential chemopreventive and anticancer agents.

Melanogenesis-Inhibitory and Cytotoxic Activities of Chemical Constituents from the Leaves of Sauropus androgynus L. Merr. (Euphorbiaceae).

A new steroid, 20-hydroxyisofucosterol (stigmasta-5,24(28)-diene-3ß,20ß-diol) (7), along with six known compounds 1 - 6 were isolated from the MeOH extract of the leaves of Sauropus androgynus L. Merr. (Euphorbiaceae). The structure of new steroid was determined by HR-APCI-MS and various NMR techniques in combination with literature data. Subsequently, their anti-inflammatory, cytotoxic activities against five human cell lines, as well as inhibitory activities against the α-MSH induced melanogenesis on the B16 cell line were evaluated. As the results, steroid compounds, 6 and 7 exhibited moderate cytotoxic to HL60, AZ521, SKBR3, and A549 tumor cell lines (IC50 26.9 - 45.1 µm) with high tumor selectivity for A549 relative to WI38 cell lines (SI 2.6 and 3.0, resp.). And, flavonoid compounds, 4 and 5 exhibited superior inhibitory activities against melanogenesis (67.0 - 94.7% melanin content), even with no or low toxicity to the cells (90.1 - 99.6% cell viability) at the concentrations from 10 to 100 µm. Furthermore, Western blot analysis suggested that compound 5 could inhibit melanogenesis by suppressing the protein expressions of MITF, TRP-1, TRP-2, and tyrosinase.

Biological Activities of Phenolics from the Fruits of Phyllanthus emblica L. (Euphorbiaceae).

Seven phenolic compounds, 1 - 7, including a new organic acid gallate, mucic acid 1-ethyl 6-methyl ester 2-O-gallate (7), were isolated from the MeOH extract of the fruits of Phyllanthus emblica L. (Euphorbiaceae). The structures were elucidated on the basis of extensive spectroscopic analysis and comparison with literature data. Upon evaluated for their antioxidant abilities by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. The inhibitory activities against melanogenesis in B16 melanoma cells induced by α-MSH, as well as cytotoxic activities against four human cancer cell lines were also evaluated. All phenolic compounds, 1 - 7, exhibited potent antioxidant abilities (DPPH: IC50 5.6 - 12.9 µm; ABTS: 0.87 - 8.43 µm Trolox/µm; FRAP: 1.01 - 5.79 µm Fe2+ /µm, respectively). Besides, 5 - 7, also exhibited moderate inhibitory activities against melanogenesis (80.7 - 86.8% melanin content), even with no or low toxicity to the cells (93.5 - 101.6% cell viability) at a high concentration of 100 µm. Compounds 1 - 3 exhibited cytotoxic activity against one or more cell lines (IC50 13.9 - 68.4%), and compound 1 with high tumor selectivity for A549 (SI 3.2).

Potent Phosphodiesterase Inhibition and Nitric Oxide Release Stimulation of Anti-Impotence Thai Medicinal Plants from "MANOSROI III" Database.

Seven plants in the top rank were selected from the "MANOSROI III" database using the two Thai keywords which meant impotence and sexual tonic. Boesenbergia rotunda (L.) Mansf. extract [EDP1-001(1)] gave the highest PDE inhibition activity of 4.36-fold sildenafil, a standard anti-impotence drug. Plumbago indica Linn. extract [EDP2-001(1)] exhibited the highest NO release stimulation activity of 666.85% which was 1.50-fold acetylcholine, a standard drug. Most selected plant extracts were nontoxic to EA.hy926 cells at 1.0 mg/mL. EDP1-001(1) exhibited the LD50 value of acute oral toxicity in male ICR mice of over 5,000 mg/kg body weight. EDP1-001(1) also indicated the improvement of sexual behaviors in the paroxetine-induced sexual dysfunction male mice with the evaluation of number of courtships (NC), mount frequency (MF), intromission frequency (IF), and ejaculatory frequency (EF) at 87.67 ± 6.17, 121.00 ± 23.50, 36.00 ± 3.21, and 13.67 ± 2.96 which were 2.63-, 1.27-, 0.53-, and 0.62-fold sildenafil-treated mice at day 14 of the treatments, respectively. The present study has not only confirmed the traditional use of Thai plants for the treatment of ED but also indicated the potential and application of the "MANOSROI III" database for Thai plant selection to be developed as ED food supplements.

Transfollicular enhancement of methyl myristate loaded in cationic niosomes incorporated in hair lotion.

Hair lotion containing methyl myristate loaded in cationic niosomes (HL-MMnio) composed of Brij72/cholesterol/DDAB at 7:3:0.65 molar ratio was developed. The remaining percentages of MM loaded in cationic niosomes in hair lotion were higher than free MM in hair lotion of about 1.2 times. The cumulative amounts in porcine skin and the receiver compartment of MM loaded in cationic niosomes incorporated in hair lotion were higher than those of free MM in hair lotion of 1.45 and 1.32 times, respectively. HL-MMnio showed very slightly irritation on rabbit skin, which was disappeared after 4 d. For melanogenesis induction in C57BL/6 mice with aged-induced grey body coat hairs, the highest pigmentation scores of HL-MMnio applied on the dorsal area were observed after 21 days, while hair lotion containing the free MM indicated after 35 days. This study has suggested that HL-MMnio was the high potential formulation for canities treatment.

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.

BIOASSAY-GUIDED FRACTIONATION AND ANTIHYPERTENSIVE PROPERTIES OF FRACTIONS AND CRUDE EXTRACTS OF PERISTROPHE BICALYCULATA (RETZ) NEES.

Hypertension is an important public health issue in both developed and developing countries due to its high incidence and morbidity. This has motivated researchers especially in developing countries to search for strategies for the treatment using different plant parts. The use of the aqueous decoction of the leaves of Peristiophe bicalyculata in the treatment of hypertension has been documented. This study was designed to carry out a bioassay-guided isolation of the antihypertensive components of the leaves of Peristrophe bicalyculata in L-NAME hypertensive rats, determine the angiotensin-converting enzyme inhibitory activity of the extracts and fractions obtained and identify the constituent(s) present. From our results, L-NAME hypertensive rats given the cold water extract had significantly (p < 0.05) lower mean arterial blood pressure (MABP) with longer duration of action than other extracts. Also, the angiotensin-converting enzyme inhibitory activity of the cold water extract was significantly (p < 0.05) higher than that of other extracts. From the GC-MS analysis of the most effective fraction (fraction 4), P,P,P-triphenyl-imino(triphenyl)phosphorane and andrographolide 2(3H)-furanone were identified among others. The present work demonstrates the hypotensive effect of the cold water extract of Peiistiophe bicalyculata on L-NAME hypertensive rats, which further justifies the folkloric application of extracts of the plant in the management as well as treatment of hypertension.

Potent Antiproliferative Effect on Liver Cancer of Medicinal Plants Selected from the Thai/Lanna Medicinal Plant Recipe Database "MANOSROI III".

Thai/Lanna medicinal plant recipes have been used for the treatment of several diseases including liver cancer. In this study, methanolic extracts (MEs) of 23 plants were tested for antiproliferative activity on human hepatoma cell line (Hep G2) by the sulforhodamine B (SRB) assay. Nine MEs with potent antiproliferative activity (IC50 < 100 µg/mL) were obtained and further semipurified by liquid/liquid partition extraction. The semipurified fractions were tested for the antiproliferative and antioxidative activities. ME of Stemona collinsae and the semipurified extract and methanol-water fraction (MF) of Gloriosa superba gave the highest antiproliferative activity on HepG2 which were 4.79- and 50.07-fold cisplatin, respectively. The semipurified fractions showed an increased antiproliferative activity. MF of Caesalpinia sappan and HF of Senna alata showed the highest free radical scavenging and metal chelating activities, respectively. The compound in n-hexane fraction (HF) of Ventilago denticulata which showed an increase in antiproliferative activity comparing to its ME was isolated and identified as emodin. This study has demonstrated the potential of the ME from S. collinsae, MF from G. superba, and emodin isolated from V. denticulata, for further development as an antiliver cancer agent.

Physicochemical properties and biological activities of Thai plant mucilages for artificial saliva preparation.

CONTEXT: Plant mucilages can be found in various parts of several Thai plants, which can be used as thickening, moisturizing, and lubricating agents in artificial saliva formulations. OBJECTIVE: The objective of this study was to evaluate the physicochemical properties, biological activity, and cytotoxicity of Thai plant mucilages. MATERIALS AND METHODS: The mucilages from Thai plants were extracted by various processes (temperature and pH variation, microwave oven, steam, and Tris-HCl buffer extraction). The viscosity and the rheology were evaluated using viscometer. Antioxidative activities including DPPH radical scavenging and metal chelating activities were investigated. The mucilages were determined for cytotoxicity on normal human gingival fibroblasts and anti-adherent activity of Streptococcus mutans. RESULTS: Mucilages from Ocimum citriodorum Vis. (Lamiaceae), Artocarpus heterophyllus Lam. (Moraceae), Abelmoschus esculentus (Linn.) Moench. (Malvaceae), and Basella alba Linn. (Basellaceae) exhibited pseudoplastic non-Newtonian rheology. The highest DPPH radical-scavenging and metal-chelating activities were observed in the mucilages from B. alba (microwave, 3 min) and A. esculentus (microwave, 1 min) with the SC50 and MC50 values (50% of scavenging activity and 50% of metal chelating activity, respectively) of 0.71 ± 0.32 and 1.11 ± 0.52 mg/ml, respectively. Most mucilages exhibited no cytotoxicity to normal human gingival fibroblasts. The mucilage from A. esculentus (microwave, 5 min) gave the shortest wetting time of 2.75 ± 0.51 min. The highest S. mutans adhesion inhibition was observed in A. esculentus (pH 11) of 5.39 ± 9.70%. DISCUSSION AND CONCLUSION: This study has indicated the suitable physicochemical and biological properties and the potential application of mucilages from Thai plants for artificial saliva preparation.

Potent anti-proliferative effects against oral and cervical cancers of Thai medicinal plants selected from the Thai/Lanna medicinal plant recipe database "MANOSROI III".

CONTEXT: Thai/Lanna medicinal plant recipes have been used for the treatment of several diseases including oral and cervical cancers. OBJECTIVE: To investigate anti-proliferative activity on human cervical (HeLa) and oral (KB) cancer cell lines of medicinal plants selected from Thai/Lanna medicinal plant recipe database "MANOSROI III". MATERIALS AND METHODS: Twenty-three methanolic plant crude extracts were tested for phytochemicals and anti-proliferative activity on HeLa and KB cell lines for 24 h by the sulforhodamine B (SRB) assay at the doses of 1 × 10(1)-1 × 10(-6 )mg/ml. The nine extracts with the concentrations giving 50% growth inhibition (GI50) lower than 100 µg/ml were further semi-purified by liquid/liquid partition in order to evaluate and enhance the anti-proliferative potency. RESULTS: All extracts contained steroids/triterpenoids, but not xanthones. The methanolic extracts of Gloriosa superba L. (Colchinaceae) root and Albizia chinensis (Osbeck) Merr. (Leguminosae-Mimosoideae) wood gave the highest anti-proliferative activity on HeLa and KB cell lines with the GI50 values of 0.91 (6.0- and 0.31-fold of cisplatin and doxorubicin) and 0.16 µg/ml (28.78- and 82.29-fold of cisplatin and doxorubicin), respectively. Hexane and methanol-water fractions of G. superba exhibited the highest anti-proliferative activity on HeLa and KB cell lines with the GI50 values of 0.15 (37- and 1.9-fold of cisplatin and doxorubicin) and 0.058 µg/ml (77.45- and 221.46-fold of cisplatin and doxorubicin), respectively. DISCUSSION AND CONCLUSION: This study has demonstrated the potential of plants selected from MANOSROI III database especially G. superba and A. chinensis for further development as anti-oral and cervical cancer agents.