Ginger and its active compounds in cancer therapy: From folk uses to nano-therapeutic applications.

Ginger is a spice that is renowned for its characteristic aromatic fragrance and pungent taste, with documented healing properties. Field studies conducted in several Asian and African countries revealed that ginger is used traditionally in the management of cancer. The scientific community has probed into the biological validation of its extracts and isolated compounds including the gingerols, shogaols, zingiberene, and zingerone, through in-vitro and in-vivo studies. Nonetheless, an updated compilation of these data together with a deep mechanistic approach is yet to be provided. Accordingly, this review highlights the mechanisms and therapeutics of ginger and its bioactive compounds focused on a cancer context and these evidence are based on the (i) cytotoxic effect against cancer cell lines, (ii) enzyme inhibitory action, (iii) combination therapy with chemotherapeutic and phenolic compounds, (iv) possible links to the microbiome and (v) the use of nano-formulations of ginger bioactive compounds as a more effective drug delivery strategy in cancer therapy.

Herbal Medicine of the 21st Century: A Focus on the Chemistry, Pharmacokinetics and Toxicity of Five Widely Advocated Phytotherapies.

Widely advocated for their health benefits worldwide, herbal medicines (HMs) have evolved into a billion dollar generating industry. Much is known regarding their wellness inducing properties, prophylactic and therapeutic benefits for the relief of both minor to chronic ailment conditions given their long-standing use among various cultures worldwide. On the other hand, their equally meaningful chemistry, pharmacokinetic profile in humans, interaction and toxicity profile have been poorly researched and documented. Consequently, this review is an attempt to highlight the health benefits, pharmacokinetics, interaction, and toxicity profile of five globally famous HMs. A systematic literature search was conducted by browsing major scientific databases such as Bentham Science, SciFinder, ScienceDirect, PubMed, Google Scholar and EBSCO to include 196 articles. In general, ginsenosides, glycyrrhizin and curcumin demonstrate low bioavailability when orally administered. Ginkgo biloba L. induces both CYP3A4 and CYP2C9 and alters the AUC and Cmax of conventional medications including midazolam, tolbutamide, lopinavir and nifedipine. Ginsenosides Re stimulates CYP2C9, decreasing the anticoagulant activity of warfarin. Camellia sinensis (L.) Kuntze increases the bioavailability of buspirone and is rich in vitamin K thereby inhibiting the activity of anticoagulant agents. Glycyrrhiza glabra L. displaces serum bound cardiovascular drugs such as diltiazem, nifedipine and verapamil. Herbal medicine can directly affect hepatocytes leading to hepatoxicity based on both intrinsic and extrinsic factors. The potentiation of the activity of concurrently administered conventional agents is potentially lethal especially if the drugs bear dangerous side effects and have a low therapeutic window.

Effect of exogenous ATP on Momordica charantia Linn. (Cucurbitaceae) induced inhibition of D-glucose, L-tyrosine and fluid transport across rat everted intestinal sacs in vitro.

Momordica charantia (MC) is a common oriental vegetable with known antidiabetic, laxative and antimicrobial properties. This study investigates the effects of aqueous fruit extract of MC on the transport of d-glucose, l-tyrosine and fluid across rat-everted intestine in vitro. Everted intestinal sacs from rats were mounted in an organ bath containing Krebs-Henseleit bicarbonate buffer. Graded concentrations (1.5-12mg/ml) of MC fruit extract were incubated in the mucosal solution with and without exogenous ATP in the mucosal bathing fluid. The serosal appearance and mucosal disappearance of d-glucose, l-tyrosine and the fluid absorptive capacity of the intestine were significantly inhibited (p<0.05) with increasing graded concentrations of MC. The concentration of d-glucose accumulated or metabolized by the enterocytes in the intestinal tissues were significantly higher (p<0.05) when incubated with MC. Increasing graded concentrations of exogenous ATP (25-200 microM) were incubated with 3.0mg/ml MC to confirm inhibition of the ATP-dependent active transport of d-glucose, l-tyrosine and fluid across rat enterocytes. It was found that increasing concentrations of mucosal ATP from 25 to 100 microM significantly (p<0.05) reverses the MC-depression of the d-glucose, l-tyrosine and fluid uptake across rat everted intestinal sacs. It is hypothesized that bioactive phytochemicals such as saponins in MC fruit extract inhibits the active transport of d-glucose, l-tyrosine and fluid across rat intestine by inhibiting the production of ATP responsible for the active transport of these molecules. It is likely that MC can be a potential alternative drug therapy of postprandial hyperglycaemia via inhibition of glucose uptake across the small intestine.

Stimulatory effects of Antidesma madagascariense on D-glucose, L-tyrosine, fluid and electrolyte transport across rat everted intestine, comparable to insulin action in vitro.

Medicinal plants are believed to be an important source of potential therapeutic agents. This study investigates the effects of Antidesma madagascariense (AM) extract on the transport of D-glucose, L-tyrosine, fluid and electrolytes (Na+ and K+) across rat everted intestinal sacs. These sacs were mounted in an organ bath containing Krebs-Henseleit bicarbonate (KHB) buffer. Experimental findings showed that incubation with graded aqueous AM extracts above 0.375 mg/mL significantly (P < 0.05) stimulated the mucosal disappearance and serosal appearance of glucose and fluid. The concentration of glucose accumulated in the intestinal tissues also increased significantly (P < 0.05) compared to that found in the controls. Transport of the amino acid L-tyrosine was not significantly enhanced (P > 0.05) when incubated with increasing concentrations of AM extract. Effects on electrolyte (K+ and Na+) transport were assessed. Na+ uptake and transport was significantly enhanced (P < 0.05) when incubated with 0.75 mg/mL AM extract; however, K+ transport was not significantly enhanced (P > 0.05). For comparison, insulin (1 and 2 units/mL) was incubated in the mucosal solution. Aqueous AM extract produced similar stimulatory effects on the transport of glucose, fluid and Na+ as were found with insulin. It is hypothesised that bioactive phytochemicals such as flavonoids, alkaloids, leucoanthocyanins, phenols and saponins from AM leaf extract might interfere with the Na+/glucose carrier, thereby enhancing the transport of glucose, Na+ and fluid across rat everted intestinal sacs. Thus, AM may represent a possible alternative dietary supplement for the treatment of type 2 diabetes.

Antioxidant and anti-glycation activities correlates with phenolic composition of tropical medicinal herbs.

OBJECTIVE: To determine the contribution of total phenolic content (TPC) in glycation inhibitory activity of common tropical medicinal food and spices with potential antioxidative properties. METHODS: In vitro glucose-bovine serum albumin (BSA) assay was used. Ethanolic extracts of ten common household condiments/herbs (Allium sativum, Zingiber officinale, Thymus vulgaris, Petroselinum crispum, Murraya koenigii Spreng, Mentha piperita L., Curcuma longa L., Allium cepa L., Allium fistulosum and Coriandrum sativum L.) were evaluated for antioxidative activity by 2,2-diphenyl-2-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP) and the TPC, flavonoid and tannins content were determined. RESULTS: Findings showed good correlation between TPC/DPPH (r = 0.8), TPC/FRAP (r = 0.8), TPC/anti-glycation (r = 0.9), DPPH/anti-glycation (r = 0.6), FRAP/anti-glycation (r = 0.9), Flavonoid/anti-glycation (r = 0.7) and Tannins/anti-glycation (r = 0.8) and relatively fair correlation for TPC/Flavonoids (r = 0.5) and TPC/Tannins (r = 0.5). Results imply that these plants are potential sources of natural antioxidants which have free radical scavenging activity and might be used for reducing oxidative stress. CONCLUSIONS: The positive glycation inhibitory and antioxidative activities of these tropical herbs suggest a possible role in targeting ageing, diabetic complications and oxidative stress related diseases.

Screening for alternative antibiotics: an investigation into the antimicrobial activities of medicinal food plants of Mauritius.

The present study was designed to evaluate the antimicrobial activities of 2 endemic medicinal plants; Faujasiopsis flexuosa (Asteraceae) (FF) and Pittosporum senacia (Pittosporaceae) (PS) and 2 exotic medicinal plants, Momordica charantia (Cucurbitaceae) (MC) and Ocimum tenuiflorum (Lamiaceae) (OT) that forms part of local pharmacopoeia of Mauritius and correlate any observed activity with its phytochemical profile. Aqueous and organic fractions of the leaves, fruits, and seeds of these plants were subjected to antimicrobial testing by the disc diffusion method against 8 clinical isolates of bacteria and 2 strains of fungus. It was found that MC, OT, and FF possessed antimicrobial properties against the test organisms. The MIC for MC ranged from 0.5 to 9 mg/mL and that of FF from 2 to 10 mg/mL and the lowest MIC value (0.5 mg/mL) was recorded for the unripe fruits of MC against E. coli. On the other hand, higher concentration of the unripe MC fruit extract of 9 mg/mL was needed to be effective against a resistant strain of Staphylococcus aureus (MRSA). The antimicrobial effect against MRSA was lost upon ripening of the fruits. The methanolic extract of both MC and FF showed highest MIC values compared to the corresponding aqueous extract, which indicates the low efficacy and the need of higher doses of the plant extract. Phytochemical screening of the plants showed the presence of at least tannins, phenols, flavonoids, and alkaloids, which are known antimicrobial phyto-compounds. In conclusion, the observed antimicrobial properties would tend to further validate the medicinal properties of these commonly used endemic medicinal and food plants of Mauritius.

Screening of traditional antidiabetic medicinal plants of Mauritius for possible alpha-amylase inhibitory effects in vitro.

In this study, seven exotic/indigenous medicinal plants of Mauritius, namely Coix lacryma-jobi (Poaceae), Aegle marmelos (Rutaceae), Artocarpus heterophyllus (Moraceae), Vangueria madagascariensis (Rubiaceae), Azadirachta indica (Meliaceae), Eriobotrya japonica (Rosaceae) and Syzigium cumini (Myrtaceae) were studied for possible effects on starch breakdown by alpha-amylase in vitro. The results showed that only Artocarpus heterophyllus significantly (p < 0.05) inhibited alpha-amylase activity in vitro. To confirm the observed effects, a further biochemical assay was undertaken to investigate the effects of Artocarpus heterophyllus on alpha-amylase activity using rat plasma in vitro. It was found that the aqueous leaf extract significantly (p < 0.05) inhibited alpha-amylase activity in rat plasma. The highest inhibitory activity (27.20 +/- 5.00%) was observed at a concentration of 1000 microg/mL. However, in both cases dose dependency was not observed. Enzyme kinetic studies using the Michaelis-Menten and Lineweaver-Burk equations were performed to establish the type of inhibition involved. In the presence of the plant extract the maximal velocity (Vmax) remained constant (1/150 g / L/s) whereas the Michaelis-Menten constant (Km) increased by 5.79 g / L, indicating that the aqueous leaf extract of Artocarpus heterophyllus behaved as a competitive inhibitor. Results from the present study tend to indicate that Artocarpus heterophyllus could act as a 'starch blocker' thereby reducing post-prandial glucose peaks.