Current developments in the nanomediated delivery of photoprotective phytochemicals.

Natural products have been used to protect the skin from harmful UV radiation for decades. Due to the ecotoxicological implications of synthetic sunscreen exposure in aquatic ecosystems, there is a greater need to explore alternative sources of UV filters. Recent research has focused on discovering novel UV absorbing photoprotective molecules from nature. In response to the excessive damage caused by UVB rays, plants induce the production of high concentrations of phytoprotective secondary metabolites and anti-oxidative enzymes. Despite promising UV absorbing and photoprotective properties, plant secondary metabolites have been underutilized in topical delivery due to low solubility and high instability. Numerous phytochemicals have been effectively nanosized, incorporated in formulations, and studied for their sustained effects in photoprotection. The present review outlines recent developments in nanosizing and delivering photoprotective crude plant extract and phytochemicals from a phytochemical perspective. We searched for articles using keywords: "UV damage," "skin photoprotection," "photodamage," and "nano delivery" in varied combinations. We identified and reviewed literature from 43 original research articles exploring nanosized phytochemicals and crude plant extracts with photoprotective activity. Nanosized phytochemicals retained higher amounts of bioactive compounds in the skin and acted as depots for their sustained release. Novel approaches in nanosizing considerably improved the photostability, efficacy, and water resistance of plant secondary metabolites. We further discuss the need for broad-spectrum sunscreen products, potential challenges, and future growth in this area.

Pinocembrin-Enriched Fractions of Elytranthe parasitica (L.) Danser Modulates Apoptotic and MAPK Cellular Signaling in HepG2 Cells.

BACKGROUND: Hepatocellular carcinoma (HCC) is the fifth leading cause of cáncer mortality. Elytranthe parasitica (L.) Danser (EP), a hemiparasitic plant (Loranthaceae) has potent anti-cancer properties. OBJECTIVE: In the study, we investigated the effect of EP fractions on the expression of apoptosis and mitogenactivated protein kinase (MAPK) markers deregulated in HCC. Bioactivity fractionation was performed to isolate the phytochemical(s) exerting anti-tumor activity in HepG2 cells. METHOD: Anti-proliferative, clonogenic and anti-metastatic effects of EP fractions were examined in hepatocellular carcinoma cell line, HepG2 by Sulphorhodamine B, colony formation and scratch wound assays respectively in hepatocellular cell line, HepG2. The effects of EP fractions on key markers of apoptosis and MAPK signaling pathways were explored. KEY FINDINGS: EP bioactive fractions showed significant anti-tumor potential, reduced clonogenicity and considerably inhibited cell migration in HepG2 cells in vitro. The fractions augmented annexin V binding and induced apoptosis by causing cell cycle arrest at G2/M and S phase checkpoints. The fractions increased expression levels of p53, bad, cleaved PARP (Poly ADP ribose polymerase) and cleaved Caspase-3. Expression levels of phosphorylated ERK1/2 (Extracellular signal-regulated kinase) were downregulated. Pinocembrin-7-O-ß-D-glucoside and chrysin were isolated and characterized for the first time from Elytranthe parasitica (L.) Danser. CONCLUSION: Our findings reveal that EP fractions induced cell cycle arrest and triggered apoptosis in HepG2 cells by upregulating apoptosis and deactivating MAPK pathway. It signifies that pinocembrin glycoside and chrysin are bioactive phytochemicals contributing to the potent anti-hepatocarcinoma effects on HepG2 cells. Hence, bioactive EP fractions could be used as a therapeutic agent for effective HCC therapy.

Pinocembrin enriched fraction of Elytranthe parasitica (L.) Danser induces apoptosis in HCT 116 colorectal cancer cells.

BACKGROUND: Colorectal cancer (CRC) is a highly predominant malignancy affecting millions worldwide. Plants belonging to Loranthaceae family have remarkable chemopreventive properties. OBJECTIVE: The goal of the present study was to assess the antiproliferative and apoptosis-inducing effects of stem parts of Elytranthe parasitica (L.) Danser (EP) on colorectal cancer and identify the bioactive phytochemicals. MATERIAL AND METHODS: EP methanol extract (EP.M) and its subsequent fractions were screened for antiproliferative activity in human colorectal carcinoma HCT 116 cell line. Phytocomposition of the bioactive fraction was analyzed by GC-MS. Further, apoptotic induction and cell cycle arrest was assessed in the most bioactive fractions. RESULTS: EP.DEE (Diethyl Ether) fraction and a subsequent fraction derived by column chromatography, Fraction 3A (FR 3A) significantly inhibited the proliferation of HCT 116 cells (P < 0.05). FR 3A triggered apoptosis and notably modulated the cell cycle checkpoints. GC-MS analysis of FR 3A revealed the presence of 24 phytochemicals, the most prominent of which was pinocembrin (70.67%), a flavonoid. CONCLUSION: Hence, it could be speculated that pinocembrin and its related derivatives may be the chief phytochemicals involved in apoptosis - mediated cytotoxicity of the enriched fraction. Our findings indicate the enriched fraction is a promising candidate which could be developed into a natural chemotherapeutic product for colorectal cancer therapy.

Pro-apoptotic and cytotoxic effects of enriched fraction of Elytranthe parasitica (L.) Danser against HepG2 Hepatocellular carcinoma.

BACKGROUND: Hepatocellular carcinoma (HCC), the most common type of liver cancer accounts for more than one million deaths worldwide. Current treatment modality for HCC is marginally effective. Plants belonging to Mistletoe family (Loranthaceae) have been used in chemotherapy for many years. The present study was aimed at exploring the anti-proliferative, pro-oxidant and pro-apoptotic potential of stem of Elytranthe parasitica (L.) Danser (EP), a parasitic shrub belonging to Loranthaceae. METHODS: Elytranthe parasitica (L.) Danser, a climbing parasitic shrub was investigated for its cytotoxic activity against HepG2, a hepatocellular carcinoma cell line by Sulforhodamine B (SRB) assay. Further, pro-oxidant activity of EP extract/fractions was studied using copper phenanthroline assay. To understand the mechanism of cell death, the pro-apoptotic effects of Hep-G2 cells treated with EP extract/fractions were visualized by dual staining using acridine orange and ethidium bromide, a morphological marker of apoptosis. Phytochemical profiling of EP was explored by estimating the phenol, flavonoid and tannin content in its various fractions and extract. The occurrence of gallic acid, a principal polyphenol in EP extract and fractions was detected and further quantified using HPTLC (High Performance Thin Layer Chromatography) fingerprinting. RESULT: Active fraction of Elytranthe parasitica, EP.DEE exhibited potent cytotoxic activity in a dose dependent manner against HepG2 hepatocellular carcinoma cell line with an IC50 of 56.7 ± 7.8 µg/mL. Dual staining with acridine orange and ethidium bromide revealed that HepG2 cells treated with EP active fractions underwent cell death chiefly by apoptosis. Highest phenol, flavonoid and tannin content were observed in active fractions, EP.EA (Ethyl acetate fraction) and EP.DEE (Diethyl ether fraction). Gallic acid was identified and quantified in EP extract and active fractions, EP.DEE and EP.EA. CONCLUSION: Our findings indicate EP active fraction could be a promising contender in the treatment of hepatocellular carcinoma.

Cytotoxic activity of Macrosolen parasiticus (L.) Danser on the growth of breast cancer cell line (MCF-7).

BACKGROUND: Macrosolen parasiticus (L.) Danser belonging to Loranthaceaea (mistletoe family) is a parasitic plant that grows on different host plants such as mango, jack fruit, peepal, neem tree, etc., This study was aimed to investigate the anti-cancer activity of methanolic and aqueous extract of stem of M. parasiticus. OBJECTIVES: To investigate the in vitro cytotoxic potential of the methanolic and aqueous extracts from stems of M. parasiticus against MCF-7 breast cancer cells by brine shrimp lethality (BSL) bioassay, MTT assay and sulforhodamine B (SRB) assay. MATERIALS AND METHODS: The extracts were tested in human breast cancer cell lines in vitro for percentage cytotoxicity, apoptosis by acridine orange/ethidium bromide staining, LD50 and IC50 values after treatment with M. parasiticus extracts. RESULTS: In BSL bioassay, aqueous extract showed more significant (P < 0.01) cytotoxicity with LD50 82.79 ± 2.67 µg/mL as compared to methanolic extract with LD50 125 ± 3.04 µg/mL. The methanolic extract of M. parasiticus showed IC50 97.33 ± 3.75 µg/mL (MTT) (P < 0.05) and 94.58 ± 3.84 µg/mL (SRB) (P < 0.01) assays against MCF-7. The aqueous extract of M. parasiticus demonstrated higher activity with IC50 59.33 ± 3.3 µg/mL (MTT) (P < 0.01) and 51.9 ± 1.87 µg/mL (SRB)(P < 0.01) assays, after 48 h of exposure and thus showed significant dose-dependent cytotoxic activity. CONCLUSION: The finding demonstrated that both extracts of M. parasiticus showed significant cytotoxic activity, however aqueous extract demonstrated higher activity against MCF-7 breast cancer cells.

Nephroprotective potential of Graptophyllum pictum against renal injury induced by gentamicin.

OBJECTIVES: To evaluate the effect of Graptophyllum pictum on lipid peroxidation and tissue antioxidant enzymes in liver and kidney of gentamicin induced nephrotoxic rats. MATERIALS AND METHODS: Animals were grouped into 6: Group 1 received gum acacia, Group 2 received G. pictum ethanol extract (300 mg/kg), Group 3 received gentamicin, Groups 4, 5, 6 received gentamicin along with G. pictum at 300, 150, 75 mg/kg, respectively. Nephroprotective activity was evaluated by measuring thiobarbituric acid-reactive substances (TBARS), biochemical markers Glutathione (GSH), Glutathione-S Transferase(GST), Superoxide dismutase (SOD), Catalase (CAT), serum urea and creatinine levels. RESULTS: Results obtained showed that gentamicin induced nephrotoxic rats exhibited lower activities of biochemical markers and raised levels of TBARS, serum creatinine and urea. Remarkably, after treatment with G. pictum extract, anomalous levels of biochemical markers, lipid peroxidation and serum creatinine were returned to normal. CONCLUSION: The results propose that G. pictum has nephroprotective effects, and can be a promising natural source against gentamicin induced nephrotoxicity.

Identity-based High-performance thin Layer Chromatography Fingerprinting Profile and Tumor Inhibitory Potential of Anisochilus carnosus (L.f.) wall Against Ehrlich Ascites Carcinoma.

CONTEXT: Anisochilus carnosus (L.f.) wall belonging to the family Lamiaceae is a plant that is widely used in folk medicine for treating eczema, cold, cough, and fever. OBJECTIVE: In the present study, we explored the anticancer potential of A. carnosus leaves against Ehrlich ascites carcinoma (EAC) and estimated the quantity of luteolin present in various extracts and fractions of A. carnosus by high-performance thin layer chromatography (HPTLC) fingerprinting. MATERIALS AND METHODS: Various factors such as tumor volume, tumor cell viability, tumor weight, prolongation of lifespan, and hematological parameters were assessed. RESULT: We observed a significant lowering in tumor volume, tumor weight, and cell viability in EAC-induced mice following intervention with A. carnosus extracts. Also, there was a considerable prolongation of host lifespan and restoration of hematological parameters to almost normal levels with A. carnosus treatment. HPTLC fingerprinting of various extracts and fractions of A. carnosus along with luteolin as the reference standard revealed the occurrence of luteolin in all tested extracts and fractions of A. carnosus with the highest concentration being reported in the ethanol fraction. CONCLUSION: A. carnosus exhibits potent anti-tumor potential which can most likely be attributed to the occurrence of different phytochemicals such as phytosterols, terpenoids, and flavonoids in the plant. Further studies to isolate compounds from A. carnosus and understand the mechanism of anti-tumor activity would be worthwhile. SUMMARY: EAC induced mice that received A. carnosus treatment exhibited significant reduction in tumor volume, tumor weight and tumor cell viability. Their life span was considerably prolonged. We detected luteolin in A. carnosus aqueous and ethanol extract using HPTLC. Hence, anticancer activity of A. carnosus can be partly attributed to the presence of luteolin.

Cytotoxic potential of Anisochilus carnosus (L.f.) wall and estimation of luteolin content by HPLC.

BACKGROUND: Anisochilus carnosus (L.f.) wall (Lamiaceae), an annual herb which grows at high altitude is used extensively in folk medicine for the treatment of ailments such as gastric ulcer and skin diseases. The aim of our study was to evaluate the anticancer activity of different extracts of the leaves of A.carnosus. An attempt was also made to estimate the luteolin content in different extracts of Anisochilus carnosus by HPLC (High Performance Liquid Chromatography). METHODS: In the current study, we explored the cytotoxic potential of petroleum ether, ethanolic and aqueous extracts of A.carnosus against breast adenocarcinoma cell line (BT-549), by in vitro MTT and SRB assay. We also detected the luteolin content in different extracts (ethanolic and aqueous) of A.carnosus by using HPLC as a tool of analysis. RESULTS: The results demonstrate that petroleum ether and ethanolic extract of A.carnosus showed potent cytotoxic effect against BT-549 with an IC50 of 22.5 µg/ml (petroleum ether extract) and 87.24 µg/ml (ethanolic extract), by SRB assay, and 18.35 µg/ml (petroleum ether extract) and 58.64 µg/ml (ethanolic extract), by MTT assay. The aqueous extracts showed less cytotoxic effect with an IC50 of 211.26 µg/ml (by SRB assay) and 238.91 µg/ml (by MTT assay). HPLC results of luteolin content in various extracts using luteolin as the marker compound indicated the ethanol extract to contain the highest concentration of luteolin (0.372% w/w). The aqueous extract contained lower concentration of luteolin (0.282% w/w). CONCLUSION: Our findings demonstrate that petroleum ether and ethanolic extract of A.carnosus shows promising anticancer activity and has the potential to be developed into a therapeutic option for the treatment of cancer.