Combined Effect of Vaccinium nilgiriensis Bark Extract and 680nm Laser Irradiation in Inducing Breast Cancer Cell Death.

BACKGROUND: Cancer refers to a collection of diseases where cells begin to multiply uncontrollably. Breast cancer is the most predominant malignancy in women. Herbal medicine is one of the important health care systems in most developing countries. Many studies have shown that naturally occurring compounds may support the prevention and treatment of various diseases, including cancer. Some of the plant extracts and isolated compounds show photosensitizing activities and reduce cell proliferation whereas some have revealed photoprotective effects. OBJECTIVES: The biological properties and medicinal uses of extracts and bioactive compounds from V. nilgiriensis have not been investigated. This study aims to evaluate the cytotoxic effects of V. nilgiriensis in combination with 680nm laser irradiation on MCF-7 breast cancer cells. METHODS: The inverted microscopy, ATP and LDH assay were used to analyze the cellular morphology, proliferation, cytotoxicity respectively after the treatment with V. nilgiriensis bark extract. The diode laser of wavelength 680nm and 15 J/cm2 fluency has been used for laser irradiation. The activity of apoptotic proteins was studied using ELISA and nuclear damage by Hoechst staining. RESULTS: The exposure of V. nilgiriensis extracts with laser irradiation at 680nm increases the cytotoxicity and decreases the proliferation of MCF-7 cells. The results of the Hoechst stain indicated nuclear damage. Our study proved that V. nilgiriensis holds a strong cytotoxic effect on breast cancer cells alone and in combination with laser irradiation by upregulating the expression of apoptotic proteins such as caspase 3, p53 and Bax. CONCLUSION: The results from this study showed that the bark ethyl acetate of V. nilgiriensis and in combination with laser is effective in preventing breast cancer cell proliferation in vitro. Further work is warranted to isolate the bioactive compounds from V. nilgiriensis bark extract and study the effect of compounds in the cell death induction. Due to the cytotoxic properties, V. nilgiriensis can be considered as a potent therapeutic agent for the treatment of cancer.

Role of Photoactive Phytocompounds in Photodynamic Therapy of Cancer.

Cancer is one of the greatest life-threatening diseases conventionally treated using chemo- and radio-therapy. Photodynamic therapy (PDT) is a promising approach to eradicate different types of cancers. PDT requires the administration of photosensitisers (PSs) and photoactivation using a specific wavelength of light in the presence of molecular oxygen. This photoactivation exerts an anticancer effect via apoptosis, necrosis, and autophagy of cancer cells. Recently, various natural compounds that exhibit photosensitising potentials have been identified. Photoactive substances derived from medicinal plants have been found to be safe in comparison with synthetic compounds. Many articles have focused on PDT mechanisms and types of PSs, but limited attention has been paid to the phototoxic activities of phytocompounds. The reduced toxicity and side effects of natural compounds inspire the researchers to identify and use plant extracts or phytocompounds as a potent natural PS candidate for PDT. This review focusses on the importance of common photoactive groups (furanocoumarins, polyacetylenes, thiophenes, curcumins, alkaloids, and anthraquinones), their phototoxic effects, anticancer activity and use as a potent PS for an effective PDT outcome in the treatment of various cancers.

Sphenodesme involucrata var. paniculata (C.B. Clarke) Munir.: Chemical characterization, anti-nociceptive and anti-inflammatory activities of methanol extract of leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: Sphenodesme involucrata var. paniculata (C. B. Clarke) Munir is native as well as endemic to South India. Its leaves are used in folklore medicine to treat pain and rheumatism. OBJECTIVE: This study was aimed to investigate the chemical characterization, anti-nociceptive and mode of action underlying the anti-inflammatory effects of methanol extract of S. involucrata leaves (MESi). METHODS: Phytoconstituents of MESi was analyzed using colorimetric and liquid chromatography-mass spectrometry (LC-MS) methods, and the oral acute toxicity was evaluated in mice up to 2000 mg/kg. The anti-nociceptive effect was evaluated in hot plate and writhing tests; whereas the anti-inflammatory effect was investigated using carrageenan, cotton pellet and lipopolysaccharide (LPS)-induced peritonitis models at doses of 100, 200 and 400 mg/kg. Additionally nitric oxide (NO) and inflammatory cytokines levels were also evaluated. RESULTS: MESi exhibited the high content of phenolics and flavonoids as well as compounds like austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin were detected in LC-MS. In the acute toxicity study, oral administration of MESi did not cause any toxic effect and mortality up to 2000 mg/kg body weight in mice. In the anti-nociceptive tests, MESi augmented the latency period at higher dose (400 mg/kg), on the other hand attenuated writhings at the dose of 400 mg/kg by 87.87% (p < 0.001). In the carrageenan induced paw oedema MESi significantly inhibited the oedema formation at dose 400 mg/kg by 32.1%; besides, anti-inflammatory effect was registered in the cotton pellets-induced inflammation model at doses 200 and 400 mg/kg by 27.09% (p < 0.001) and 35.47% (p < 0.001) respectively. On the other hand, MESi appreciably reduced leukocyte, neutrophils infiltration, nitric oxide, TNF-α and IL-1ß levels and increased the IL-10 level in the (LPS)-induced peritonitis model. CONCLUSION: The results conclude that MESi has no acute toxic effect and it demonstrated potent anti-nociceptive and anti-inflammatory activities. Its anti-nociceptive activities are probably mediated through peripheral and central mechanisms. The anti-inflammatory effect of MESi involved the inhibition of neutrophils migration and the modulation of Th1 and Th2 cytokines, besides the attenuation of production of PGE2 and NO. LC-MS analysis revealed the predominant presence of the austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin compounds, which are possibly involved in the anti-nociceptive and anti-inflammatory effects of MESi. The current study provided supportive evidence for the folklore use of S. involucrata in the treatment of pain and inflammatory conditions.

Cytotoxic, analgesic and anti-inflammatory properties of Syzygium calophyllifolium bark.

The present study explores the effect of Syzygium calophyllifolium bark methanol (SCBM) extract on pain and inflammation as cancer associated symptoms. The anti-proliferative and cell death-inducing ability of the extract was analysed using MCF-7 breast cancer cells. ATP and LDH levels, along with the cell morphology were noted. The anti-proliferative ability of the extract was examined in relation to pain and inflammation. Analgesic activity was determined using a hot plate, acetic acid and formalin-induced pain models in mice. Acute anti-inflammatory activity was observed in carrageenan and egg albumin induced paw oedema in Wistar rats. Chronic inflammation was induced by placing a cotton pellet under the skin at the axial region of rats. Reduced ATP and increased LDH content indicated the cytotoxic effect of the extract. SCBM at 200 mg/kg dose depicted good activity in acetic acid (77.69%) and formalin (80.81%) induced pain models compared to the standard drug indomethacin. However, only a moderate activity was observed in the hot plate method (53.85%). The higher dose of SCBM was equally effective in anti-inflammatory models. The dose (200 mg/kg) significantly reduced the paw oedema in carrageenan (96.71%) and egg albumin models (54.24%) compared to the control. The chronic inflammation was also inhibited upto 70.46% by SCBM. These activities can be attributed to the phenolic compounds detected in HPLC. The outcome of the study states that the extract can reduce both acute and chronic inflammatory conditions and kill the cancer cells, proposing the dual role of SCBM in treating inflammatory pains in cancer. The result of these studies indicated that wild plants like Syzygium calophyllifolium could be taken forward for a detailed study to accomplish the demand for a better treatment against diseases.

Study of intestinal anti-inflammatory activity of Phoenix loureiroi Kunth (Arecaceae) fruit.

Phoenix loureiroi Kunth belongs to the family Arecaceae, the fruits are widely consumed by Kurumba and Irula tribes of Tamil Nadu (India) and also used to cure intestinal related diseases in folklore medicine. Therefore, in vivo animal studies were evaluated to confirm the prevention of inflammatory bowel disease (IBD) with the treatment of this plant fruits. The IBD was studied in Wistar albino rats by indomethacin (s.c.), acetic acid (i.c.) and dextran sulfate sodium (DSS) induced models. The diseases parameters such as macroscopic, microscopic features, serum biomarkers levels, haematological profile, biochemical and antioxidant levels were determined. The fruit extract (50, 100 and 200mg/kg) treated enterocolitis rats significantly retain their body weight, organ weight, stool consistency, macroscopic score, histology, haematological parameters, antioxidative enzyme levels and also reduce the serum marker levels and myeloperoxidase (MPO) activity compared to prednisolone (2mg/kg) and sulfasalazine (50mg/kg) drugs. In conclusion, regular consumption of P. loureiroi fruit may prevent IBD and strongly support the folklore use of fruit in the treatment of intestinal ailments.

Polyphenols rich Passiflora leschenaultii leaves modulating Farnesoid X Receptor and Pregnane X Receptor against paracetamol-induced hepatotoxicity in rats.

The hepatoprotective effect of P. leschenaultii. (DC) leaves was investigated in rats under paracetamol induced oxidative stress. Leaf acetone extract (200 and 400mg/kg) were administered daily via gavage for 14days before paracetamol (2000mg/kg, p.o.) treatment. After the experiment, the levels of serum biochemical parameters and enzymatic antioxidant levels were determined. Furthermore, liver tissues were analyzed histopathologically. Additionally, the molecular docking studies of the identified compounds against PXR and FXR proteins were also performed. The assessment revealed that the acetone extract significantly reduced the elevated levels of SGPT, SGOT and ALP in serum. Moreover, the enzymatic antioxidants such as SOD, CAT and LPO were also retained normally by the plant extract. From histopathological analysis, it was clearly evident that the cellular architecture of plant extract treated rat liver tissues were not affected by the paracetamol induction at the higher dose. The results of docking studies also revealed that the identified compounds showed steric interactions (between nonpolar atoms) with amino acid groups. Collectively, the present study suggests that P. leschenaultii leaves extract protects the liver from paracetamol induced hepatic damage.

Antitumor and Wound Healing Properties of Rubus ellipticus Smith.

The present investigation has been undertaken to study the antioxidant, antitumor, and wound healing properties of Rubus ellipticus. The R. ellipticus leaves were extracted using organic solvents in Soxhlet and were subjected to in vitro antioxidant assays. R. ellipticus leaf methanol (RELM) extract, which showed higher in vitro antioxidant activity, was taken for the evaluation of in vivo antioxidant, antitumor, and wound healing properties. Acute oral and dermal toxicity studies showed the safety of RELM up to a dose of 2 g/kg. A significant wound healing property was observed in incision, excision, and Staphylococcus aureus-induced infected wound models in the treatment groups compared to the control group. A complete epithelialization period was noticed during the 13(th) day and the 19(th) day. A 250-mg/kg treatment was found to prolong the life span of mice with Ehrlich ascite carcinoma (EAC; 46.76%) and to reduce the volume of Dalton's lymphoma ascite (DLA) solid tumors (2.56 cm(3)). The present study suggests that R. ellipticus is a valuable natural antioxidant and that it is immensely effective for treating skin diseases, wounds, and tumors.

Evaluation of nutritional composition and antioxidant properties of underutilized Ficus talboti King fruit for nutraceuticals and food supplements.

This study investigated change in the chemical components and antioxidant activity of Ficus talboti fruit for the development of functional foods. Proximate compositions of crude protein, ash and fat were 23.28, 10.47 and 3.86% respectively. Macro-nutrient contents were found to be higher in the fruit when compared to micronutrients. The analysis also showed the presence of almost all the essential and non-essential amino acids especially Leucine, Phenylalanine and tyrosine in higher amount. Linolenic acid content was higher than stearic acid among the fatty acids in the fruit. Total phenolic content (35.4 ± 0.32 g GAE /100 g) was found in higher amount in acetone extract. The IC50 values of 1,1-diphenyl-2-picrylhydrazyl, hydroxyl and superoxide radical scavenging of acetone extract were 346, 252 and 652 µg/mL respectively. Thus, F. talboti fruit can be used as a healthy and functional food ingredient which will ensure dietary diversity and food security among the marginalized and poor communities.

Antitumor and wound healing properties of Rubus niveus Thunb. root.

The main objective of this study is to highlight the importance of Rubus niveus in the pharmaceutical industry for the development of cost-effective drugs. The study was undertaken to explore the HPLC profile, wound healing, antitumor, and free radical scavenging properties of R. niveus. The root of R. niveus was extracted using organic solvents and subjected to in vitro antioxidant assays. Acetone extract, which showed better in vitro antioxidant properties, was evaluated for in vivo antioxidant, wound healing, and antitumor properties. The polyphenolic acetone extract showed significant in vivo antioxidant, wound healing, and antitumor properties. In the wound healing study, complete epithelialization was noticed during the 13th to 17th days for treated groups. The 250 mg/kg group was found to prolong the life span of mice with Ehrlich ascites carcinoma (70.04%) and reduced the volume of Daltons lymphoma ascites solid tumors (2.07 cm3). The HPLC analysis of acetone extract revealed the presence of Quercetin, a natural flavonoid with the retention time of 20.89 min. The results of the current study suggest the use of R. niveus as a valuable natural antioxidant that has an immense scope as an effective source to cure skin diseases, wounds, and tumors.

Nutritional composition and antioxidant properties of Cucumis dipsaceus Ehrenb. ex Spach leaf.

The leaf of C. dipsaceus was evaluated for its nutritional and antioxidant properties. From the present investigation, significant amount of almost all essential amino acids and important minerals were quantified. Low levels of trypsin inhibitory units, phenolics, and tannins content were found as antinutritional content. Further, hot water extract of C. dipsaceus showed good activity especially in ABTS(+), metal chelating, nitric oxide, and DPPH assays. Hence, the results conclude that C. dipsaceus could be a valuable nutraceutical supplement to the human diet.

Free radical scavenging property and antiproliferative activity of Rhodiola imbricata Edgew extracts in HT-29 human colon cancer cells.

OBJECTIVE: To investigate the in vitro antioxidant and antiproliferative activity of rhizome extracts of Rhodiola imbricata (R. imbricata) in HT-29 human colon cancer cell line. METHODS: The successively extracted rhizome of R. imbricata using various solvents was analyzed for their total phenolics, tannins and flavonoid contents. In vitro antioxidant activity was evaluated by employing different assays, including DPPH, ABTS radical scavenging assays, FRAP, phosphomolybdenum reduction assay, superoxide anion, hydroxyl radical scavenging activities and metal chelating ability. RESULTS: Acetone and methanol extracts recorded higher phenolic content and showed comparable antioxidant activity with standard reference. Additionally, they also inhibited the proliferation of HT-29 cells upon treatment at higher concentration (200 µg/mL) (acetone and methanol, 84% and 84%, respectively). On examination acetone extract exhibited antiproliferative activity in a concentration dependent manner whereas, methanol extract showed both dose dependent and time dependent inhibitory activity. CONCLUSIONS: The results obtained justify the traditional usage of R. imbricata from their promising antioxidant activity.