In-silico characterization of phytochemicals identified from Vitex negundo (L) extract as potential therapy for Wnt-signaling proteins

Background Colorectal cancer is the third most diagnosed disease in the world population and current chemotherapy has been used for targeting the cell proliferation and metastasizing ability of tumor cells. Potent chemotherapeutic drugs for colorectal cancer are capecitabine, fluorouracil, irinotecan, etc. which have toxic effects in normal tissues and adverse effects in multiple organs leading to major obstacles in clinical use. The aim of the study is the use of plant-derived compounds that improve the effectiveness of chemotherapeutics with lower and alleviate toxic side effects and reduce the risk of tumor progression. Results The current study is performed using Vitex negundo leaf which has been demonstrated to have positive effects against colorectal cancer. The use of computational approaches will help improve the identification and screening of lead molecules using AutoDock 4.2 and AutoDock Vina. Using computational approaches will help to improve lead identification and screening. Herein, we have retrieved six phytochemicals from published literature and investigated their inhibitory effect with Wnt-associated signaling proteins. Authentication of phytocompounds and Wnt-associated signaling proteins was done using AutoDock.4.2. Conclusions The results are screened based on the number of hydrogen bonds, binding energy, and interacting amino acids. The Isoorientin, luteolin, and Chrysophanol get the highest binding energy with target receptors. The binding energy is calculated with all target receptors from the range of − 6.0 to − 8.9 kcal/mol. The In-silico drug likeliness properties are predicted to be the best interacting compounds based on Lipinski Rule of 5 and ADMET analysis. Hence, we propose that Isoorientin, luteolin, and Chrysophanol are the potential inhibitors of Wnt signaling inhibitors, and preclinical studies are needed to confirm the promising therapeutic ability of colorectal cancer.

Flavonoids containing Vitex negundo extract displayed calcium channels blocking property underlying its anti-diarrheal and anti-spasmodic activities

Diarrhea is a major health problem and despite of interventions, it remains a substantial cause of mortality and morbidity. In this study, a flavonoids-rich Vitex negundo extract was mechanistically evaluated for its effectiveness in diarrheal diseases. The Vitex negundo ethanolic extract was subjected to extraction for isolation of total flavonoids and qualitative phytochemical analysis. The acute toxicity of flavonoids-extract was done in mice to assess its safety and tolerability. The anti-diarrhoeal activity was determined using the castor oil induced diarrhea mouse model at doses of 10, 30 and 100 mg/kg in relation to loperamide (10 mg/kg, oral). The antispasmodic profile was determined by using cut pieces of rabbit’s jejunum in Tyrode’s solutions, employing acetylcholine (0.03μM) as a tissue stabilizer and verapamil, as a calcium channel blocker. The preliminary qualitative analysis of extract revealed different phytochemicals, in addition to flavonoids. The acute toxicity profile showed that the flavonoids-extract is safe and tolerable (LD50 = 1678 mg/kg). In the tissue experiments, the total flavonoids exhibited an EC50 of 1.52 mg/mL and showed maximum relaxation of spontaneous contractions at 5.0 mg/mL and against high-K + induced contractions at 3 mg/mL (EC50 = 0.43 mg/mL). The spasmolytic activity of total flavonoids was comparable to verapamil which suggests that the activity might be due to the blockade of calcium channels. The flavonoids extract (0.1, 0.3 and 1.0 mg/mL) produced an adequate right shift in the calcium concentration response curve as compared to the control (EC50 value = –2.67 mg/mL), which confirmed that the extract has calcium channel blocking activity.

Development and Evaluation of Herbal Mosquito Repellent Cream

Mosquito repellent is a product that is applied to the skin or other surfaces to deter insects (and arthropods in general) from landing or climbing on that surface. The interest in plant-based repellants has been revived seeing that the development of resistance, cross-resistance and possible toxicity hazards associated with synthetic insecticides and their rising cost. The present study aimed towards the development and evaluation of safe and efficient herbal mosquito repellent from leaf extracts of Azadirachta indica, Vitex negundo, and Ocimum gratissimum. Six different types of formulation (Type-1 to 6) were prepared using each plant extract and optimized ingredients. The mosquito repellent activity of the formulation was tested using the arm-in-cage method. One skin rubbed with a small quantity of formulation was exposed to 20 mosquitoes and the number of mosquitoes that aligned or biting the arm was recorded in each minute for five minutes. The most effective repellent activity of the Type2 formulation was 87.5% (Y-shaped Model) and 91.62% (Rectangular-shaped Model). The Type1, Type3, Type4, Type5 and Type6 formulation showed 66.62% , 58.25%, 68.75%, 70.75% and 62.5% repellent activity in Y shaped model and 66.62%, 62.5%, 70.75%, 83.25% and 62.5% repellent activity in Rectangular shaped model respectively. During these studies, we found that Hexane extract showed higher repellent activity. No allergic reactions were observed upon the skin. So, it is a safe product. The formulation was ecological, economical and highly efficient.

Comparitive Study of Formulated Herbal Mosquito Repellent Incense Sticks with Market Product

The mosquito repellent formulations that are available on the market are causing irritations like coughing, sneezing, allergic reactions and respiratory disorders to human.The mosquito repellents available in the market are in various forms like colis,mats,sprays and fast cards. So the present study was carried out to formulate mosquito repellent incense sticks using herbals like Vitex negundo, Neem, Holy basil, and Garlic. The poly herbal mosquito repellent formulation are made by hand rolling method.The solid formulation containing binders and additives are rolled in the form of incense sticks and dried for 24 hrs. After drying its evaluated and compared with the market formulation. The prepared herbal mosquito incense sticks are potent, safe with more duration of time and less cost.

The Potency of Six Medicinal Plant Extracts Against the Stored Grain Insect Pest Sitophilus granarius L.

Jawalkar, N.B., S.P. Zambare and M.I. Al Ghannoum. 2021. The Potency of Six Medicinal Plant Extracts Against the Stored Grain Insect Pest Sitophilus granarius L. Arab Journal of Plant Protection, 39(4): 323-328. https://doi.org/10.22268/AJPP-039.4.323328 This study was conducted on six medicinal plants viz., Vitex negundo (leaves), Xanthium strumarium, Caesalpinia bonduc, Mucuna pruriens, Moringa oleifera (seed kernels), Tagetes erecta (petals) for their bio-insecticidal activity. The powders of various parts of plants were extracted using the MARS6 microwave acid digestion system. Three different concentrations (20, 30, and 40%) of plant extracts were tested against granary weevil, Sitophilus granarius L. (Coleoptera: Curculionidae) for their bio-insecticidal activities under laboratory conditions. The results of statistical analysis showed a good performance of all plant extracts, especially at the high concentrations of the extracts, where they showed different levels of insect mortality and their developmental rate was also reduced leading to significant reduction in insect numbers. The mortality rate ranged was 0-100% with S. granarius adults (p < 0.01). There was significant correlation (R=1) between mortality rate and the concentration of plant extracts. However, the extract of Mucuna pruriens with solvents (Acetone + Petroleum Ether) showed the highest mortality rate of 100% at the three concentrations used (p < 0.01), whereas, the lowest average mortality of 43.3% (p < 0.01) was observed with Xanthium strumarium and Vitex negundo extracts with solvents (Methanol + n-Hexane) compared with 0% mortality in the control. All plant extracts have revealed insecticidal as well as propitious protective effect on grains, and it can be selected as effective control treatment after proper dose formulation to prevent weevil infestation in stored grains. Keywords: Bioinsecticide, stored grains, Sitophilus granarius, mortality, medicinal plants, MARS 6.