Abstract: Biotransformation of an aromatase inhibitor, testolactone (1), yielded four metabolites, 7?-hydroxy-3-oxo-13,17-seco-5?-androsta-1-eno-17,13?-lactone (2), 3?,11?-dihydroxy-13,17-seco-5?-androsta-17,13?-lactone (3), 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (4), and 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (5). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+(estrogen-positive) breast-cancers. Metabolites 2 (IC50=8.63±0.402 nM), and 3 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 ?M), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 ?M). Derivatives 4 (IC50=10.37±0.50 ?M) and 5 (IC50=0.82±0.059 ?M) also showed a good inhibition against aromatase enzyme.

Abstract: Biotransformation of gestonorone acetate (1) with Cunninghamella blakesleeana (ATCC 8688) yielded a new analogue, 17?-actoxy-10?,11?-dihydroxy-progesterone (2). Compound 2 was identified as non-cytotoxic inhibitor of human aromatase enzyme (IC50=0.827±0.066 ?M). Compound 2 showed a significant aromatase inhibitory activity, as compared to the standard aromatase inhibitory drug, exemestane (IC50=0.232±0.03 ?M).

Abstract: Chronic wounds are medical care concern and severe clinical challenge worldwide. A nanofiber based new wound dressing scaffold and a method of developing thereof for treating diabetic wounds is described here. More specifically, the present invention relates to the preparation of biocompatible Polyacrylonitrile (PAN) nanofiber scaffold comprising of Quercetin, Zinc oxide and polyacrylonitrile by electrospinning. The nanofibers formed has the average diameter of approximately 160 nm and show excellent antibacterial and wound healing potentials.

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

Abstract: Biotransformation of medroxyprogesterone acetate (MPA) (1) with Cunninghamella blakesleeana (ATCC 8688) yielded five new analogues, i.e. 17?-acetoxy-6?-methylpregn-4-ene-3,11,20-trione (2), 17?-acetoxy-15?-hydroxy-6?-methylpregn-4-ene-3,11,20-trione (3), 17?-acetoxy-6?-hydroxy-6?-methylpregn-4-ene-3,11,20-trione (4), 17?-acetoxy-11?,15?-dihydroxy-6?-methylpregn-4-ene-3,20-dione (5), and 17?-acetoxy-6?,11?-dihydroxy-6?-methylpregn-4-ene-3,20-dione (6). In T-cell proliferation assay, metabolites 2, and 5 were found to be potent inhibitors with IC50<0.5 ?M, metabolite 6 showed a significant activity with IC50=8.64±0.02 ?M, while metabolites 3 and 4 were found to be moderately active with IC50=41.59±8.14, and 40.14±0.12 ?M, as compared to substrate 1 (IC50=6.48±5.18 ?M) and standard prednisolone (IC50=9.75±0.03 ?M) in in vitro assay. To establish the binding mode of medroxyprogesterone acetate (MPA) and the bio-transformed derivatives, molecular docking simulations were carried out using Vina.

Abstract: The present invention identifies new steroidal analogues of formestane synthesized through biotransformation with significant aromatase inhibitory activity, and thus can serve as possible safe, effective, and selective anti-cancer agent towards estrogen-responsive (ER+) breast cancer. Four new derivatives of anticancer drug formestane (1), 4?,5?,7?-trihydroxyandrostane-3,17-dione (2), 3?,7?-dihydroxyandrostane-4,17-dione (3), 3?,5?,7?-trihydroxyandrostane-4,17-dione (4), and 4,11?-dihydroxyandrosta-1,4-diene-3,17-dione (5) were synthesized through bio-catalyzed structural modifications by Cunninghamella. blakesleeana and Fusarium lini. The new derivatives showed varying degree of inhibition of aromatase enzyme. Metabolite 4 (IC50=0.386±0.072 ?M), showed a significant inhibitory potential, comparable to substrate 1 (IC50=0.335±0.011 ?M) and standard aromatase inhibitory anti-cancer drug exemestane (IC50=0.232±0.031 ?M). Metabolites 3 (IC50=1.37±0.029 ?M), and 2 (IC50=5.229±0.

Abstract: The present disclosure is related to a fertilizer (inorganic/organic/natural/synthetic) enriched with acclimatized (preferably halotolerant) effective microorganisms (AEM) and optionally with an organic emulsion (OE). The present disclosure provides a bioaugmented fertilizer enriched with AEM and optionally OE. Provide product (fertilizer) specific AEM, and method for producing such fertilizers. Fertilizer enriched with AEM, OMP, and OE renders it an Integrated Plant Nutrient Management (IPNM) principles based product (fertilizer). This makes it superior in performance over conventional fertilizers (inorganic/organic/natural/synthetic) due to better nutrient use efficiency.

Abstract: Four new analogues, 17?-hydroxy-7?,17?-dimethylestr-4,6-diene-3-one (2), 11?,17?-dihydroxy-7?, 17?-dimethyl-estra-1,3,5-triene-3-one (3), 3?,10?,17?-trihydroxy-7?,17?-dimethyl-5?-estrane (4), and 17?-hydroxy-7?,17?-dimethyl-5?-estrane-3,6-dione (5) of anabolic drug mibolerone (1) were synthesized. Derivatives 2 (IC50=3.83 ±0.3 ?M) and 3 (IC50=4.24 ±0.2 ?M) were identified as potent anti-inflammatory agents against T-cell proliferation. Derivative 4 (IC50=28.5 ±0.07 ?M) showed a potent anti-inflammatory activity against TNF-? production. In addition, compounds 1 (IC50=46.0 ±2.4 ?M), 2 (IC50=54.4 ±0.3 ?M), 3 (IC50=49.1 ±0.4 ?M), 4 (IC50=58.0 ±0.1 ?M) and 5 (IC50=52.7 ±0.3 ?M) showed a remarkable anti-inflammatory activity against NO? production. Metabolite 4 (IC50=0.072 ±0.001 ?M) showed a potent inhibitory activity against human placental aromatase. Compound 1 (IC50=24.19 ±2.1 ?g/mL) was found to be cytotoxic against BJ normal cell line, while metabolites 2-5 were identified as non-cytotoxic.

Abstract: Due to the SARS-CoV-2 pandemic, the development and screening of novel antiviral agents are urgently required. Herein, we developed herbal extracts with promising antiviral activity against SARS-CoV-2. Antiviral effects of Mentha piperita, and Flos chrysanthemi extracts alone, in combination and their fractions were found to decrease viral load. To determine which step of the virus is inhibited by the treatment, the extracts were administered at different time points of treatment, namely prophylactic (Full-time), pre-adsorption (Entry), and post adsorption (Post-entry). Most of the fractions, exhibited high efficacy upon prophylactic administration. The viral load was lower in prophylactic-treated cells than in non-treated cells. Administration of combinations, following 2:1 molar ratio of Mentha piperita, and Flos chrysanthemi significantly reduced the viral load by increasing the Cq values.

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

Abstract: A dietary herbal health supplement to reduce the symptoms of Parkinson's disease in a human subject comprising orally administering to a subject in need thereof an effective amount of the supplement comprising Mucuna puriens L. (velvet beans), Camellia sinensis L. (green tea), Allium sativum L. (ginger), Juglan regia L. (walnut), Arachis hypogaea L. (peanut), Vitis vinifera L. (red grapes), and Eugenia caryophyllata Thunb. (clove). The supplement is safe with only natural ingredients.

Abstract: New analogues of anti-cancer drugs atamestane (1), drostanolone enanthate ((3), and exemestane (6) were synthesized through biotransformation. New derivatives, 14?-hydroxy-1-methylandrosta-1,4-diene-3,17-dione ((2) (IC50, 9.7±0.72 nM) of 1 (IC50, 13.8±0.2 nM), and 2-methylandrosta-12?,17?-dihydroxy-1,4-diene-3-one (4) (IC50, 4.23±0.133 nM) of 3 (IC50, 6.4±0.06 nM) showed a potent inhibition against human aromatase enzyme and thus have the potential to treat ER+ breast-cancers and other related diseases. New metabolites, 2?-methyl-9?,17?-dihydroxy-5?-androstan-3-one ((5) (IC50=793.0±29.9 nM) of 3, 6-methylene-3?,7?,17?-trihydroxy-5?-androstane (7) (IC50, 46.1±0.81 nM), and 11?,17?-dihydroxy-6-methylene-androsta-1,4-diene-3-one (8) (IC5O=12797.0±844 nM) of exemestane (6) (IC50=232.0±31 nM) also showed a remarkable anti-aromatase activity. Aromatase is an enzyme, involves in the synthesis of estrogen (ER).

Abstract: Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7?-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13?-lactone (2), 7?-hydroxy-3-oxo-13,17-seco-5?-androsta-1-eno-17,13?-lactone (3), 3?,11?-dihydroxy-13,17-seco-5?-androsta-17,13?-lactone (4), 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (5), and 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (6). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+ (estrogen-positive) breast-cancers and several other diseases caused by overexpression of aromatase enzyme. Metabolites 3 (IC50=8.60±0.402 nM), and 4 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 ?M), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 ?M). Derivatives 2 (IC50=11.68±0.

Abstract: This invention provides an effective method and a composition for treating neurodegenerative diseases and conditions of the central and peripheral nervous system by stimulating neurogenesis by the use isoxylitones or an isomer, acid analog, a salt or a solvate, thereof.

Abstract: This invention demonstrates that silver nanoparticles can be synthesized by reducing silver nitrate with sodium borohydride in a presence of surface stabilizer polystyrene-block-poly(2-vinyl pyridine) in order to overcome the aggregation of silver nanoparticles.

Abstract: A food supplement to reduce symptoms of Parkinson's disease is disclosed. The food supplements contains a mixture of garlic, almond, peanut, tomato, grape, clove, black eye pea turmeric, tea and velvet bean.

Abstract: Techniques for providing email reactions via embedded tokens are disclosed. One example technique includes outputting an original email with an emoji interface that allows selection of emojis at a first computing device. Then, upon detecting selection of one of the emojis, the first computing device can automatically generate a reply email without manual composition. The reply email has data of an email reaction token and the selected one of the multiple emojis. Upon receiving the reply email, a second computing device can determine whether the reply email includes any email reaction token. In response to determining that the received reply email includes the email reaction token, the second computing device can render and surface the one of the multiple emojis on the original email without appending the reply email to an email thread corresponding to the original email.

Abstract: A food supplement to reduce symptoms of Parkinson's disease is disclosed. The food supplements contains a mixture of garlic, almond, peanut, tomato, grape, clove, black eye pea turmeric, tea and velvet bean.

Abstract: A method for treating the onset of obesity, reducing dyslipidemia and improving insulin sensitivity in mammals comprising administering a therapeutically effective amount of dried alcoholic extract of Cordia latifolia orally at a dose of 300 mg/kg of body weight to mammals in need for the reducing body weight and managing diabetic conditions.

Abstract: This invention provides new anticancer analogs of antimicrobial peptide temporin-SHa. New analogs (SEQ ID NOs: 2-6) of temporin SHa and, two different conjugates (7 & 8) comprising of monomeric and dimeric form of SEQ ID NO 4 with cancer targeting ligand were identified as anticancer peptides.