Chemical composition, cholinesterase, and α-glucosidase inhibitory activity of the essential oils of some Iranian native Salvia species.

BACKGROUND: The plants from Salvia genus contain widely distributed species which have been used in folk medicine as well as pharmaceutical and food industries. METHODS: The chemical composition of 12 native Iranian Salvia species (14 plants) was identified using gas chromatography-mass spectrometry (GC-MS). Also, the inhibitory activity of all essential oils (EOs) was evaluated toward α-glucosidase and two types of cholinesterase (ChE) using spectrophotometric methods. The in vitro α-glucosidase inhibition assay was performed by the determination of p-nitrophenol (pNP) obtained from the enzymatic dissociation of p-nitrophenol-α-D-glucopyranoside (pNPG) as the substrate. In vitro ChE inhibitory assay was conducted based on the modified Ellman's procedure using the measurement of 5-thio-2-nitrobenzoic acid produced from the hydrolysis of thiocholine derivatives as the substrate, in the presence of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). RESULTS: Totally, 139 compounds were detected and caryophyllene oxide and trans-ß-caryophyllene were the most abundant compounds in all EOs. The yield of EOs extracted from the plants were also calculated in the range of 0.06 to 0.96% w/w. Herein, α-glucosidase inhibitory activity of 8 EOs was reported for the first time and among all, S. spinosa L. was found to be the most potent inhibitor (90.5 inhibition at 500 µg/mL). Also, the ChE inhibitory activity of 8 species was reported for the first time and our results showed that the BChE inhibitory effect of all EOs was more potent than that of AChE. The ChE inhibition assay indicated that S. mirzayanii Rech.f. & Esfand. collected from Shiraz was the most potent inhibitor (72.68% and 40.6% at the concentration of 500 µg/mL, toward AChE and BChE, respectively). CONCLUSIONS: It seems that native Salvia species of Iran could be considered in the development of anti-diabetic and anti-Alzheimer's disease supplements.

Cedrus deodara: In Vivo Investigation of Burn Wound Healing Properties.

Objective: Cedrus deodara (Roxb. Ex Lamb.) G. Don possesses various biological activities, which have been documented in modern and traditional medicine. In this study, burn wound healing activity of the methanol extract of C. deodara wood was evaluated via a burn wound model in Wistar rats. Methods: The methanol extract of C. deodara was evaluated for the contents of phenolic compounds, flavonoids, and tannins. Also, its antioxidant activity was determined using the DPPH assay. Then, a topical ointment containing the methanol extract of C. deodara (10%) was used to evaluate the healing effects on a model of second-degree thermal burn in 4 groups of 7 rats within 21 days. In this respect, average wound surface area, wound closure, and various histological features were examined. Results: Our findings revealed that the wounds treated with the methanol extract of C. deodara showed higher wound contraction (33.6, 87.1, and 93.4% on days 7, 14, and 21, respectively) compared with the positive control (27.6, 80.7, and 88.3% on days 7, 14, and 21, respectively) and the negative control (20.1, 77.9, and 80.2% on days 7, 14, and 21, respectively). According to the results from epitheliogenesis score, the number of inflammatory cells, neovascularization, and collagen density, good burn wound healing activity of the methanol extract of C. deodarawas demonstrated. Conclusion: Using the methanol extract of C. deodara in an ointment formulation can be developed to prevent or reduce burn injury progression.

Phytochemical investigation and biological activity of Doronicum pardalianches L. roots against Alzheimer's disease.

The methanol extract of Doronicum pardalianches L. was fractionated using n-hexane, chloroform, and ethyl acetate to evaluate their cholinesterase (ChE) inhibitory activity via modified Ellman's method. It was perceived that only the ethyl acetate fraction was active toward acetylcholinesterase (AChE) with IC50 value of 172.21 µg/mL. Also, all fractions showed no butyrylcholinesterase (BChE) inhibitory activity. The ethyl acetate fraction was also investigated for its neuroprotectivity and metal chelating ability (Zn2+, Fe2+, and Cu2+) which demonstrated desired activity. Phytochemical analysis of the ethyl acetate fraction led to isolation and identification of formononetin 7-O-ß-D-glucopyranoside which has not been previously reported for this plant.

Cinnamomum verum J. Presl. Bark essential oil: in vitro investigation of anti-cholinesterase, anti-BACE1, and neuroprotective activity.

BACKGROUND: Cinnamomum verum J. Presl. (Lauraceae), Myrtus communis L. (Myrtaceae), Ruta graveolens L. (Rutaaceae), Anethum graveolens L. (Apiaceae), Myristica fragrans Houtt. (Myristicaceae), and Crocus sativus L. (Iridaceae) have been recommended for improvement of memory via inhalation, in Iranian Traditional Medicine (ITM). In this respect, the essential oils (EOs) from those plants were obtained and evaluated for cholinesterase (ChE) inhibitory activity as ChE inhibitors are the available drugs in the treatment of Alzheimer's disease (AD). METHODS: EOs obtained from the plants under investigation, were evaluated for their potential to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro based on the modified Ellman's method. The most potent EO was candidate for the investigation of its beta-secretase 1 (BACE1) inhibitory activity and neuroprotectivity. RESULTS: Among all EOs, C. verum demonstrated the most potent activity toward AChE and BChE with IC50 values of 453.7 and 184.7 µg/mL, respectively. It also showed 62.64% and 41.79% inhibition against BACE1 at the concentration of 500 and 100 mg/mL, respectively. However, it depicted no neuroprotective potential against ß-amyloid (Aß)-induced neurotoxicity in PC12 cells. Also, identification of chemical composition of C. verum EO was achieved via gas chromatography-mass spectrometry (GC-MS) analysis and the major constituent; (E)-cinnamaldehyde, was detected as 68.23%. CONCLUSION: Potent BChE inhibitory activity of C. verum EO can be considered in the development of cinnamon based dietary supplements for the management of patients with advanced AD.

Phytochemical investigation and anticholinesterase activity of ethyl acetate fraction of Myristica fragrans Houtt. seeds.

In this work, n-hexane, chloroform, and ethyl acetate fractions of the methanol extract of Myristica fragrans Houtt. seeds were evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) via Ellman's method. It was found that all fractions depicted no anti-AChE activity, however, they were active toward BChE with IC50 values of 361.8, 215.0, and 145.8 µg/mL, respectively comparing with donepezil as the reference drug (IC50 = 1.97 µg/mL). The ethyl acetate fraction which also showed high neuroprotectivity and metal chelating ability was selected for the phytochemical analysis. Our results confirmed the presence of trimyristin and 5,7-diacetyl chrysin (reported for the first time in M. fragrans) in the corresponding fraction.

Treatment of Lupus Nephritis from Iranian Traditional Medicine and Modern Medicine Points of View: A Comparative Study.

OBJECTIVE: Nephritis or kidney inflammation is characterized as one of the most common renal disorders leading to serious damage to the kidneys. Nephritis, especially lupus nephritis (LN), has remained as the main cause of chronic renal failure which needs serious therapeutic approaches such as dialysis and kidney transplant. Heredity, infection, high blood pressure, inflammatory diseases such as lupus erythematosus and inflammatory bowel disease, and drug-related side effects are known as the main causes of the disease. According to Iranian traditional medicine (ITM), infectious diseases and fever are the main reasons of nephritis, which is called "Varam-e-Kolye" (VK). RESULTS: There are various plant-based remedies recommended by ITM for the treatment of nephritis, as discussed herein, comparing with those available in the modern medicine. There is no definite cure for the treatment of nephritis, and immunosuppressive drugs such as corticosteroids and nonsteroidal anti-inflammatory drugs, antibiotics, diuretics, analgesics, and finally dialysis and kidney transplantation are usually used. Based on the efficacy of medicinal plants, jujube (Ziziphus jujuba), almond (Prunus amygdalus), pumpkin seeds (Cucurbita pepo), purslane (Portulaca oleracea), and fig (Ficus carica) were found to be effective for the treatment of kidney inflammation in ITM. CONCLUSION: Considering the fact that there is no efficient strategy for the treatment of nephritis, use of herbal medicine, particularly based on the fruits or nuts that have been safely used for several years can be considered as a versatile supplement along with other therapeutic methods.

Phytochemical Analysis and Evaluation of Biological Activity of Lawsonia inermis Seeds Related to Alzheimer's Disease.

Using Lawsonia inermis L. (henna) seeds has been frequently recommended for the improvement of memory in Iranian Traditional Medicine (ITM). In this respect, different fractions of the plant were prepared and evaluated for their in vitro biological assays related to Alzheimer's disease (AD), including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity as well as metal chelating ability and DPPH antioxidant activity. The dichloromethane and ethyl acetate fractions were able to inhibit the BChE selectively with IC50 values of 113.47 and 124.90 µg/mL, respectively, compared with donepezil as the reference drug (IC50 = 1.52 µg/mL). However, all fractions were inactive toward AChE. Phytochemical analysis of the dichloromethane fraction indicated the presence of ß-sitosterol (1), 3-O-ß-acetyloleanolic acid (2), 3-O-(Z)-coumaroyl oleanolic acid (3), betulinic acid (4), and oleanolic acid (5). The inhibitory activity of isolated compounds was also evaluated toward AChE and BChE. Among them, compounds 2 and 5 showed potent inhibitory activity toward BChE with IC50 values of 77.13 and 72.20 µM, respectively. However, all compounds were inactive toward AChE. Moreover, molecular docking study confirmed desired interactions between those compounds and the BChE active site. The ability of fractions and compounds to chelate biometals (Cu2+, Fe2+, and Zn2+) was also investigated. Finally, DPPH antioxidant assay revealed that the ethyl acetate (IC50 = 3.08 µg/mL) and methanol (IC50 = 3.64 µg/mL) fractions possessed excellent antioxidant activity in comparison to BHA as the positive control (IC50 = 3.79 µg/mL).

A Review on Antidiabetic Activity of Centaurea spp.: A New Approach for Developing Herbal Remedies.

OBJECTIVE: Diabetes mellitus (DM) is a long-life metabolic disorder, characterized by high blood glucose levels. The hyperglycemic condition generally leads to irreversible nerve injury and vascular damage. Among different types of diabetes, type 2 is more common and has spread all over the world. Although various therapeutic approaches have been developed to control type 2 DM, regulating blood glucose levels has still remained a controversial challenge for patients. Also, most prescription drugs cause different side effects, such as gastrointestinal disorders. Thus, developing novel and efficient antidiabetic agents possessing fewer adverse effects is in high demand. METHOD: The literature was comprehensively surveyed via search engines such as Google Scholar, PubMed, and Scopus using appropriate keywords. RESULTS: Medicinal plants, both extracts and isolated active components, have played a significant role in controlling the blood glucose levels. Good-to-excellent results documented in the literature have made them a precious origin for developing and designing drugs and supplements against DM. Centaurea spp. have been traditionally used for controlling high blood glucose levels. Also, the antidiabetic properties of different species of Centaurea have been confirmed in recent studies through in vitro assays as well as in vivo experiments. CONCLUSION: Potent results encouraged us to review their efficacy to open a new horizon for development of herbal antidiabetic agents.

Investigation of anti-Alzheimer's activity of aqueous extract of areca nuts (Areca catechu L): in vitro and in vivo studies / Investigación de la actividad anti-Alzheimer del extracto acuoso de nueces de areca (Areca catechu L): estudios in vitro e in vivo

Alzheimer's disease (AD) is an age-related neurodegenerative disorder. Sever cognitive and memory impairments, huge increase in the prevalence of the disease, and lacking definite cure have absorbed worldwide efforts to develop therapeutic approaches. Since many drugs have failed in the clinical trials due to multifactorial nature of AD, symptomatic treatments are still in the center attention and now, nootropic medicinal plants have been found as versatile ameliorators to reverse memory disorders. In this work, anti-Alzheimer's activity of aqueous extract of areca nuts (Areca catechu L.) was investigated via in vitro and in vivo studies. It depicted good amyloid ß (Aß) aggregation inhibitory activity, 82% at 100 µg/mL. In addition, it inhibited beta-secretase 1 (BACE1) with IC50 value of 19.03 µg/mL. Evaluation of neuroprotectivity of the aqueous extract of the plant against H2O2-induced cell death in PC12 neurons revealed 84.5% protection at 1 µg/mL. It should be noted that according to our results obtained from Morris Water Maze (MWM) test, the extract reversed scopolamine-induced memory deficit in rats at concentrations of 1.5 and 3 mg/kg.

La enfermedad de Alzheimer (EA) es un trastorno neurodegenerativo relacionado con la edad. Los severos deterioros cognitivos y de la memoria, el enorme aumento de la prevalencia de la enfermedad y la falta de una cura definitiva han absorbido los esfuerzos mundiales para desarrollar enfoques terapéuticos. Dado que muchos fármacos han fallado en los ensayos clínicos debido a la naturaleza multifactorial de la EA, los tratamientos sintomáticos siguen siendo el centro de atención y ahora, las plantas medicinales nootrópicas se han encontrado como mejoradores versátiles para revertir los trastornos de la memoria. En este trabajo, se investigó la actividad anti-Alzheimer del extracto acuoso de nueces de areca (Areca catechu L.) mediante estudios in vitro e in vivo. Representaba una buena actividad inhibidora de la agregación de amiloide ß (Aß), 82% a 100 µg/mL. Además, inhibió la beta-secretasa 1 (BACE1) con un valor de CI50 de 19,03 µg/mL. La evaluación de la neuroprotección del extracto acuoso de la planta contra la muerte celular inducida por H2O2 en neuronas PC12 reveló una protección del 84,5% a 1 µg/mL. Cabe señalar que, de acuerdo con nuestros resultados obtenidos de la prueba Morris Water Maze (MWM), el extracto revirtió el déficit de memoria inducido por escopolamina en ratas a concentraciones de 1,5 y 3 mg/kg.

Plant Polyphenols: Natural and Potent UV-Protective Agents for the Prevention and Treatment of Skin Disorders.

Nowadays, destructive and immunosuppressive effects from long-term exposure to UV radiation have been fully investigated and documented in the literature. UV radiation is known as the main cause of skin aging and carcinogenesis. Hence, skin protection against anti-oxidative and immunosuppressive processes is highly in demand. Now, plant polyphenols have been found as a versatile and natural tool for the prevention and treatment of various skin diseases. The presence of a large number of hydroxyl groups in the cyclic structure of polyphenols has induced valuable biological activities. Among them, their UV protective activity has attracted lots of attention due to promising efficacy and simple instruction to use.

Thieno[2,3-b]pyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease.

In search of safer tacrine analogs, various thieno[2,3-b]pyridine amine derivatives were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs). Among the synthesized compounds, compounds 5e and 5d showed the highest activity towards acetylcholinesterase and butyrylcholinesterase, with IC50 values of 1.55 and 0.23 µM, respectively. The most active ChE inhibitors (5e and 5d) were also candidates for further complementary assays, such as kinetic and molecular docking studies as well as studies on inhibitory activity towards amyloid-beta (ßA) aggregation and ß-secretase 1, neuroprotectivity, and cytotoxicity against HepG2 cells. Our results indicated efficient anti-Alzheimer's activity of the synthesized compounds.

Anti-cholinesterase and Neuroprotective Activities of Sweet and Bitter Apricot Kernels (Prunus armeniaca L.).

Apricot (Prunus armeniaca L.) is a fruit cultivated in various parts of the world. Both sweet and bitter kernels of apricot have been used for the treatment of different diseases such as loss of memory in Iranian traditional medicine (ITM). In the present study, the inhibitory activity of sweet and bitter extracts of apricot kernels towards cholinesterase (ChE) enzymes, both acetyl and butyrylcholinesterase was examined through Ellman's method. In addition, neuroprotectivity of aqueous extracts and amygdalin were investigated against H2O2-induced cell death in PC12 neurons. Among them, the best acetylcholinesterase (AChE) inhibitory activity (IC50 = 134.93 ± 2.88 µg/mL) and neuroprotectivity (P-value < 0.0001) were obtained by the aqueous extract of bitter type. It was found that all extracts showed no butyrylcholinesterase (BChE) inhibitory activity.

Glycosides from Medicinal Plants as Potential Anticancer Agents: Emerging Trends Towards Future Drugs.

BACKGROUND: Cancer continues to be a global burden, despite the advancement of various technological and pharmaceutical improvements over the past two decades. Methods for treating cancer include surgery, radiotherapy and chemotherapy in addition to other specialized techniques. On the other hand, medicinal plants have been traditionally employed either as the complementary medicine or dietary agents in the treatment and management of cancer. Medicinal plants are a rich source of secondary metabolites with interesting biological and pharmacological activities. Among these metabolites, glycosides are naturally occurring substances and have outstanding therapeutic potential and clinical utility. METHODS: Different medical research engines such as, GoogleScholar, PubMed, SpringerLink, ScienceDirect were used to collect related literature on the subject matter. In this regard, only peer-reviewed journals were considered. RESULTS: Emerging results showed that numerous glycosides isolated from various plants possessed marked anticancer activity against a variety of cancer cell lines. Accordingly, the aim of the present review is to shed light on the anticancer effects of glycosides, analyze possible mechanisms of action, and highlight the role of these natural agents as complementary and alternative medicine in combating and managing cancer. CONCLUSION: The glycosides isolated from different plants demonstrated potent cytotoxic effects against various cancer cell lines in initial preclinical studies. The anticancer effect was mediated through multiple mechanisms; however further detailed studies are needed to understand the full potential of glycosides for clinical utility.

Phthalate contamination of some plants and herbal products / Contaminación de algunas plantas y productos herbales con ftalatos

Phthalate derivatives cause a number of risks to human health and the environment. Essential oil and volatile fractions of some vegetables and herbal products were extracted by hydrodistillation and percolation methods to analyze using gas chromatography and mass spectrometry (GC-MS) for evaluation of phthalate contaminations. The results revealed that four vegetables and all aromatic waters were contaminated by phthalate derivatives including di-n-butyl phthalate (DBP), diisobutyl phthalate and di-(2-ethylhexyl) phthalate (DEHP) (0.1-7.95%). Butylated hydroxytoluene (BHT), a widely used synthetic antioxidant, was also found in the most of the aromatic waters in the range of 3.15-61.3%. In addition, three vegetable samples contained diazinon (0.36-4.61%), an organophosphorus insecticide. Plants and herbal preparations may be contaminated by the absorption of phthalates from contaminated water or soil or by the migration of phthalates from inexpensive recycled plastic. Regarding the widespread use and associated health risks of phthalates, effective quality and safety regulations for herbal products should be implemented with respect to their phthalate content.

Los derivados de ftalato causan una serie de riesgos para la salud humana y el medio ambiente. El aceite esencial y las fracciones volátiles de algunos vegetales y productos a base de hierbas fueron extraídos mediante hidrodestilación y métodos de percolación y luego fueron analizados mediante cromatografía de gases y espectrometría de masas (GC-MS) con el propósito de identificar contaminación con ftalatos. Los resultados revelaron que cuatro productos herbales y todas las aguas aromáticas analizadas estaban contaminadas con derivados de ftalato, incluyendo el ftalato de dibutulo (DBP), ftalato de diisobutilo y ftalato de bis(2-etilhexilo) (DEHP) (0.1-7.95%). El butilhidroxitolueno (BHT), un antioxidante sintético ampliamente utilizado, también se encontró en aguas aromáticas en el rango de 3.15- 61.3%. Además, tres muestras vegetales contenían diazinón (0.36-4.61%), un insecticida organofosforado. Las plantas y las preparaciones herbales pueden ser contaminadas a partir de absorción de ftalatos del agua o el suelo contaminados o por la migración de ftalatos desde plástico reciclado de bajo costo. Con respecto al uso generalizado y los riesgos asociados a la salud de los ftalatos, deben implementarse normas efectivas de calidad y seguridad para los productos a base de hierbas con respecto a su contenido de ftalato.

In vitro cholinesterase inhibitory activity of some plants used in Iranian traditional medicine.

In this study, in vitro evaluation of cholinesterase inhibitory (ChEI) activity of various plants including betel nuts (Areca catechu L.), clove buds (Syzygium aromaticum L.), aerial parts of dodder (Cuscuta chinensis Lam.), common polypody rhizomes (Polypodium vulgare L.) and turpeth roots (Ipomoea turpethum R. Br.) which were recommended for the treatment of AD symptoms in Iranian Traditional Medicine (ITM) is reported. Among them, aqueous extract of A. catechu L. was found as the most potent anti-AChE (IC50 = 32.00 µg/mL) and anti-BChE (IC50 = 48.81 ± 0.1200 µg/mL) agent.

Caring for Newborn's Umbilical Cord from Iranian Traditional Medicine Point of View.

BACKGROUND: It is evident that infant's umbilical cord is essential for its survival and growth. In the past, it was not considered as a necessary tissue. However, nowadays, it has attracted lots of attention and its relation to different diseases has been demonstrated. In Iranian traditional medicine, caring for newborn's umbilical cord has been frequently recommended and it has been associated with different diseases. METHODS: Herein, Iranian traditional medicine resources such as "Qanun-fil-Tibb", "Exir-e-Azam", and "Tib-e-Akbari" were studied. In addition, recent developments in classical medicine were reviewed using search engines including Google Scholar, PubMed, SID, and IranMedex. RESULTS: It has been revealed that there is a direct relation between early cord clamping and oxidative stress, anemia, and low cardiac output. In Iranian traditional medicine, it is believed that the umbilical cord length, which should be cut off, is important. A short cord may lead to bladder contraction and frequent urination. Furthermore, if the umbilical cord is not squeezed efficiently, its content may enter the bladder, testis, and stomach leading to various diseases. CONCLUSION: It seems that the remarks by the Iranian traditional medicine on caring for newborn's umbilical cord can be useful for the prevention of different diseases.

Medicinal Plants Used in Iranian Traditional Medicine (ITM) as Contraceptive Agents.

BACKGROUND: In recent years, rapid population growth and unsafe abortions have emerged as controversial health issues in some countries. Hence, safe and effective contraceptive methods or agents have attracted a great deal of attention and the corresponding market has been widely expanded. OBJECTIVE: In this study, we present a review profiting from Iranian Traditional Medicine (ITM) to introduce expedient plants as efficient contraceptive agents. METHODS: Medicinal plants suggested as contraceptive agents were obtained from ITM text books and they were also investigated using search engines to confirm their in vitro and in vivo efficacy. RESULTS: According to credible Iranian medical literature a wide spectrum of plants possesses contraceptive activity and among them, Ruta graveolens, Ricinus communis, Piper nigrum, and Physalis alkekengi were found to be more efficient. CONCLUSION: Complementary and Alternative Medicine (CAM), particularly herbal remedies have received a lot of attention because of their truly healing properties. Focusing on ITM knowledge, there are various comments based on medicinal plants to reduce unsafe abortions leading to better public health in the society.

Curcumin-loaded guanidine functionalized PEGylated I3ad mesoporous silica nanoparticles KIT-6: practical strategy for the breast cancer therapy.

In this research, we have synthesized guanidine functionalized PEGylated mesoporous silica nanoparticles as a novel and efficient drug delivery system (DDS). For this purpose, guanidine functionalized PEGylated I3ad mesoporous silica nanoparticle KIT-6 [Gu@PEGylated KIT-6] was utilized as a promising system for the effective delivery of curcumin into the breast cancer cells. The modified mesoporous silica nanoparticles (MSNs) was fully characterized by different techniques such as transmission and scanning electron microscopy (TEM & SEM), N2 adsorption-desorption measurement, thermal gravimetric analysis (TGA), X-ray powder diffraction (XRD), and dynamic light scattering (DLS). The average particle size of [Gu@PEGylated KIT-6] and curcumin loaded [Gu@PEGylated KIT-6] nanoparticles were about 60 and 70 nm, respectively. This new system exhibited high drug loading capacity, sustained drug release profile, and high and long term anticancer efficacy in human cancer cell lines. It showed pH-responsive controlled characteristics and highly programmed release of curcumin leading to the satisfactory results in in vitro breast cancer therapy. Our results depicted that the pure nanoparticles have no cytotoxicity against human breast adenocarcinoma cells (MCF-7), mouse breast cancer cells (4T1), and human mammary epithelial cells (MCF10A).