Chemical Composition and Enzymatic Screening of Micromeria fruticosa serpyllifolia Volatile Oils Collected from Three Different Regions of West Bank, Palestine

Introduction. Volatile oils (VOs) have been commonly used in cosmetics and food as fragrances, flavoring, and preservative agents or in alternative medicine for their therapeutic effects. This necessitates investigating those plants and their VOs. This study was conducted to investigate the chemical compositions of the VOs of Micromeria fruticosa serpyllifolia growing widely in three regions in Palestine (i.e., Hebron, Ramallah, and Nablus districts representing south, middle, and north of West Bank). Afterwards, VOs were subjected to in vitro screening and their enzymatic properties were compared. Methods. The analysis of chemical components of VOs was performed by gas chromatography coupled with mass spectrometry (GC-MS). The antilipase activity was evaluated using porcine pancreatic lipase and p-nitrophenyl butyrate. The antiamylase activity was assessed using porcine pancreatic α-amylase, starch, and 3,5-dinitrosalicylic. Results. Plant extracts yield range was 0.67 to 0.99 w/w%. GC-MS analysis showed the high percentages of oxygenated components in the range of 86.1-89.88% and nonoxygenated components in the range of 4.38-4.71%. Seven components were observed, pulegone was the most abundant component in the three samples in the range of 74.43-86.04%, and isomenthone was the second most abundant component with the range of 3.16-14.41%. The sample collected from Nablus showed the most potent antilipase and antiamylase activity with IC50 values of 39.81 μg/mL and 3.31 μg/mL, respectively. Conclusions. The study showed that Micromeria fruticosa serpyllifolia volatile oils samples from different regions in Palestine contained different proportions of phytochemicals which provided different potential biological activities such as antiobesity and antidiabetes activities that were in line with traditional uses of the plant extracts. The plant extracts showed higher antilipase and antiamylase potency than that of the relative references and there were significant differences in these activities compared to each other.

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Houttuynia cordata Thunb: An Ethnopharmacological Review

Frontiers in Pharmacology ◽

10.3389/fphar.2021.714694 ◽

2021 ◽

Vol 12 ◽

Author(s):

Zhao Wu ◽

Xinyu Deng ◽

Qichao Hu ◽

Xiaolin Xiao ◽

Jing Jiang ◽

...

Keyword(s):

Biological Activities ◽

Chemical Constituents ◽

Inflammatory Factors ◽

Lung Tumour ◽

Therapeutic Effects ◽

Volatile Oils ◽

Edible Plant ◽

Houttuynia Cordata

Houttuynia cordata Thunb (H. cordata; Saururaceae) is widely distributed in Asian regions. It plays an important role in traditional health care and disease treatment, as its aboveground stems and leaves have a long medicinal history in China and are used in the treatment of pneumonia and lung abscess. In clinical treatment, it can usually be combined with other drugs to treat dysentery, cold, fever, and mumps; additionally, H. cordata is an edible plant. This review summarizes detailed information on the phytochemistry and pharmacological effects of H. cordata. By searching the keywords “H. cordata and lung”, “H. cordata and heart”, “H. cordata and liver”, and “H. cordata and inflammation” in PubMed, Web of Science and ScienceDirect, we screened out articles with high correlation in the past ten years, sorted out the research contents, disease models and research methods of the articles, and provided a new perspective on the therapeutic effects of H. cordata. A variety of its chemical constituents are characteristic of medicinal plants, the chemical constituents were isolated from H. cordata, including volatile oils, alkaloids, flavonoids, and phenolic acids. Flavonoids and volatile oils are the main active components. In pharmacological studies, H. cordata showed organ protective activity, such as reducing the release of inflammatory factors to alleviate lung injury. Moreover, H. cordata regulates immunity, enhances the immune barriers of the vagina, oral cavity, and intestinal tract, and combined with the antibacterial and antiviral activity of its extract, effectively reduces pathogen infection. Furthermore, experiments in vivo and in vitro showed significant anti-inflammatory activity, and its chemical derivatives exert potential therapeutic activity against rheumatoid arthritis. Antitumour action is also an important pharmacological activity of H. cordata, and studies have shown that H. cordata has a notable effect on lung tumour, liver tumour, colon tumour, and breast tumour. This review categorizes the biological activities of H. cordata according to modern research papers, and provides insights into disease prevention and treatment of H. cordata.

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Novel Iodinated Hydrazide-hydrazones and their Analogues as Acetyl- and Butyrylcholinesterase Inhibitors

Current Topics in Medicinal Chemistry ◽

10.2174/1568026620666200819155503 ◽

2020 ◽

Vol 20 (23) ◽

pp. 2106-2117

Author(s):

Martin Krátký ◽

Šárka Štěpánková ◽

Michaela Brablíková ◽

Katarína Svrčková ◽

Markéta Švarcová ◽

...

Keyword(s):

Biological Activities ◽

Structural Parameters ◽

Covalent Binding ◽

Docking Studies ◽

Potent Inhibition ◽

Brain Barrier Permeability ◽

Electric Eel ◽

Ic50 Values ◽

Ellman’S Method

Background: Hydrazide-hydrazones have been known as scaffold with various biological activities including inhibition of acetyl- (AChE) and butyrylcholinesterase (BuChE). Cholinesterase inhibitors are mainstays of dementias’ treatment. Objective: Twenty-five iodinated hydrazide-hydrazones and their analogues were designed as potential central AChE and BuChE inhibitors. Methods: Hydrazide-hydrazones were synthesized from 4-substituted benzohydrazides and 2-/4- hydroxy-3,5-diiodobenzaldehydes. The compounds were investigated in vitro for their potency to inhibit AChE from electric eel and BuChE from equine serum using Ellman’s method. We calculated also physicochemical and structural parameters for CNS delivery. Results: The derivatives exhibited a moderate dual inhibition with IC50 values ranging from 15.1-140.5 and 35.5 to 170.5 μmol.L-1 for AChE and BuChE, respectively. Generally, the compounds produced a balanced or more potent inhibition of AChE. N'-[(E)-(4-Hydroxy-3,5-diiodophenyl)methylidene]-4- nitrobenzohydrazide 2k and 4-fluoro-N'-(2-hydroxy-3,5-diiodobenzyl)benzohydrazide 3a were the most potent inhibitors of AChE and BuChE, respectively. Structure-activity relationships were established, and molecular docking studies confirmed interaction with enzymes. Conclusion: Many novel hydrazide-hydrazones showed lower IC50 values than rivastigmine against AChE and some of them were comparable for BuChE to this drug used for the treatment of dementia. They interact with cholinesterases via non-covalent binding into the active site. Based on the BOILEDEgg approach, the majority of the derivatives met the criteria for blood-brain-barrier permeability.

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Melatonin in Cancer Treatment: Current Knowledge and Future Opportunities

Molecules ◽

10.3390/molecules26092506 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2506

Author(s):

Wamidh H. Talib ◽

Ahmad Riyad Alsayed ◽

Alaa Abuawad ◽

Safa Daoud ◽

Asma Ismail Mahmod

Keyword(s):

Clinical Trials ◽

Current Knowledge ◽

Biological Activities ◽

Experimental Studies ◽

Therapeutic Effects ◽

Cell Proliferation Inhibition ◽

Different Types ◽

Solid Foundation

Melatonin is a pleotropic molecule with numerous biological activities. Epidemiological and experimental studies have documented that melatonin could inhibit different types of cancer in vitro and in vivo. Results showed the involvement of melatonin in different anticancer mechanisms including apoptosis induction, cell proliferation inhibition, reduction in tumor growth and metastases, reduction in the side effects associated with chemotherapy and radiotherapy, decreasing drug resistance in cancer therapy, and augmentation of the therapeutic effects of conventional anticancer therapies. Clinical trials revealed that melatonin is an effective adjuvant drug to all conventional therapies. This review summarized melatonin biosynthesis, availability from natural sources, metabolism, bioavailability, anticancer mechanisms of melatonin, its use in clinical trials, and pharmaceutical formulation. Studies discussed in this review will provide a solid foundation for researchers and physicians to design and develop new therapies to treat and prevent cancer using melatonin.

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In Vitro Study of Multi-Therapeutic Properties of Thymus bovei Benth. Essential Oil and Its Main Component for Promoting Their Use in Clinical Practice

Journal of Clinical Medicine ◽

10.3390/jcm7090283 ◽

2018 ◽

Vol 7 (9) ◽

pp. 283 ◽

Cited By ~ 8

Author(s):

Sherif Hassan ◽

Kateřina Berchová-Bímová ◽

Miroslava Šudomová ◽

Milan Malaník ◽

Karel Šmejkal ◽

...

Keyword(s):

Gas Chromatography ◽

Clinical Practice ◽

Essential Oil ◽

Biological Activities ◽

Structural Parameters ◽

Antihypertensive Agents ◽

Gas Chromatography Mass Spectrometry ◽

Ic50 Values ◽

Main Component

Thymus bovei Benth. (TB) is an important plant in the traditional medicine of the Mediterranean region. This study investigates the health-promoting properties of TB essential oil (TB-EO) for its possible use in clinical practice with regards to its cytotoxic, anti-herpes simplex virus type 2 (HSV-2), and antihypertensive (through inhibition of human angiotensin-converting enzyme; ACE) properties. The phytochemical profile of EO (99.9%) was analyzed by Gas Chromatography with Flame-Ionization Detection (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS). In this study, all biological methods were performed at the level of in vitro studies. The results showed that TB-EO exerted remarked cytotoxic properties against human cervical carcinoma cells, colon cancer cells, and lung adenocarcinoma cells with the half-maximal inhibitory concentration (IC50) values of 7.22, 9.30, and 8.62 µg/mL, respectively, in comparison with that of standard anticancer drug cisplatin with IC50 values of 4.24, 5.21, and 5.43 µg/mL, respectively. Fascinatingly, TB-EO showed very weak cytotoxicity on the healthy human fetal lung fibroblast cells with an IC50 value of 118.34 µg/mL compared with that of cisplatin (IC50 = 10.08 µg/mL). TB-EO, its main component geraniol, TB-EO combined with acyclovir (ACV) along with standard ACV, have displayed pronounced inhibitory properties against the replication of HSV-2 with the half-maximal effective concentration (EC50) values of 2.13, 1.92, 0.81 and 1.94 µg/mL, respectively, with corresponding selectivity indices (SI) 98.59, 109.38, 259.26 and 108.25, respectively. TB-EO and geraniol at a concentration of 15 µg/mL showed prominent inhibitory activities against ACE with % of inhibition 95.4% and 92.2%, respectively, compared with that of standard inhibitor captopril (99.8%; 15 µg/mL). Molecular docking studies were performed to unveil the mechanism of action of geraniol as well as structural parameters necessary for anti-HSV-2 activity (through the inhibition of HSV-2 protease) and ACE inhibition. This is the first report on the chemical composition of Egyptian TB-EO along with the above-mentioned biological activities. Our results may be considered as novel findings in the course of a search for new and active anticancer, anti-HSV-2 and antihypertensive agents, and expand the medicinal value of this plant and its phytochemicals in clinical practice.

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In Vitro study for hesperidin nanoparticles effect on phagocytic activity against Staphylococcus aureus

Journal of Biotechnology Research Center ◽

10.24126/jobrc.2018.12.2.536 ◽

2018 ◽

Vol 12 (2) ◽

pp. 36-39

Author(s):

Saja Ali ◽

Ghassan Sulaiman ◽

Mohammed M. Al-Halbosiy

Keyword(s):

Biological Activities ◽

In Vitro Study ◽

Particle Size Analysis ◽

Poloxamer 407 ◽

Size Analysis ◽

Therapeutic Effects ◽

X Ray Diffraction ◽

Setup Cost ◽

Phagocytosis Index

Hesperidin is one of the flavonoids from citrus peels and it recognized to possess various biological activities such as, anti-inflammatory, anti-carcinogenic, antioxidant and antimicrobial potentials. The present investigation studies the immunological adjuvant influence of hesperidin nanoparticles. Hesperidin nanoparticles were prepared by nano-precipitation technique by using Poly (D, L-lactic-co-glycolic acid) (PLGA) polymer and Poloxamer 407 was used as a stabilizer. This method was used because of their advantage of low setup cost and simplicity. Hesperidin nanoparticles were characterized by fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD) and particle size analysis (PSA) analytical methods. The effect of hesperidin nanoparticles was higher than the effect of pure hesperidin, and there was an obvious increase in phagocytosis index (PI 82%) of hesperidin nanoparticles when compared with pure hesperidin (PI 56%) and in comparison with the control samples (PI 22%). In conclusion we need further studies about if nano-hesperidin has therapeutic effects.

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Machine Learning Analyses on Data including Essential Oil Chemical Composition and In Vitro Experimental Antibiofilm Activities against Staphylococcus Species

Molecules ◽

10.3390/molecules24050890 ◽

2019 ◽

Vol 24 (5) ◽

pp. 890 ◽

Cited By ~ 17

Author(s):

Alexandros Patsilinakos ◽

Marco Artini ◽

Rosanna Papa ◽

Manuela Sabatino ◽

Mijat Božović ◽

...

Keyword(s):

Machine Learning ◽

Opportunistic Pathogen ◽

Genetic Mutation ◽

Bacterial Biofilm ◽

Chemical Components ◽

Chemical Compositions ◽

Biofilm Production ◽

Major Interest ◽

Intravascular Catheters

Biofilm resistance to antimicrobials is a complex phenomenon, driven not only by genetic mutation induced resistance, but also by means of increased microbial cell density that supports horizontal gene transfer across cells. The prevention of biofilm formation and the treatment of existing biofilms is currently a difficult challenge; therefore, the discovery of new multi-targeted or combinatorial therapies is growing. The development of anti-bioﬁlm agents is considered of major interest and represents a key strategy as non-biocidal molecules are highly valuable to avoid the rapid appearance of escape mutants. Among bacteria, staphylococci are predominant causes of biofilm-associated infections. Staphylococci, especially Staphylococcus aureus (S. aureus) is an extraordinarily versatile pathogen that can survive in hostile environmental conditions, colonize mucous membranes and skin, and can cause severe, non-purulent, toxin-mediated diseases or invasive pyogenic infections in humans. Staphylococcus epidermidis (S. epidermidis) has also emerged as an important opportunistic pathogen in infections associated with medical devices (such as urinary and intravascular catheters, orthopaedic implants, etc.), causing approximately from 30% to 43% of joint prosthesis infections. The scientific community is continuously looking for new agents endowed of anti-biofilm capabilities to fight S. aureus and S epidermidis infections. Interestingly, several reports indicated in vitro efficacy of non-biocidal essential oils (EOs) as promising treatment to reduce bacterial biofilm production and prevent the inducing of drug resistance. In this report were analyzed 89 EOs with the objective of investigating their ability to modulate bacterial biofilm production of different S. aureus and S. epidermidis strains. Results showed the assayed EOs to modulated the biofilm production with unpredictable results for each strain. In particular, many EOs acted mainly as biofilm inhibitors in the case of S. epidermidis strains, while for S. aureus strains, EOs induced either no effect or stimulate biofilm production. In order to elucidate the obtained experimental results, machine learning (ML) algorithms were applied to the EOs’ chemical compositions and the determined associated anti-biofilm potencies. Statistically robust ML models were developed, and their analysis in term of feature importance and partial dependence plots led to indicating those chemical components mainly responsible for biofilm production, inhibition or stimulation for each studied strain, respectively.

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Derivatization of Rosmarinic Acid Enhances its in vitro Antitumor, Antimicrobial and Antiprotozoal Properties

Molecules ◽

10.3390/molecules24061078 ◽

2019 ◽

Vol 24 (6) ◽

pp. 1078 ◽

Cited By ~ 9

Author(s):

Silvia Bittner Fialová ◽

Martin Kello ◽

Matúš Čoma ◽

Lívia Slobodníková ◽

Eva Drobná ◽

...

Keyword(s):

Rosmarinic Acid ◽

Antimicrobial Agents ◽

Biological Activities ◽

Fold Increase ◽

Inhibitory Effect ◽

Phosphonium Salts ◽

Ros Scavenging ◽

Ic50 Values ◽

Quaternary Phosphonium Salts

On its own, rosmarinic acid possesses multiple biological activities such as anti-inflammatory, antimicrobial, cardioprotective and antitumor properties, and these are the consequence of its ROS scavenging and inhibitory effect on inflammation. In this study, two quaternary phosphonium salts of rosmarinic acid were prepared for the purpose of increasing its penetration into biological systems with the aim of improving its antimicrobial, antifungal, antiprotozoal and antitumor activity. The synthetized molecules, the triphenylphosphonium and tricyclohexylphosphonium salts of rosmarinic acid, exhibited significantly stronger inhibitory effects on the growth of HCT116 cells with IC50 values of 7.28 or 8.13 μM in comparison to the initial substance, rosmarinic acid (>300 μM). For the synthesized derivatives, we detected a greater than three-fold increase of activity against Acanthamoeba quina, and a greater than eight-fold increase of activity against A. lugdunensis in comparison to rosmarinic acid. Furthermore, we recorded significantly higher antimicrobial activity of the synthetized derivatives when compared to rosmarinic acid itself. Both synthetized quaternary phosphonium salts of rosmarinic acid appear to be promising antitumor and antimicrobial agents, as well as impressive molecules for further research.

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Screening of Antioxidant and Antimicrobial Activity of Micromeria fruticosa serpyllifolia Volatile Oils: A Comparative Study of Plants Collected from Different Regions of West Bank, Palestine

BioMed Research International ◽

10.1155/2020/4851879 ◽

2020 ◽

Vol 2020 ◽

pp. 1-7

Author(s):

Nihaya Salameh ◽

Naser Shraim ◽

Nidal Jaradat ◽

Motasem El Masri ◽

Lina Adwan ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Antioxidant Activity ◽

Antifungal Activity ◽

Plant Extracts ◽

Dilution Method ◽

Volatile Oils ◽

Three Samples ◽

Broth Microdilution Method ◽

Micromeria Fruticosa

Background. The investigation of volatile oils used in traditional medicine is vital to enhance the quality of healthcare. This study is aimed at screening the antioxidant and antimicrobial properties of Micromeria fruticosa serpyllifolia volatile oils from three different regions in Palestine (north, middle, and south). Methods. Volatile oils of three samples of M. fruticosa serpyllifolia were extracted using the microwave-ultrasonic apparatus. The antioxidant activity of the volatile oils was assessed by inhibition of DPPH free radical. The antimicrobial activity was examined using the broth microdilution method. Assessment of antifungal activity was achieved using the agar dilution method. Results. Screening the biological activity of plant extracts revealed that the sample from Ramallah (middle region) possessed the most potent antioxidant activity with an IC50 value of 0.45 μg/mL. The three samples exhibited broad antimicrobial activity and showed potential antifungal activity. The sample from the southern region showed the highest potency against Shigella sonnei with the lowest reported MIC; the sample from the northern region demonstrated the least potency against clinical isolate of Staphylococcus aureus and “methicillin”-resistant Staphylococcus aureus. Conclusions. The study showed that Micromeria fruticosa serpyllifolia volatile oil samples from different regions in Palestine possess different potential antioxidant and antimicrobial activities that were in line with traditional uses of the plant extracts.

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Momilactones A, B, and Tricin in Rice Grain and By-Products are Potential Skin Aging Inhibitors

Foods ◽

10.3390/foods8120602 ◽

2019 ◽

Vol 8 (12) ◽

pp. 602 ◽

Cited By ~ 3

Author(s):

Nguyen Van Quan ◽

Dam Duy Thien ◽

Tran Dang Khanh ◽

Hoang-Dung Tran ◽

Tran Dang Xuan

Keyword(s):

Liquid Chromatography ◽

High Performance ◽

Biological Activities ◽

Ultra Performance Liquid Chromatography ◽

Skin Aging ◽

Ionization Mass ◽

Rice Grain ◽

Synergistic Activity ◽

Ic50 Values

We previously reported the inhibitory potentials of momilactones A (MA) and B (MB) against key enzymes related to type 2 diabetes and obesity. In this study, antioxidant and anti-skin-aging activities of MA and MB were investigated and compared with tricin, a well-known antioxidant and antiaging flavonoid in rice. MA, MB, and tricin were purified from rice husk by column chromatography and their biological activities were subsequently assayed by in vitro trials. The contents of MA, MB, and tricin of different commercial rice cultivars in Japan were quantified and confirmed by ultra-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS) and high-performance liquid chromatography (HPLC) analyses. The antioxidant assays revealed a synergistic activity of the mixture MA and MB (MAB, 1:1, v/v). In addition, in 2,2’-azino-bis (ABTS) assay, IC50 values of MAB (0.3 mg/mL) and tricin (0.3 mg/mL) was 4-fold and 9-fold greater than that of individual MB (1.3 mg/mL) or MA (2.8 mg/mL), respectively. The in vitro enzymatic assays on pancreatic elastase and tyrosinase indicated that MA and MB were potential to relief skin wrinkles and freckles. In detail, MA exerted higher inhibition on both enzymatic activities (30.9 and 37.6% for elastase and tyrosinase inhibition, respectively) than MB (18.5 and 12.6%) and MAB (32.0 and 19.7%) at a concentration of 2.0 mg/mL. Notably, MA and the mixture MAB exhibited stronger inhibitions on elastase and tyrosinase in comparison with tricin and vanillin. MA, MB, and tricin in rice are potential to develop cosmetics as well as supplements for skin aging treatments.

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The Difference of Chemical Components and Biological Activities of the Raw Products slices and the Wine Steam-Processed Product from Cistanche deserticola

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/2167947 ◽

2019 ◽

Vol 2019 ◽

pp. 1-10 ◽

Cited By ~ 2

Author(s):

Ying Zhang ◽

Yuewu Wang ◽

Song Yang ◽

Yunfeng Xiao ◽

Haibin Guan ◽

...

Keyword(s):

Quantitative Analysis ◽

Biological Activities ◽

Biological Effects ◽

Chinese Herb ◽

Principal Component ◽

Deficiency Syndrome ◽

Chemical Components ◽

Chemical Compositions ◽

Kidney Deficiency ◽

Cistanche Deserticola

As a well-known Chinese herb medicine, the Cistanche deserticola has been used for the treatment of kidney deficiency syndrome in China for thousands of years. Both the raw product of Cistanche deserticola slices (RCD) and its Wine Steam-Processed Product (WSCD) are used clinically for different effects. In this study, the influences of steaming process with wine (SPW) from Cistanche deserticola on chemical compositions and biological effects were investigated. The principal component analysis (PCA) and quantitative analysis were used to study the differences of the chemical compositions. The effects of nourishing kidney were also investigated to compare the differences between the RCD and the WSCD. The PCA results indicated that the obvious separation was achieved in the RCD and WSCD. The results of quantitative analysis showed that the WSCD has higher amounts of total polysaccharides, total PhGs, isoacteoside, and osmanthuside B than RCD, while the content of 2′-acetylacteoside and acteoside decreased after the SPW. The comparison of RCD and WSCD on biological activities showed that both could restore the level of sex hormone in the model of kidney-yang deficiency and improve the antioxidant effect. The WSCD were much better in increasing the viscera weight of kidney and seminal vesicle. The results indicated that SPW changed its chemical components and enhanced its biological activities.

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