Haralambos E. Katerinopoulos

Professor of Organic Chemistry

Tel: +30 2810 545026
Fax: +30 2810 545001
E-mail: kater@chemistry.uoc.gr
Link to Group page: http://www.chemistry.uoc.gr/katerinopoulos

Education

Research interests

1. Synthesis of Fluorescent Ion Indicators.        

Our contribution to this field includes the synthesis of a number of fluorescent probes for intracellular ions.  Initial experiments performed by the author during his post doctoral work at Smith Kline and French Labs (USA), aimed at the synthesis of calcium probes with improved fluorescent properties than those already available in the market such as fura-2.  This project ended successfully with the synthesis of a number of intracellular calcium probes such as FuraRed and FuraRed-AM which were patented by SKF Labs and are currently commercially available (Handbook of Fluorescent Probes and Research Chemicals, Molecular Probes, Eugene, OR, USA).   
This project was continued in our laboratory resulting in the preparation of seven new calcium probes including BTC and BTC-AM, with improved properties (chemical stability, fluorescence profile) incorporating the coumarin chromophore.  The inventorship on these materials has been granted by a joint patent with Molecular Probes-USA.  A number of structural modifications on the above mentioned compounds led to further improved calcium as well as magnesium ion probes such as APTRA-BTC and APTRA BTC-AM.  A third project on zinc probes in collaboration with the University of Iowa yielded a number of zinc robes such as ICPBC-Zin.
We have recently completed the design and synthesis of ratiometric and “turn-on” probes for lead and mercury.

2. Isolation and Structure Determination of Components from Aromatic and Pharmaceutical Plants from the Flora of Crete.    
This project that has been financed from various sources, targets the systematic characterization of the active ingredients from plants with known aromatic and/or pharmaceutical properties and the total synthesis of isolated new natural products.    
The shrub of labdanum ( Cistus creticus L., subspecies creticus), a plant that grows only in a few areas of the Mediterranean and it is known for its pharmaceutical  properties, was initially selected as a representative species.  The project was extended in a study of the components from a second subspecies of the plant (ssp. Eriocephalus) aiming at the chemotaxinomic differentiation of the two subspecies, as a part of a project in collaboration with the local Chamber of Commerce.  We also studied the composition of the essential oils of a number of plants (Lavandula stoechas L., Salvia fructicosa Miller, Laura sp, Rosmarinus officinalis L) in collaboration with the local Plant Protection Institute.  The total synthesis of Drymenene , a proposed component of Cistus creticus L., has been reported in the literature.
Our group expanded its activities in the study of aromatic and pharmaceutical plants with tasks such as:

  1. Improvement of the isolation methodology for the aromatic resin “Labdanum” from Cistus Creticus L. Supported by local companies.
  2. Use of extracts from rosemary, lavender, sage and laurel as pest control agents in vineyards as well as in the preservation of raisins.
  3.  Production and quality control of essential oils from sage, dictamo (O. dictamnus L.) and the resin of labdanum.
  4. Scientific support in securing the certificate of origin of the herb Origanum dictamnus L. to the region of Crete (initiative taken by the Co-operative of Embaros, Crete).
  5. Quality control of local Origanum species cultivated under controlled conditions.
  6. Quality control of herbs available in the local market by using the composition of their essential oils as “fingerprint” of each subspecies.
  7. Identification of components of aromatic plants with anti-microbial and anti-cancer agents.
  8. Use of natural colorants from Dittrichia viscosa in textile dyeing.
  9. Use of costic acid and other components from the plant Dittrichia viscosa as acaricide against Varroa destructor, the acari acting as parasite of the European honey bee.
Verifying the proposed activity of Chios Mastic Gum (Pistacia lentiscus var. chia) against Helicobacter pylori using in vitro and in vivo studies.

 

Synthesis and Structure - Activity Relationship (SAR) Studies of Rigid Dopamine Analogs.

This program was terminated in 2001. It included the total synthesis of compounds which incorporate the dopamine moiety in a larger carbon framework. In vitro (binding and functional ) studies of this analogs provided valuable information on the relation of their activity to structural elements such as O-N distance, dihedral angles and oxygen and nitrogen substitution within the dopamine group. The discovery that a number of these compounds also exhibited adrenergic activity prompted us to extend our studies to a1 and a2 adrenergic receptors. Our methodology involved "Selected Disconnections" on known active compounds such as ABBOT-68930 leading to less complex molecules. Results from SAR studies on such compounds provided valuable information on the "active moiety" of the mother molecules, leading to the synthesis of drugs with optimized activity and higher selectivity.

Recent publications

  1. Roussakis, E., Voutsadaki, S., Pinakoulaki, E., Sideris, D.P., Tokatlidis, K., Katerinopoulos, H.E. 
    ICPBCZin: A red emitting ratiometric fluorescent indicator with nanomolar affinity for Zn2+ ions
    .
    Cell Calcium 2008, 44,270-275. 
  2. Roussakis, E., Pergantis, S.A., Katerinopoulos, H.E.
    Coumarin-based ratiometric fluorescent indicators with high specificity for lead ions
    Chem. Commun.  2008, 46, 6221-6223. 
  3. Dakanali, M., Tsikalas, G.K., Krautscheid, H., Katerinopoulos, H.E. 
    Formate ester synthesis via reaction of 2-bromoethylamines with dimethylformamide
    Tet. Letters 2008, 49, 1648-1651.
  4. H. E. Katerinopoulos, D. Isaakidis, K. Sofou, A. Spyros
    Use of costic acid and other components from the plant Dittrichia viscosa (Greek: “Aconiza”) and related species, as acaricide against Varroa destructor, the acari acting as parasite of the European honey bee.
    WO/2009/153607

  5. H. E. Katerinopoulos, D. Isaakidis, K. Sofou, A. Spyros
    Use of costic acid and other components from the plant Dittrichia viscosa (Greek: “Aconiza”) and related species, as acaricide against Varroa destructor, the acari acting as parasite of the European honey bee.
    International Patent, PCT Appl. No. 20080100414, 2009
  6. Kokolakis, A. K.; Kouvarakis, A. N.; Katerinopoulos, H. E.
    Effect of hydrodistillation with phosphoric acid on the yield of Chios mastic gum essential oil.
    Flav. Fragr.
    2010, 25,48-53
  7. Voutsadaki, S., Tsikalas, G.K., Klontzas, E., Froudakis, G.E., Katerinopoulos, H.E.
    A "turn-on" coumarin-based fluorescent sensor with high selectivity for mercury ions in aqueous media 
    Chemical Communications
    2010, 46, 3292-3294
  8. Tagmatarchis, N., Pagona, G., Economopoulos, E. P., Tsikalas, G. K., Katerinopoulos, H. E.
    Fullerene-coumarin dyad as selective metal receptor. Synthesis, photophysical properties, electrochemistry and ion binding studies
    Chem. Eur. J. http://dx.doi.org/10.1002/chem.201001665