Psychoactive Plant Database - Neuroactive Phytochemical Collection

1. Nucleosides Nucleotides Nucleic Acids. 2024 Nov 7:1-14. doi: 
10.1080/15257770.2024.2426160. Online ahead of print.

In memory of an exquisite medicinal chemist, Prof. Morris Robins.

De Clercq E(1).

Author information:
(1)Department of Microbiology, Immunology and Transplantation, Rega Institute 
for Medical Research, Laboratory of Virology and Chemotherapy, KU Leuven, 
B-3000Leuven, Belgium.

Among the most prominent realizations of Morris J. Robins in the antiviral 
nucleoside chemistry are (i) the synthesis of 8-substituted (methyl-, amino-, 
bromo-, iodo) derivatives of acyclovir, (ii) xylotubercidin as an inhibitor of 
herpes simplex virus (HSV) infections, (iii) the anti-HIV activity of the 
2',3'-dideoxyriboside of 2,6-diaminopurine (ddDAPR) and the 3'-azido- and 
3'-fluoro derivatives thereof (AzddDAPR and FddDAPR, respectively), (iv) the 
potentiating effect of ribavirin on the anti-HIV activity of 
2',3'-dideoxyinosine (ddI) and ddDAPR, (v) S-adenosylhomocysteine hydrolase 
(SAH) inhibitors principally active against vaccinia virus (VV) and vesicular 
stomatitis virus (VSV), and (vi) furo[2,3-d]pyrimidinone derivatives active 
against varicella-zoster virus (VZV).

DOI: 10.1080/15257770.2024.2426160
PMID: 39508253


2. Inorg Chem. 2024 Nov 7. doi: 10.1021/acs.inorgchem.4c04050. Online ahead of 
print.

Tuning the Properties of Rigidified Acyclic DEDPA(2-) Derivatives for 
Application in PET Using Copper-64.

Torralba-Maldonado D(1), Marlin A(2), Lucio-Martínez F(3), Freire-García A(3), 
Whetter J(2), Brandariz I(3), Iglesias E(3), Pérez-Lourido P(4), Ortuño RM(1), 
Boros E(2), Illa O(1), Esteban-Gómez D(3), Platas-Iglesias C(3).

Author information:
(1)Departament de Química, Universitat Autònoma de Barcelona, 08193, Cerdanyola 
del Vallès, Spain.
(2)Department of Chemistry, University of Wisconsin-Madison, Madison, Wisconsin 
53706, United States.
(3)Centro Interdisciplinar de Química e Bioloxía (CICA) and Departamento de 
Química, Facultade de Ciencias, Universidade da Coruña, Galicia, 15071 A Coruña, 
Spain.
(4)Departamento de Química Inorgánica, Facultad de Química, Universidade de 
Vigo, As Lagoas, Marcosende, 36310 Pontevedra, Spain.

We present a detailed investigation of the coordination chemistry toward 
[natCu/64Cu]copper of a series of H2DEDPA derivatives (H2DEDPA = 
6,6'-((ethane-1,2-diylbis(azanediyl))bis(methylene))dipicolinic acid) containing 
cyclohexyl (H2CHXDEDPA), cyclopentyl (H2CpDEDPA) or cyclobutyl (H2CBuDEDPA) 
spacers. Furthermore, we also developed a strategy that allowed the synthesis of 
a H2CBuDEDPA analogue containing an additional NHBoc group at the cyclobutyl 
ring, which can be used for conjugation to targeting units. The X-ray structures 
of the Cu(II) complexes evidence distorted octahedral coordination around the 
metal ion in all cases. Cyclic voltammetry experiments (0.15 M NaCl) evidence 
quasi-reversible reduction waves associated with the reduction of Cu(II) to 
Cu(I). The complexes show a high thermodynamic stability, with log KCuL values 
of 25.11(1), 22.18(1) and 20.19(1) for the complexes of CHXDEDPA2-, CpDEDPA2- 
and CBuDEDPA2-, respectively (25 °C, 1 M NaCl). Dissociation kinetics 
experiments reveal that both the spontaneous- and proton-assisted pathways 
operate at physiological pH. Quantitative labeling with 64CuCl2 was observed at 
0.1 nmol for CHXDEDPA2- and CpDEDPA2-, 0.025 nmol for CBuDEDPA2- and 1 nmol for 
CBuDEDPA-NHBoc2-, with no significant differences observed at 15, 30, and 60 
min. The radio-complexes are stable in PBS over a period of 24 h.

DOI: 10.1021/acs.inorgchem.4c04050
PMID: 39508185


3. Acta Orthop. 2024 Nov 7;95:625-632. doi: 10.2340/17453674.2024.42182.

Measurement of acute postoperative pain intensity in orthopedic trials: a 
qualitative concept elicitation study.

Bjørnholdt KT(1), Andersen CWG(2).

Author information:
(1)Department of Orthopedic Surgery, Horsens Regional Hospital, Denmark. 
karebo@rm.dk.
(2)Department of Orthopedic Surgery, Svendborg Hospital, Denmark.

BACKGROUND AND PURPOSE: Pain intensity is an important outcome in clinical 
trials of surgery because pain relief is important to patients. Currently, 
recommended scales are the numeric rating scale 0-10 and visual analogue scale. 
However, these scales allow for considerable influence of individual 
imagination, previous experience, and coping skills, limiting proficiency in 
comparative clinical trials. We aimed to explore postoperative expressions of 
"how much it hurts"-the first step to improve pain intensity measurement.
METHODS: This was a qualitative study using inductive content analysis: words 
and visual cues describing pain intensity were collected from (i) existing pain 
intensity measures by search of COSMIN, PubMed, and Google, (ii) patient 
interviews recorded and transcribed word-for-word, (iii) clinician interviews 
transcribed likewise, and (iv) 100 patient telephone interviews with notes 
taken. After familiarization, the collected expressions were labelled 
inductively in categories and assembled in tables (case and theme-based 
matrices).
RESULTS: Descriptors fell into 12 categories: intensity (slight/strong), 
evaluative (negligible/unbearable), cognitive impact (distracting/can be 
ignored), activity impact (limits some/all activity), sleep impact (can/cannot 
sleep), examples (like stubbing a toe), physical signs (crying/writhing), 
associated symptoms (nauseating/tiring), treatment (ice helps/need morphine), 
affective (annoying/dreadful), discriminative (aching/piercing), and general 
recovery (hindering recovery/functional interference). Many visual cues were 
also identified. Literature and recorded interviews gave rise to the categories, 
and telephone interviews found saturation, providing no further categories.
CONCLUSION: Pain intensity is expressed by terms that fall into 12 categories 
and by a variety of graphic elements. This advances development of a 
patient-reported outcome measure of pain intensity for orthopedic trials.

DOI: 10.2340/17453674.2024.42182
PMID: 39508169 [Indexed for MEDLINE]


4. Circ Cardiovasc Imaging. 2024 Nov 7:e016815. doi: 
10.1161/CIRCIMAGING.124.016815. Online ahead of print.

Prognostic Value of Coronary Flow Capacity by (82)Rb PET in Patients With 
Suspected Coronary Artery Disease and Normal Myocardial Perfusion at 
Semiquantitative Imaging Analysis.

Zampella E(1), Assante R(1), D'Antonio A(1), Mannarino T(1), Gaudieri V(1), 
Nappi C(1), Arumugam P(2), Panico M(3), Buongiorno P(1), Petretta M(4), Cuocolo 
A(1), Acampa W(1).

Author information:
(1)Department of Advanced Biomedical Sciences, University Federico II, Naples, 
Italy (E.Z., R.A., A.D., T.M., V.G., C.N., P.B., A.C., W.A.).
(2)Department of Nuclear Medicine, Central Manchester Foundation Trust, 
Manchester, United Kingdom (P.A.).
(3)Institute of Biostructure and Bioimaging, National Research Council, Naples, 
Italy (M. Panico).
(4)Institute for Research and Healthcare SYNLAB SDN, Diagnostic Imaging, Naples, 
Italy (M. Petretta).

BACKGROUND: Coronary flow capacity (CFC) is a measure that integrates hyperemic 
myocardial blood flow and myocardial flow reserve to quantify the 
pathophysiological impact of coronary artery disease on vasodilator capacity. We 
assessed the prognostic value of CFC derived from 82Rb positron emission 
tomography/computed tomography in patients with suspected coronary artery 
disease and normal myocardial perfusion imaging.
METHODS: We studied 1967 patients with suspected coronary artery disease and 
normal myocardial perfusion at the semiquantitative analysis of stress/rest 
cardiac 82Rb positron emission tomography/computed tomography imaging. Coronary 
artery calcium scores were calculated and categorized into 3 groups: 0, 0.1 to 
99.9, and ≥100. Patients were classified as having myocardial steal, severely 
reduced CFC, moderately reduced CFC, mildly reduced CFC, minimally reduced CFC, 
or normal flow using previously defined thresholds. The outcome end points were 
myocardial infarction and cardiac death, whichever occurred first.
RESULTS: During a mean time of 41±27 months, 49 events occurred (2.5% cumulative 
event rate, with an annualized event rate of 0.5% person-years). At 
multivariable Cox analysis, coronary artery calcium score categories and 
impaired CFC resulted as independent predictors of events (both P<0.001). The 
annualized event rate was higher in patients with impaired CFC compared with 
those with normal CFC (P<0.05). Kaplan-Meier analysis showed that patients with 
impaired CFC were at the highest risk of events.
CONCLUSIONS: In patients with suspected coronary artery disease and normal 
myocardial perfusion, impaired CFC is associated with a higher risk of cardiac 
events. Evaluating CFC can help identify patients' candidates for additional 
therapies to prevent future events.

DOI: 10.1161/CIRCIMAGING.124.016815
PMID: 39508096


5. Palliat Support Care. 2024 Nov 7:1-9. doi: 10.1017/S1478951524001445. Online 
ahead of print.

Behavioral activation program for reducing depressive symptoms among the 
bereaved of cancer patients: A feasibility and preliminary effectiveness study 
in Japan.

Asai M(1)(2)(3)(4)(5), Ogawa Y(6), Hirayama T(6)(7), Sukigara N(2), Yoshikawa 
E(1)(2), Furutani S(8), Fujimori M(3), Akechi T(9)(10), Suzuki S(11).

Author information:
(1)Department of Medical Psychology, Nippon Medical School, Tokyo, Japan.
(2)Department of Student Counseling, Nippon Medical School, Tokyo, Japan.
(3)Division of Supportive Care, Survivorship and Translational Research, 
National Cancer Center Institute for Cancer Control, Tokyo, Japan.
(4)Graduate School of Clinical Psychology, Teikyo Heisei University, Tokyo, 
Japan.
(5)Faculty of Pharma-Sciences, Teikyo University, Tokyo, Japan.
(6)Psycho-Oncology Division, National Cancer Center Hospital, Tokyo, Japan.
(7)Kokoro Support Clinic, Tokyo, Japan.
(8)NPO Pancreatic Cancer Action Network, Chiba, Japan.
(9)Department of Psychiatry and Cognitive-Behavioral Medicine, Nagoya City 
University Graduate School of Medical Sciences, Aichi, Japan.
(10)Division of Palliative Care and Psycho-oncology, Nagoya City University 
Hospital, Aichi, Japan.
(11)Faculty of Human Sciences, Waseda University, Saitama, Japan.

OBJECTIVES: This study aimed to examine the feasibility and preliminary 
effectiveness of a behavioral activation (BA) program for the bereaved of cancer 
patients toward reducing depressive symptoms.
METHODS: The BA program for the bereaved was a partially modified version for 
cancer patients. This program encompassed a preinterview and seven 50-minute 
sessions every 1-2 weeks, using worksheets, with homework assignments each day. 
To examine feasibility, the completion rates of intervention and 3 months of 
follow-up were examined. To examine the preliminary effectiveness, psychological 
symptoms were assessed with the Patient Health Questionnaire (PHQ-9; primary 
outcome) and Beck Depression Inventory-II (BDI-II) for depression and the 
Generalized Anxiety Disorder-7 (GAD-7) for anxiety. These were evaluated 3 
times: before, immediately after, and 3-month post-intervention. Non-parametric 
tests were used for comparison of scores at 3 time points and calculation of 
effect size.
RESULTS: Of the 42 bereaved who were contacted, 21 were eligible and 20 were 
participated, while 19 and 18 were in the completed intervention and completed 
3-month post-intervention categories (intervention completion rate was 95% and 
follow-up completion rate was 90%). PHQ-9, BDI-II, and GAD-7 showed significant 
reductions immediately and 3 months after the intervention compared to 
pre-intervention, and the effect sizes were all large after 3 months, although 
they were less than immediately after (PHQ-9: 0.89, 0.71; BDI-II: 0.88, 0.67; 
GAD-7: 0.57, 0.53).
SIGNIFICANCE OF RESULTS: This study indicated that the BA program for the 
bereaved of cancer patients was feasible and effective vis-à-vis reducing 
depressive symptoms.

DOI: 10.1017/S1478951524001445
PMID: 39508087