Psychoactive Plant Database - Neuroactive Phytochemical Collection

1. Int Immunopharmacol. 2024 Dec 5;142(Pt A):112996. doi: 
10.1016/j.intimp.2024.112996. Epub 2024 Sep 6.

Vasicine attenuates atherosclerosis via lipid regulation, inflammation 
inhibition, and autophagy activation in ApoE(-/-) mice.

Sun Y(1), Zhu D(1), Kong L(1), Du W(1), Qu L(1), Yang Y(2), Rao G(1), Huang 
F(3), Tong X(4).

Author information:
(1)College of Pharmaceutical Science, Yunnan University of Chinese Medicine, 
Kunming 650500, People's Republic of China.
(2)Zhaotong Hospital of Chinese Traditional Medicine, Zhaotong 657000, People's 
Republic of China.
(3)College of Pharmaceutical Science, Yunnan University of Chinese Medicine, 
Kunming 650500, People's Republic of China; School of Chinese Materia Medica and 
Yunnan Key Laboratory of Southern Medicinal Utilization, Yunnan University of 
Chinese Medicine, Kunming 650500, People's Republic of China. Electronic 
address: fenghuang_ynutcm@163.com.
(4)College of Pharmaceutical Science, Yunnan University of Chinese Medicine, 
Kunming 650500, People's Republic of China; The First Affiliated Hospital of 
Yunnan University of Chinese Medicine, Kunming 650021, People's Republic of 
China. Electronic address: xiaoyuntong_ynutcm@163.com.

Atherosclerosis is marked with the accumulation of low-density lipoproteins and 
chronic inflammation. The anti-inflammatory therapies exert protective effects 
on atherosclerosis. Vasicine is a bioactive alkaloid with anti-inflammatory 
activity from a medicinal plant in Ayurveda and Unani. In this study, the 
effects of vasicine were evaluated on atherosclerosis in vivo and in vitro. The 
results showed that vasicine alleviated atherosclerotic lesions and regulated 
the lipid synthesis by reducing the levels of TC, TG, LDL-C and inhibiting the 
expresses of scavenger receptors (SR-A, CD36 and LOX-1) to inhibit foam cell 
formations. And vasicine decreased the levels of IL-1β, IL-6, MCP-1, and TNF-α 
to modulate inflammatory response. Besides, vasicine downregulated MAPK and 
PI3K/AKT/mTOR pathway to activated autophagy, which inhibited the procession of 
atherosclerosis.

Copyright © 2024 Elsevier B.V. All rights reserved.

DOI: 10.1016/j.intimp.2024.112996
PMID: 39243558 [Indexed for MEDLINE]

Conflict of interest statement: Declaration of competing interest The authors 
declare that they have no known competing financial interests or personal 
relationships that could have appeared to influence the work reported in this 
paper.


2. J Ethnopharmacol. 2024 Sep 15;331:118345. doi: 10.1016/j.jep.2024.118345. Epub
 2024 May 14.

Identification of hydroxyquinazoline alkaloids from Justicia adhatoda L. leaves, 
a traditional natural remedy with NF-κB and AP-1-mediated anti-inflammatory 
properties and antioxidant activity.

Peron G(1), Prasad Phuyal G(2), Hošek J(3), Adhikari R(4), Dall'Acqua S(5).

Author information:
(1)Department of Molecular and Translational Medicine (DMMT), University of 
Brescia, viale Europa 11, 25123, Brescia, Italy; Research Centre for Applied 
Science and Technology (RECAST), Tribhuvan University, Kiritipur, 44613, 
Kathmandu, Nepal. Electronic address: gregorio.peron@unibs.it.
(2)Research Centre for Applied Science and Technology (RECAST), Tribhuvan 
University, Kiritipur, 44613, Kathmandu, Nepal. Electronic address: 
gangaprasadphuyal@gmail.com.
(3)Veterinary Research Institute, Hudcova 296/70, CZ-621 00, Brno, Czech 
Republic; Department of Molecular Pharmacy, Faculty of Pharmacy, Masaryk 
University, Palackého tř. 1946/1, CZ-612 00, Brno, Czech Republic. Electronic 
address: jan.hosek@vri.cz.
(4)Research Centre for Applied Science and Technology (RECAST), Tribhuvan 
University, Kiritipur, 44613, Kathmandu, Nepal; Central Department of Chemistry, 
Tribhuvan University, Kiritipur, 44613, Kathmandu, Nepal. Electronic address: 
rameshwar.adhikari@cdc.tu.edu.np.
(5)Department of Pharmaceutical and Pharmacological Sciences, University of 
Padova, via Marzolo 5, 35131, Padova, Italy. Electronic address: 
stefano.dallacqua@unipd.it.

ETHNOPHARMACOLOGICAL RELEVANCE: Justicia adhatoda L. is used as traditional 
medicine in Nepal to treat cough, asthma, and inflammatory disorders, and is 
indicated as "Asuro". Leaves are used worldwide as herbal medicine due to 
cardiotonic, expectorant, anti-asthmatic, and bronchodilatory properties. The 
aim of this work was to study the phytochemical composition of leaves of 
Nepalese J. adhatoda and assess their anti-inflammatory and antioxidant 
properties in vitro.
MATERIALS AND METHODS: Secondary metabolites were extracted from dried leaves 
using methanol (JAME: J. adhatoda methanol extract). They were analysed by means 
of liquid chromatography coupled with multiple-stage mass spectrometry (LC-MSn). 
Anti-inflammatory potential was determined by the NF-κB and AP-1 inhibition 
assay, and DPPH, ABTS, and β-carotene bleaching assays were performed to assess 
its antioxidant properties.
RESULTS: JAME is a rich source of secondary metabolites, especially quinazoline 
alkaloids such as vasicine, vasicinone, vasicoline, and adhatodine. 7-Hydroxy 
derivatives of peganidine, vasicolinone, and adhatodine were also identified by 
means of MSn data and are here reported in J. adhatoda for the first time. JAME 
inhibited NF-κB and AP-1 expression in THP-1 cells to a greater extent than the 
positive control prednisolone. A moderate radical-quenching property was 
observed in DPPH and ABTS assays, but the anti-carotene bleaching activity was 
significantly higher than the reference BHT.
CONCLUSIONS: To the best of our knowledge, this is the first insight into the 
phytochemical composition of Asuro leaves from Nepal and their bioactivity. Our 
results will contribute to the valorisation of this medicinal species still 
widely used in the traditional and complementary medicine.

Copyright © 2024 The Author(s). Published by Elsevier B.V. All rights reserved.

DOI: 10.1016/j.jep.2024.118345
PMID: 38754645 [Indexed for MEDLINE]

Conflict of interest statement: Declaration of competing interest The authors 
declare that they have no known competing financial interests or personal 
relationships that could have appeared to influence the work reported in this 
paper.


3. Heliyon. 2024 Feb 8;10(4):e25727. doi: 10.1016/j.heliyon.2024.e25727. 
eCollection 2024 Feb 29.

Exploring the pharmacological and chemical aspects of pyrrolo-quinazoline 
derivatives in Adhatoda vasica.

Khandelwal P(1), Wadhwani BD(1), Rao RS(1), Mali D(1), Vyas P(1), Kumar T(1), 
Nair R(2).

Author information:
(1)Department of Chemistry, Mohanlal Sukhadia University, Udaipur, 313001, 
Rajasthan, India.
(2)Department of Chemistry, S.S. Jain Subodh P.G. College, Jaipur, 302004, 
Rajasthan, India.

Adhatoda or Justicia is one of the biggest and complex genera of the Acanthaceae 
family. Adhatoda vasica is commonly known as 'Adosa'. It is an ayurvedic 
medicine with a medicinal history of more than a thousand years in India. 
Traditionally, it is used to treat cough, asthma, phlegm, bleeding hemorrhoids, 
for both adults and youth. This plant possesses antiarthritis, antiseptic, 
antimicrobial, anti-tuberculosis, anti-inflammatory and abortifacient 
properties. Alkaloids are the major phytoconstituents present in the plant in 
the form of pyrrolo-quinazoline derivatives viz vasicine, vasicinone, vasicinol, 
adhatodine, adhatodinine, adhavasinone and anisotine etc. The asserted 
objectives are to conduct a systematic review on the phytochemistry, 
pharmacology and traditional uses of A. vasica, as well as highlighting the 
challenges found in the research. This will promote the utilization of A. vasica 
at extract level and further development of new drug leads based on the 
compounds isolated and used for treatment of various ailments. The present 
review covers the literature survey from 1888 to 2023. The relevant data has 
been collected from various peer-reviwed journals, and books via Sci-Finder, 
PubMed, Science Direct, Google Scholar, EBSCO, online electronic journals, 
SpringerLink and Wiley. This paper aims to present a systematic review of known 
traditional applications, pharmacological and chemical aspects in Adhatoda 
vasica.

© 2024 Published by Elsevier Ltd.

DOI: 10.1016/j.heliyon.2024.e25727
PMCID: PMC10877266
PMID: 38379997

Conflict of interest statement: The authors declare the following financial 
interests/personal relationships which may be considered as potential competing 
interests:Barkha Darra Wadhwani reports financial support was provided by 
10.13039/100022833India Ministry of Science & Technology Department of Science 
and Technology. Poonam Khandelwal reports administrative support was provided by 
10.13039/501100004541Ministry of Education and 10.13039/501100020970SPD-RUSA 
Rajasthan. If there are other authors, they declare that they have no known 
competing financial interests or personal relationships that could have appeared 
to influence the work reported in this paper.


4. Curr Pharm Des. 2024;30(7):552-563. doi: 10.2174/0113816128278324240115104615.

A New Cell Model Overexpressing sTGFBR3 for Studying Alzheimer's Disease In 
vitro.

Chen J(1), Zhou L(1), Zhao Q(1), Qi Z(1).

Author information:
(1)General Hospital of Northern Theatre Command, Bei Fang Hospital of Shenyang 
Pharmaceutical University, Shenyang, China.

BACKGROUND: Recent studies have suggested that abnormal microglial 
hyperactivation has an important role in the progression of Alzheimer's disease 
(AD). sTGFBR3 (a shed extracellular domain of the transforming growth factor 
type III receptor) is a newly identified target of microglia polarization 
dysregulation, whose overexpression can cause abnormal accumulation of 
transforming growth factor β1 (TGF-β1), promoting Aβ, tau, and neuroinflammatory 
pathology.
OBJECTIVE: The objective of this study is to develop and validate a new cell 
model overexpressing sTGFBR3 for studying AD in vitro.
METHODS: BV2 cells (a microglial cell derived from C57/BL6 murine) were used as 
a cell model. Cells were then treated with different concentrations of 
lipopolysaccharide (LPS) (0, 1, or 0.3 μg/mL) for 12, 24, or 48h and then with 
or without sodium pervanadate (100 μM) for 30 min. Next, the effect surface 
optimization method was used to determine optimal experimental conditions. 
Finally, the optimized model was used to assess the effect of ZQX series 
compounds and vasicine on cell viability and protein expression. Expression of 
TGFBR3 and TNF-α was assessed using Western blot. MTT assay was used to assess 
cell viability, and enzyme- linked immunosorbent assay (ELISA) was employed to 
evaluate extracellular TGF-β1 and sTGFBR3.
RESULTS: LPS (0.3 μg/mL) treatment for 11 h at a cell density of 60% and 
pervanadate concentration (100 μM) incubation for 30 min were the optimal 
experimental conditions for increasing membrane protein TGFBR3 overexpression, 
as well as extracellular sTGFBR3 and TGF-β1. Applying ZQX-5 and vasicine 
reversed this process by reducing extracellular TGF-β1, promoting the 
phosphorylation of Smad2/3, a protein downstream of TGF-β1, and inhibiting the 
release of the inflammatory factor TNF-α.
CONCLUSION: This new in vitro model may be a useful cell model for studying 
Alzheimer's disease in vitro.

Copyright© Bentham Science Publishers; For any queries, please email at 
epub@benthamscience.net.

DOI: 10.2174/0113816128278324240115104615
PMID: 38362698 [Indexed for MEDLINE]


5. Sci Rep. 2024 Feb 14;14(1):3736. doi: 10.1038/s41598-024-54470-6.

Molecular docking of bioactive compounds extracted and purified from selected 
medicinal plant species against covid-19 proteins and in vitro evaluation.

Khanum A(1), Bibi Y(2), Khan I(3), Mustafa G(3), Attia KA(4), Mohammed AA(4), 
Yang SH(5), Qayyum A(6).

Author information:
(1)Department of Biology, PMAS-Arid Agriculture University Rawalpindi, 
Rawalpindi, 46300, Pakistan.
(2)Department of Botany, Rawalpindi Women University, Rawalpindi, 46300, 
Pakistan. yamin.bibi@f.rwu.edu.pk.
(3)Department of Plant Sciences, Quaid-I-Azam University, Islamabad, 45320, 
Pakistan.
(4)Department of Biochemistry, College of Science, King Saud University, P.O. 
Box 2455, 11451, Riyadh, Saudi Arabia.
(5)Department of Biotechnology, Chonnam National University, Yeosu, 59626, 
Republic of Korea. ymichigan@chonnam.ac.kr.
(6)Department of Agronomy, The University of Haripur, Haripur, 22620, Pakistan. 
aqayyum@uoh.edu.pk.

Bioactive compounds are secondary metabolites of plants. They offer diverse 
pharmacological properties. Peganum harmala is reported to have pharmaceutical 
effects like insecticidal, antitumor, curing malaria, anti-spasmodic, 
vasorelaxant, antihistaminic effect. Rosa brunonii has medicinal importance in 
its flower and fruits effective against different diseases and juice of leaf is 
reported to be applied externally to cure wounds and cuts. Dryopteris ramosa 
aqueous leaf extract is used to treat stomach ulcers and stomachaches. Each of 
these three medicinal plants have been indicated to have anticancer, antiviral, 
antioxidant, cytotoxic and antifungal effects but efficacy of their bioactive 
compounds remained unexplored. Study was aimed to explore In-vitro and In-silico 
anticancer, antiviral, antioxidant, cytotoxic and antifungal effects of 
bioactive compounds of above three medicinal plants. DPPH and ABTS assay were 
applied for assessment of antioxidant properties of compounds. Antibacterial 
properties of compounds were checked by agar well diffusion method. Brine shrimp 
lethality assay was performed to check cytotoxic effect of compounds. Molecular 
docking was conducted to investigate the binding efficacy between isolated 
compounds and targeted proteins. The compound isomangiferrin and tiliroside 
presented strong antioxidant potential 78.32% (± 0.213) and 77.77% (± 0.211) 
respectively in DPPH assay while harmaline showed 80.71% (± 0.072) at 200 µg/mL 
in ABTS assay. The compound harmine, harmaline and PH-HM 17 exhibited highest 
zone of inhibition 22 mm, 23 mm, 22 mm respectively against Xanthomonas while 
Irriflophenone-3-C-β- D-glucopyranoside showed maximum zone of inhibition 34 mm 
against E. coli. The compound isomangiferrin and vasicine contained strong 
antibacterial activity 32 mm and 22 mm respectively against S. aureus. The 
compound mangiferrin, astragalin, tiliroside, quercitin-3-O-rhamnoside showed 
maximum inhibitory zone 32 mm, 26 mm, 24 mm and 22 mm respectively against 
Klebsiella pneumoniae. Highest cytotoxic effect was observed by compound 
tiliroside i.e. 95% with LD50 value 73.59 µg/mL. The compound tiliroside showed 
the best binding mode of interaction to all targeted proteins presenting maximum 
hydrophobic interactions and hydrogen bonds. The binding affinity of tiliroside 
was - 17.9, - 14.9, - 14.6, - 13.8, - 12.8 against different proteins 6VAR, 
5C5S, IEA3, 2XV7 and 6LUS respectively. Bioactive compounds are significant 
natural antioxidants, which could help to prevent the progression of various 
diseases caused by free radicals. Based on molecular docking we have concluded 
that phytochemicals can have better anticancer and antiviral potential.

© 2024. The Author(s).

DOI: 10.1038/s41598-024-54470-6
PMCID: PMC10866962
PMID: 38355953 [Indexed for MEDLINE]

Conflict of interest statement: The authors declare no competing interests.